Cosmetic composition for improving skin elasticity or reducing pore size comprising amphiphilic biocompatible polymer
Patent Information
- Application Number
- PCT/KR2026/002941
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2025-02-21
- Filing Date
- 2026-02-23
- Publication Date
- 2026-08-27
Smart Images

Figure KR2026002941_27082026_PF_FP_ABST
Abstract
Description
Cosmetic composition for improving skin elasticity or shrinking pores containing an amphiphilic biocompatible polymer
[0001] The present invention relates to a cosmetic composition for improving skin elasticity or reducing pores, comprising an amphiphilic biocompatible polymer. Specifically, the present invention relates to a cosmetic composition having efficacy in improving skin elasticity or reducing pores, comprising an amphiphilic biocompatible polymer having a hydrophilic biocompatible polymer block and a hydrophobic biocompatible polymer block.
[0002] The skin is divided into the epidermis, dermis, and subcutaneous layer, and pores are openings through which hair grows and are connected to sebaceous glands. The diameter of pores is approximately 0.02 mm to 0.05 mm, but it can increase due to surrounding environmental factors such as the season. Pores exist on the skin of the entire body, excluding the palms, soles, and lips, and are mainly distributed on the face and neck.
[0003] Pores expand with age. Skin aging affects the degeneration or reduction of collagen and elastic fibers, which play a role in supporting the pores. As the fibers supporting the pores decrease, the pores expand.
[0004] Collagen, an extracellular matrix protein found in the skin's connective tissue within the dermis, is known to account for approximately 30% of the biological proteins in mammals and is primarily distributed in muscles, cartilage, and bones. The polypeptide chain of collagen consists of three amino acid residues: glycine, proline, and hydroxyproline, and 19 types of collagen have been studied to date. While adult skin contains types I through IV collagen, type I collagen accounts for 90% of the dermis. Collagen plays a role in maintaining skin connective tissue, thereby providing strength and tensile strength to the skin. Newly synthesized procollagen undergoes enzymatic reactions and is secreted into the extracellular space of skin cells to form collagen fibers, which then support the pores.
[0005] Collagen is known as a key component that provides elasticity to the skin, along with elastin, which accounts for approximately 70% to 80% of the skin's total dry weight. Collagen's biosynthesis is reduced or its degradation is accelerated due to internal factors, such as the decline in cellular activity associated with natural aging, as well as external factors, such as increased stress in various harmful environments or an increase in reactive oxygen species caused by sunlight, which lead to pore enlargement. Enlarged pores are not only a cosmetic issue but can also serve as a pathway for bacterial invasion, potentially increasing the risk of skin problems. Therefore, there is a need for research and development on cosmetic compositions that can effectively improve the number and area of pores.
[0006] One objective of the present invention is to provide a cosmetic composition for improving skin elasticity or reducing pores, comprising an amphiphilic biocompatible polymer.
[0007] The present invention provides a cosmetic composition for improving skin elasticity or reducing pores, comprising a hydrophilic biocompatible polymer block formed from a hydrophilic biocompatible polymer and a hydrophobic biocompatible polymer block formed from a hydrophobic biocompatible polymer, and an amphiphilic biocompatible polymer having a molecular weight of 500 g / mol to 15,000 g / mol, wherein the molecular weight ratio of the hydrophilic biocompatible polymer block and the hydrophobic biocompatible polymer block is 1:1 to 10:1.
[0008] In some embodiments, the molecular weight ratio of the hydrophilic biocompatible polymer block and the hydrophobic biocompatible polymer block may be 2:1 to 5:1.
[0009] In some embodiments, the polymerization ratio of the hydrophilic biocompatible polymer and the hydrophobic biocompatible polymer may be 1:1 to 15:1.
[0010] In some embodiments, the polymerization ratio of the hydrophilic biocompatible polymer and the hydrophobic biocompatible polymer may be 2:1 to 8:1.
[0011] In some embodiments, the molecular weight of the amphiphilic biocompatible polymer may be 3,000 to 9,000 g / mol.
[0012] In some embodiments, the cosmetic composition may contain the amphiphilic biocompatible polymer in an amount of 0.001 volume% to 50 volume%.
[0013] In some embodiments, the amphiphilic biocompatible polymer may form vesicles within the composition.
[0014] In some embodiments, the particle size of the vesicle may be 30 μm or less.
[0015] In some embodiments, the particle size of the vesicle may be 1 μm or less.
[0016] In some embodiments, the melting point (T) of the amphiphilic biocompatible polymer m ) can be 35℃ to 65℃.
[0017] In some embodiments, the hydrophilic biocompatible polymer block may be formed from at least one hydrophilic biocompatible polymer selected from the group consisting of polyethylene glycol, polyvinyl alcohol, polyvinylpyrrolidone, poly(N-isopropylacrylamide), hyaluronic acid, dextran, derivatives thereof, and copolymers thereof.
[0018] In some embodiments, the hydrophobic biocompatible polymer block may be formed from at least one hydrophobic biocompatible polymer selected from the group consisting of polycaprolactone, polylactic acid, polyglycolic acid, poly(3-hydroxybutyrate), polydioxanone, derivatives thereof, and copolymers thereof.
[0019] In some embodiments, the amphiphilic biocompatible polymer may be a block copolymer in which the hydrophobic biocompatible polymer block is bonded to one end of the hydrophilic biocompatible polymer block.
[0020] In some embodiments, the amphiphilic biocompatible polymer may be formed by polymerizing a monomer of the hydrophobic biocompatible polymer at one end of the hydrophilic biocompatible polymer block.
[0021] In some embodiments, the amphiphilic biocompatible polymer may be a methoxypolyethylene glycol-polycaprolactone copolymer.
[0022] In some embodiments, the cosmetic composition for improving skin elasticity or shrinking pores may further include at least one selected from the group consisting of amino acids, vitamins, moisturizing ingredients, and whitening ingredients.
[0023] In some embodiments, the cosmetic composition for improving skin elasticity or shrinking pores may be provided in at least one formulation selected from the group consisting of toner, essence, serum, ampoule, mist, lotion, cream, gel, balm, oil, mask pack, stick, primer, and foundation.
[0024] The cosmetic composition for improving skin elasticity or reducing pores according to the present invention includes an amphiphilic biocompatible polymer and has the effects of promoting collagen production, inhibiting collagen degradation, inhibiting elastin degradation, and reducing the number and area of pores, thereby being effectively used for the recovery of damaged skin and for improving and preventing skin aging. In addition, it can be used to improve skin problems caused by skin dryness due to keratinization and minor burns of less than 1 degree caused by erythema.
[0025] Figure 1 is a graph of the mRNA expression levels of collagen type I in human skin fibroblasts.
[0026] Figure 2 is a graph of the content of PIP according to the composition treatment in human skin fibroblasts (Hs68).
[0027] Figure 3 is a graph of the content of MMP-1 according to the composition treatment in human skin fibroblasts.
[0028] Figure 4 is a graph of the elastase content according to the composition treatment in human skin fibroblasts.
[0029] Figure 5 is an optical microscope image of H&E staining according to the composition treatment in an artificial skin tissue model.
[0030] Figure 6 is an optical microscope image of MT staining according to the composition treatment in an artificial skin tissue model.
[0031] Figure 7 is a graph of collagen density according to composition treatment in an artificial skin tissue model.
[0032] Figure 8 is a graph of the number of pores on the skin according to treatment with the composition alone and treatment with microneedles in combination.
[0033] Figure 9 is a graph of the average pore area of the skin according to treatment with the composition alone and treatment with microneedles in combination.
[0034] FIG. 10 shows Antera 3D on skin pores treated with the composition alone. ® This is a CS image.
[0035] Fig. 11 shows Antera 3D on skin pores according to combined treatment with the composition and microneedles. ® This is a CS image.
[0036] Hereinafter, embodiments and examples of the present invention are described in detail with reference to the attached drawings so that those skilled in the art can easily implement the present invention. However, the present invention may be embodied in various forms and is not limited to the embodiments and examples described herein.
[0037] Throughout this specification, when a part is described as "comprising" a certain component, this means that, unless specifically stated otherwise, it does not exclude other components but may include additional components.
[0038]
[0039] A cosmetic composition for improving skin elasticity or reducing pores according to one embodiment of the present invention comprises a hydrophilic biocompatible polymer block formed from a hydrophilic biocompatible polymer and a hydrophobic biocompatible polymer block formed from a hydrophobic biocompatible polymer, and an amphiphilic biocompatible polymer having a molecular weight of 500 g / mol to 15,000 g / mol. The molecular weight ratio of the hydrophilic biocompatible polymer block and the hydrophobic biocompatible polymer block is 1:1 to 10:1.
[0040] The molecular weight ratio of the hydrophilic biocompatible polymer block and the hydrophobic biocompatible polymer block is 1:1 to 10:1. Within the molecular weight ratio range of the hydrophilic block and the hydrophobic block, the length or size of the hydrophilic portion and the hydrophobic portion of the amphiphilic biocompatible polymer can be controlled in an appropriate ratio to effectively form vesicles. Furthermore, as the length or size of the hydrophilic portion and the hydrophobic portion is controlled in an appropriate ratio, the effects of inhibiting the secretion of collagen-degrading enzymes and elastases, promoting collagen production, reducing the number of pores, and shrinking the pore area can be enhanced. For example, the molecular weight ratio of the hydrophilic biocompatible polymer block and the hydrophobic biocompatible polymer block may be 1:1 to 8:1, 1:1 to 6:1, 1:1 to 5:1, 2:1 to 10:1, 2:1 to 8:1, 2:1 to 6:1, 2:1 to 5:1, 3:1 to 10:1, 3:1 to 3:1, 3:1 to 6:1, or 3:1 to 5:1.
[0041] For example, when a sufficient amount of monomer of a hydrophobic biocompatible polymer is reacted with a hydrophilic biocompatible polymer having a specific molecular weight, a hydrophobic biocompatible polymer block may be formed at one end of a block formed from the hydrophilic biocompatible polymer. The approximate molecular weight of the total amphiphilic biocompatible polymer may be defined as the sum of the molecular weight of the hydrophilic biocompatible polymer block and the molecular weight of the hydrophobic biocompatible polymer block, and the approximate molecular weight of the hydrophobic biocompatible polymer block may be defined as the value obtained by subtracting the molecular weight of the hydrophilic biocompatible polymer block from the molecular weight of the total amphiphilic biocompatible polymer. The molecular weight may have an error corresponding to the molecular weight of hydrogen cations, hydroxide ions, etc., that are dropped or added during the reaction process.
[0042] In some embodiments, the molecular weight ratio of the hydrophilic biocompatible polymer block and the hydrophobic biocompatible polymer block may be 2:1 to 5:1.
[0043] In some embodiments, the polymerization ratio of the hydrophilic biocompatible polymer and the hydrophobic biocompatible polymer may be 1:1 to 15:1. In one embodiment, the polymerization ratio of the hydrophilic biocompatible polymer and the hydrophobic biocompatible polymer may be 2:1 to 8:1. Preferably, the polymerization ratio may be 2:1 to 4:1. Within the range of the polymerization ratio, the length or size of the hydrophilic portion and the hydrophobic portion of the amphiphilic biocompatible polymer can be controlled in an appropriate ratio to effectively form vesicles. Furthermore, as the length or size of the hydrophilic portion and the hydrophobic portion are controlled in an appropriate ratio, the effects of inhibiting the secretion of collagen-degrading enzymes and elastases, promoting collagen production, reducing the number of pores, and shrinking the pore area of the amphiphilic biocompatible polymer may be enhanced.
[0044] The molecular weight of the above amphiphilic biocompatible polymer is 500 g / mol to 15,000 g / mol. For example, the molecular weight of the amphiphilic biocompatible polymer is 500 g / mol to 12,000 g / mol, 500 g / mol to 10,000 g / mol, 500 g / mol to 9,000 g / mol, 1,000 g / mol to 15,000 g / mol, 1,000 g / mol to 12,000 g / mol, 1,000 g / mol to 10,000 g / mol, 1,000 g / mol to 9,000 g / mol, 1,500 g / mol to 15,000 g / mol, 1,500 g / mol to 12,000 g / mol, 1,500 g / mol to 10,000 g / mol, 1,500 g / mol to 9,000 g / mol, and 2,000 g / mol. It may be up to 15,000 g / mol, 2,000 g / mol to 12,000 g / mol, 2,000 g / mol to 10,000 g / mol, 2,000 g / mol to 9,000 g / mol, 2,500 g / mol to 15,000 g / mol, 2,500 g / mol to 12,000 g / mol, 2,500 g / mol to 10,000 g / mol, 2,500 g / mol to 9,000 g / mol, 3,000 g / mol to 15,000 g / mol, 3,000 g / mol to 12,000 g / mol, 3,000 g / mol to 10,000 g / mol, or 3,000 g / mol to 9,000 g / mol. Within the above molecular weight range, the amphiphilic biocompatible polymer can easily form vesicles and exhibit excellent inhibition of collagen-degrading enzyme and elastase secretion, promotion of collagen production, reduction of pore number, and reduction of pore area.
[0045] In some embodiments, the cosmetic composition may contain the amphiphilic biocompatible polymer in an amount of 0.001 volume% to 50 volume%. In some embodiments, the amphiphilic biocompatible polymer is 0.005 volume% to 50 volume%, 0.01 volume% to 50 volume%, 0.02 volume% to 50 volume%, 0.001 volume% to 40 volume%, 0.005 volume% to 40 volume%, 0.01 volume% to 40 volume%, 0.02 volume% to 40 volume%, 0.001 volume% to 30 volume%, 0.005 volume% to 30 volume%, 0.01 volume% to 30 volume%, 0.02 volume% to 30 volume%, 0.001 volume% to 20 volume%, 0.005 volume% to 20 volume%, 0.01 volume% to 20 volume%, 0.02 volume% to 20 volume%, 0.001 volume% to 10 It may be included in volume%, 0.005 volume% to 10 volume%, 0.01 volume% to 10 volume%, 0.02 volume% to 10 volume%, 0.001 volume% to 5 volume%, 0.005 volume% to 5 volume%, 0.01 volume% to 5 volume%, or 0.02 volume% to 5 volume%. In this case, the effects of inhibiting the secretion of collagen-degrading enzymes and elastases, promoting collagen production, reducing the number of pores, and shrinking the pore area may be enhanced.
[0046] In some embodiments, the cosmetic composition may contain the amphiphilic biocompatible polymer in an amount of 0.1% to 50% by weight. In some embodiments, the concentration of the amphiphilic biocompatible polymer in the composition may preferably be 5% to 40% by weight. In this case, the effects of inhibiting the secretion of collagen-degrading enzymes and elastases, promoting collagen production, reducing the number of pores, and reducing the pore area may be enhanced.
[0047] In some embodiments, the amphiphilic biocompatible polymer may form vesicles within the composition. The vesicles may increase collagen production on their own. Additionally, the vesicles may inhibit collagen-degrading enzymes (MMP-1) on their own. Additionally, the vesicles may inhibit elastase on their own. Accordingly, a composition containing the amphiphilic biocompatible polymer may effectively improve pore area or prevent pore enlargement.
[0048] The above-mentioned vesicle may include micelles, microvesicles, liposomes, polymerosomes, etc. The micelles may include normal-phase micelles or reverse-phase micelles. For example, the amphiphilic biocompatible polymer may have hydrophilic and hydrophobic blocks and form a double layer or double membrane to form a spherical vesicle. The polymerosomes may be nanometer-sized capsule-shaped structures formed by the self-assembly of polymeric materials such as amphiphilic copolymers. The polymerosomes may have a structure in which a hydrophobic shell membrane surrounds a hydrophilic nucleus. Accordingly, various drugs or compounds can be encapsulated and stably transported.
[0049] In some embodiments, the particle size of the vesicle may be 30 μm or less. In some embodiments, the particle size of the vesicle may be 25 μm or less, 20 μm or less, 15 μm or less, 10 μm or less, 5 μm or less, 3 μm or less, 2 μm or less, or 1 μm or less. In this case, the composition containing the amphiphilic biocompatible polymer may be formulated into a cosmetic composition of uniform composition, and the vesicle may penetrate the skin barrier and effectively penetrate and act within the skin.
[0050] In some embodiments, the particle size of the vesicle may be 10 nm or more, 20 nm or more, 30 nm or more, 40 nm or more, 50 nm or more, 80 nm or more, or 100 nm or more.
[0051] In some embodiments, the melting point (T) of the amphiphilic biocompatible polymer m The temperature may be 35°C to 65°C. In some embodiments, the melting point (Tm) of the amphiphilic biocompatible polymer may be 40°C to 60°C. When the melting point of the amphiphilic biocompatible polymer is within the above range, the amphiphilic biocompatible polymer does not melt during storage and use of the composition and can exhibit properties suitable for external use.
[0052] The viscosity of the composition containing the above-mentioned amphiphilic biocompatible polymer may decrease as the temperature increases.
[0053] In the present invention, "molecular weight" may be defined as number average molecular weight, weight average molecular weight, order average molecular weight, etc.
[0054] In the present invention, “hydrophilic biocompatible polymer” refers to a polymer having affinity for water-soluble solvents and biocompatibility, and is a general term for all biocompatible polymers useful to the human body that can be added to biologically active substances such as natural or artificial synthetic polymer materials, and is mainly used to improve the solubility and biocompatibility of drugs, but is not limited thereto.
[0055] In some embodiments, the hydrophilic biocompatible polymer block may be formed from at least one hydrophilic biocompatible polymer selected from the group consisting of polyethylene glycol, polyvinyl alcohol, polyvinylpyrrolidone, poly(N-isopropylacrylamide), hyaluronic acid, dextran, derivatives thereof, and copolymers thereof.
[0056] The above derivative may be one in which one or more substituents selected from alkyl, hydroxy, alkoxy, acyl, carboxy, etc. are substituted on the original compound. The alkyl, alkoxy, and acyl groups are composed of 1 to 6 carbon atoms, each C 1-6 Alkyl, C 1-6 Alkoxy and C 1-6 It may include acyl groups. For example, derivatives of polyethylene glycol may include dihydroxypolyethylene glycol, methoxypolyethylene glycol, ethoxypolyethylene glycol, polyethylene glycol-NHS ester, methoxypolyethylene glycol-succinimidyl succinate, methoxypolyethylene glycol-succinimidyl glutarate, methoxypolyethylene glycol-carboxylic acid, etc.
[0057] In the present invention, "hydrophobic biocompatible polymer" is a polymer having affinity for water-insoluble solvents and biocompatibility, and is used for the manufacture of water-insoluble pharmaceutical vehicles or hydrophobic medical materials, but is not limited thereto.
[0058] In some embodiments, the hydrophobic biocompatible polymer block may be formed from at least one hydrophobic biocompatible polymer selected from the group consisting of polycaprolactone, polylactic acid, polyglycolic acid, poly(3-hydroxybutyrate), polydioxanone, derivatives thereof, and copolymers thereof.
[0059] The above hydrophobic biocompatible polymer may be a polymer in which monomers corresponding to the polymer are polymerized. For example, the monomers may include caprolactone, lactic acid, glycolic acid, β-hydroxybutyric acid, and p-dioxanone.
[0060] In some embodiments, the amphiphilic biocompatible polymer may be a block copolymer in which the hydrophobic biocompatible polymer block is bonded to one end of the hydrophilic biocompatible polymer block.
[0061] In some embodiments, the amphiphilic biocompatible polymer may be formed by polymerizing a monomer of the hydrophobic biocompatible polymer at one end of the hydrophilic biocompatible polymer block.
[0062] In some embodiments, the amphiphilic biocompatible polymer may be a methoxypolyethylene glycol-polycaprolactone copolymer. For example, the amphiphilic biocompatible polymer may be formed by reacting a hydrophilic biocompatible polymer with a sufficient amount of monomer of a hydrophobic biocompatible polymer. For example, an mPEG-PCL copolymer may be formed by reacting methoxypolyethylene glycol of a specific molecular weight with caprolactone.
[0063] In the present invention, methoxypolyethylene glycol-polycaprolactone copolymer (mPEG-PCL) refers to a copolymer having the following structure.
[0064] [Chemical Formula 1]
[0065]
[0066] (where n is an integer from 20 to 150, and m is an integer from 10 to 50.)
[0067] The above methoxypolyethylene glycol-polycaprolactone copolymer refers to a linear diblock amphiphilic copolymer in which a block formed from methoxypolyethylene glycol, a hydrophilic component, and a block formed from polycaprolactone, a hydrophobic component, are interconnected.
[0068] In some embodiments, the cosmetic composition may be provided for promoting collagen production, inhibiting collagenase, or inhibiting elastase. In some embodiments, the cosmetic composition may exhibit effects of promoting collagen production, inhibiting collagenase, and inhibiting elastase.
[0069] In some embodiments, the cosmetic composition may be used to reduce the number and area of pores or to prevent an increase thereof.
[0070] In some embodiments, the cosmetic composition may be provided in the form of a powder, hydrogel, emulsion, ointment, cream, lotion, gel, foam, spray, patch, etc.
[0071]
[0072] In some embodiments, the cosmetic composition for improving skin elasticity or shrinking pores can aesthetically improve the appearance of the skin. In this specification, “aesthetically improved” does not mean medical or therapeutic treatment of the skin, but rather visual and tactile improvement of appearance, such as making the skin look smoother, more moist, more elastic, brighter, and more uniform by controlling the condition of the skin surface. For example, the application of the cosmetic composition can alleviate skin roughness, dryness, flaking due to dryness, dull skin tone, and uneven skin texture associated with aging, thereby making the overall appearance of the skin look aesthetically healthier.
[0073] In this specification, "improvement of skin elasticity" means providing tension to skin tissue that has lost strength and become sagging due to aging or external stimuli, and enhancing the skin's natural restorative power. The amphiphilic biocompatible polymer according to the present invention can help improve skin elasticity by promoting collagen synthesis and inhibiting collagen-degrading enzymes or elastin-degrading enzymes. In addition, based on its excellent affinity with the skin, the amphiphilic biocompatible polymer can help improve overall skin elasticity by providing elasticity to the skin structure itself or by effectively delivering other active ingredients that contribute to elasticity enhancement into the skin.
[0074] In this specification, "pore reduction" refers to visibly reducing the area and volume of pores that have become enlarged or elongated due to excessive sebum secretion, aging, or decreased skin elasticity, thereby smoothing the skin texture. The amphiphilic biocompatible polymer according to the present invention can reduce the size of enlarged pores by improving the density of skin tissue. In addition, the amphiphilic biocompatible polymer can contribute to reducing the number of large pores and the overall pore size by increasing the tension of the skin around the pores to aid in contraction, or by acting as a carrier that maximizes the penetration of related active ingredients.
[0075] In one embodiment, the cosmetic composition for improving skin elasticity or shrinking pores may further include at least one efficacy selected from the group consisting of improving skin tissue density, preventing pore enlargement, alleviating skin sagging, improving skin elasticity loss, improving skin collagen density, improving wrinkles, and preventing skin aging.
[0076] In this specification, "improvement of skin tissue density" means to make the loosened internal structure of the skin dense and firm. The amphiphilic biocompatible polymer according to the present invention can increase skin tissue density by promoting collagen synthesis and inhibiting collagen-degrading enzymes and elastin-degrading enzymes.
[0077] In this specification, "prevention of pore enlargement" refers to the effect of suppressing the phenomenon in which pores widen or sag due to aging or a decrease in skin elasticity. The amphiphilic biocompatible polymer according to the present invention can suppress the enlargement of pores by improving the density of skin tissue.
[0078] In this specification, "alleviation of skin sagging" refers to improving the phenomenon of skin sagging downward due to gravity and aging, thereby providing tension to the skin. The amphiphilic biocompatible polymer according to the present invention can increase skin elasticity and thereby suppress skin sagging.
[0079] In this specification, "improvement of skin elasticity loss" refers to the effect of restoring skin that has lost flexibility and resilience due to the external environment or aging to its original healthy state. The amphiphilic biocompatible polymer according to the present invention can inhibit the loss of skin elasticity by promoting collagen synthesis and inhibiting collagen-degrading enzymes and elastin-degrading enzymes.
[0080] In this specification, "improvement of skin collagen density" refers to the effect of improving skin volume and support by increasing the density of collagen, which is a major component of the dermal layer of the skin. The amphiphilic biocompatible polymer according to the present invention can increase the collagen density of the skin by promoting collagen synthesis and inhibiting collagenase and elastinase.
[0081] In this specification, "wrinkle improvement" refers to the effect of making the skin surface smooth by visibly alleviating fine wrinkles and deep wrinkles formed due to skin aging, etc. The amphiphilic biocompatible polymer according to the present invention can increase skin tissue density and reduce the depth and number of wrinkles.
[0082] In this specification, "anti-aging of the skin" refers to a comprehensive effect of delaying or inhibiting overall degenerative changes in the skin caused by ultraviolet rays or the passage of time. The amphiphilic biocompatible polymer according to the present invention can improve the appearance of aged skin by increasing the collagen density of the skin.
[0083]
[0084] One aspect of the present invention provides a method for improving skin elasticity or reducing pores, comprising the step of applying the cosmetic composition to a skin surface.
[0085] The above cosmetic composition may be applied by methods such as application, spraying, or attachment, but is not limited thereto.
[0086] For example, the cosmetic composition may be applied directly by hand or using tools such as brushes, cotton swabs, or sticks, or sprayed in the form of an aerosol or mist. Additionally, the cosmetic composition may be applied by being absorbed or deposited onto a substrate such as a patch or mask and adhering to the skin.
[0087] The above cosmetic composition may be applied 1 to 5 times, 1 to 4 times, 1 to 3 times, or 1 to 2 times per day. The number of daily applications may be adjusted according to the number and size of pores and the condition of the skin of the subject.
[0088] In some embodiments, the cosmetic composition may be used in conjunction with absorption-promoting treatments such as massage, microneedle treatment, chemical peeling, or microdermabrasion. In some embodiments, the treatment with the cosmetic composition and the absorption-promoting treatment may be performed simultaneously or sequentially. For example, the absorption-promoting treatment may be performed after the treatment with the cosmetic composition, or conversely, the treatment with the cosmetic composition may be performed after the absorption-promoting treatment. In this case, the effects of the cosmetic composition on promoting collagen production, inhibiting collagenase, inhibiting elastase, and improving pore condition may be enhanced.
[0089] In some embodiments, the absorption-promoting treatment may be performed for a time of 1 to 60 minutes, 1 to 40 minutes, 1 to 30 minutes, 1 to 20 minutes, 1 to 10 minutes, 1 to 5 minutes, or 1 to 3 minutes.
[0090] In some embodiments, the length of the microneedle used for the microneedle treatment may be 0.1 mm to 2 mm, 0.1 mm to 1.5 mm, 0.1 mm to 1 mm, 0.1 mm to 0.8 mm, 0.1 mm to 0.6 mm, 0.2 mm to 2 mm, 0.2 mm to 1.5 mm, 0.2 mm to 1 mm, 0.2 mm to 0.8 mm, 0.2 mm to 0.6 mm, 0.3 mm to 2 mm, 0.3 mm to 1.5 mm, 0.3 mm to 1 mm, 0.3 mm to 0.8 mm, or 0.3 mm to 0.6 mm. In this case, the intradermal absorption of the cosmetic composition may be promoted.
[0091] In some embodiments, the cosmetic composition may be applied in combination with known non-drug treatments such as high-frequency therapy, anion therapy, and argon plasma therapy. For example, non-drug treatment may be performed after the application of the cosmetic composition. In this case, the efficacy for improving the number and area of pores may be enhanced.
[0092] Additionally, the cosmetic composition according to the present invention may be applied repeatedly over a limited period. In one embodiment, the cosmetic composition may be applied for a period of 1 month to 12 months. In one embodiment, the cosmetic composition may be applied 1 to 4 times per month. In one embodiment, the cosmetic composition may be applied 1 to 4 times per week. In one embodiment, the cosmetic composition may be applied at substantially equal intervals within the application period, or in a manner that includes a rest period after intensive application. For example, it may be applied 2 to 4 times at 1-week intervals over 1 month, 1 to 3 times at 1-week intervals over 12 months, 1 to 3 times at 2-week intervals over 12 months, 1 to 3 times at 4-week intervals over 12 months, and so on.
[0093] The above cosmetic composition may be applied in an amount that can be spread evenly on the skin of a subject. The amount applied may be adjusted according to the area of the skin. For example, the above cosmetic composition may be applied in an amount of 0.1 mL to 20 mL, 0.5 mL to 15 mL, 1 mL to 10 mL, or 1 mL to 5 mL per application.
[0094] In one embodiment, the cosmetic composition may be applied in an amount of 1 g to 10 g, 1 g to 8 g, 1 g to 6 g, 1 g to 5 g, 1 g to 4 g, 1 g to 3 g, 2 g to 10 g, 2 g to 8 g, 2 g to 6 g, 2 g to 5 g, 2 g to 4 g, or 2 g to 3 g. The volume of the cosmetic composition may be applied at once in a single application or divided into several applications.
[0095] In one embodiment, the method for improving skin elasticity or reducing pores may include the step of applying the cosmetic composition to the surface of the skin; and the step of promoting the absorption of the cosmetic composition into the skin using microneedles.
[0096] In one embodiment, the microneedles may have a form selected from solid, hollow, coated, soluble, or hydrogel types. Hollow, coated, soluble, and hydrogel type microneedles may contain an active ingredient and, after insertion into the skin, release the active ingredient into the skin (e.g., stratum corneum, epidermis, dermis, etc.). The active ingredient may be supported in the hollow of the microneedles, coated on the surface of the microneedles, or mixed with a soluble or hydrogel type support to form the microneedles.
[0097] In one embodiment, the microneedle may be applied to a device selected from a pen, a roller, or a stamp.
[0098] In one embodiment, the microneedles may be integrated with a high-frequency generator. Accordingly, high frequency may be emitted during microneedle processing.
[0099] The step of promoting the absorption of the above cosmetic composition into the skin may include treating the microneedle on the skin surface (e.g., gliding, needling, stamping, rolling, etc.).
[0100] In one embodiment, the cosmetic composition may further include at least one selected from the group consisting of amino acids, vitamins, moisturizing ingredients, and whitening ingredients together with the amphiphilic biocompatible polymer.
[0101] The above amino acid may include at least one selected from the group consisting of glycine, glutamine, isoleucine, leucine, methionine, phenylalanine, serine, threonine, tryptophan, valine, alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, histidine, lysine, proline, and tyrosine.
[0102] In some embodiments, the amino acid may include at least one selected from the group consisting of glycine, glutamine, isoleucine, leucine, methionine, phenylalanine, serine, threonine, tryptophan, and valine.
[0103] The above vitamins may include components of the vitamin A, B, C, D, E, and K series, such as retinol, ascorbic acid, vitamin D, tocopherol, vitamin K, niacinamide, riboflavin, thiamine, inositol, pantothenic acid, pyridoxine, biotin, folic acid, and cobalamin.
[0104] In some embodiments, the vitamin may include at least one selected from the group consisting of niacinamide, riboflavin, thiamine, and inositol.
[0105] The above moisturizing ingredients may include, but are not limited to, glycerin, polyacrylic acid, hyaluronic acid, ceramide, aloe vera, panthenol, sodium polyacrylate, propylene glycol, butylene glycol, carboxymethylcellulose, collagen, etc.
[0106] The above whitening ingredients may include, but are not limited to, sodium pyruvate, hydroquinone, arbutin, retinoic acid, etc.
[0107] In addition, the above cosmetic composition may further include auxiliary ingredients known to have soothing and skin elasticity-improving effects, such as polynucleotides and polydeoxynucleotides.
[0108] The cosmetic composition according to the present invention may additionally include excipients, auxiliary agents, or emulsifiers, etc.
[0109] In some embodiments, the cosmetic composition may be provided in at least one formulation selected from the group consisting of toner, essence, serum, ampoule, mist, lotion, cream, gel, balm, oil, mask pack, stick, primer, and foundation.
[0110] The above amphiphilic biocompatible polymer may be biodegradable within 12 weeks, preferably within 10 weeks, and more preferably between 2 and 8 weeks.
[0111] In some embodiments, the cosmetic composition may be provided as an aqueous solution or a hydrogel. The aqueous solution may be formed by mixing or dissolving the amphiphilic biocompatible polymer in an aqueous solution (e.g., physiological saline) containing water or other components. The hydrogel may be formed by mixing the amphiphilic biocompatible polymer with a gel-like substrate.
[0112] In some embodiments, the substrate may include, but not limited to, sodium polyacrylate, carboxymethyl cellulose, sodium alginate, collagen, gelatin, hyaluronic acid, chitosan, xanthan gum, pectin, starch, cellulose, agar, polyethylene glycol, polyacrylic acid, carrageenan, glycerin, propylene glycol, etc.
[0113]
[0114] The present invention will be explained in more detail through the following examples. The following examples are for illustrative purposes only and do not limit the scope of the present invention.
[0115] Preparation Example: Preparation of MPEG-PCL copolymer
[0116] The copolymer of Preparation Example 1 (MPEG1500-PCL750) was prepared by polymerizing a polycaprolactone (PCL) hydrophobic polymer block with a molecular weight of 750 g / mol using a caprolactone monomer with 1,500 g / mol of methoxypolyethylene glycol (MPEG) as a hydrophilic polymer under a catalyst.
[0117] In the copolymer of Preparation Example 1, MPEG-PCL copolymers with various physical properties were obtained by changing the molecular weight of the hydrophilic polymer MPEG and the molecular weight of the hydrophobic polymer block PCL as shown in the table below.
[0118] Preparation Example Molecular Weight (g / mol) Hydrophilic Block:Hydrophilic Block Molecular Weight Non-copolymer Hydrophilic Block Hydrophilic Block Preparation Example 1 2,250 1,500 750 2:1 Preparation Example 2 6,000 2,000 4,000 1:2 Preparation Example 3 4,000 2,000 2,000 1:1 Preparation Example 4 3,500 2,000 1,500 1.33:1 Preparation Example 5 3,000 2,000 1,000 2:1 Preparation Example 6 6,500 2,000 500 4:1 Preparation Example 7 78,000 4,000 4,000 1:1 Preparation Example 86,000 4,000 2,000 2:1 Preparation Example 9 95,500 4,000 1,500 2.67:1 104,5004,0005008:1 Manufacturing Example 115,5004,0001,5002.67:1 Manufacturing Example 125,5005,00050010:1 Manufacturing Example 1310,0005,0005,0001:1 Manufacturing Example 147,5005,0002,5002:1 Manufacturing Example 1516,0008,0008,0001:1 Manufacturing Example 1612,0008,0004,0002:1 Manufacturing Example 1710,0008,0002,0004:1 Manufacturing Example 185504001502.67:1 Manufacturing Example 198004004001:1 Manufacturing Example 205004001004:1 Manufacturing Example 218005502502.2:1 Manufacturing Example 221,1005505501:1
[0119] Example 1: Composition containing a methoxypolyethylene glycol-polycaprolactone copolymer
[0120] An aqueous solution was prepared by adding phosphate-buffered physiological saline to the methoxypolyethylene glycol-polycaprolactone copolymers of Preparation Examples 1 to 22 so that the concentration of each copolymer was 20%, and then mixing and stirring.
[0121] Example 2: Composition containing methoxypolyethylene glycol-polycaprolactone copolymer
[0122] An aqueous solution was prepared by adding phosphate-buffered physiological saline to the methoxypolyethylene glycol-polycaprolactone copolymers of Preparation Examples 1 to 22 so that the concentration of each copolymer was 30%, and then mixing and stirring.
[0123] Example 3: Composition containing methoxypolyethylene glycol-polycaprolactone copolymer
[0124] An aqueous solution was prepared by adding phosphate-buffered physiological saline to the methoxypolyethylene glycol-polycaprolactone copolymers of Preparation Examples 1 to 22 so that the concentration of each copolymer was 40%, and then mixing and stirring.
[0125] Example 4: Composition containing methoxypolyethylene glycol-polycaprolactone copolymer
[0126] An aqueous solution was prepared by adding phosphate-buffered physiological saline to the methoxypolyethylene glycol-polycaprolactone copolymers of Preparation Examples 4, 6, 8, 9, 10, 11, 18, and 21 so that the concentration of each copolymer was 10%, and then mixing and stirring.
[0127] Example 5: Composition containing methoxypolyethylene glycol-polycaprolactone copolymer
[0128] An aqueous solution was prepared by adding phosphate-buffered physiological saline to the methoxypolyethylene glycol-polycaprolactone copolymers of Preparation Examples 4, 6, 8, 9, 10, and 11, respectively, and then mixing and stirring to achieve concentrations of 5%, 10%, 20%, 25%, 30%, and 40%.
[0129] Example 6: Composition containing methoxypolyethylene glycol-polycaprolactone copolymer
[0130] An aqueous solution was prepared by adding sterile distilled water to the methoxypolyethylene glycol-polycaprolactone copolymer of Preparation Example 8 so that the concentration was 10%, and then mixing and stirring. The aqueous solution was prepared to contain glycerin, glycine, glutamine, isoleucine, leucine, methionine, phenylalanine, serine, threonine, tryptophan, valine, polyacrylic acid, niacinamide, riboflavin, thiamine HCl, inositol, calcium chloride, magnesium sulfate, potassium chloride, sodium chloride, and sodium pyruvate.
[0131]
[0132] Experimental Example 1: Evaluation of the properties of a composition according to the polymerization ratio and molecular weight of a hydrophilic biocompatible polymer and a hydrophobic biocompatible polymer copolymer
[0133] 3 mL of the compositions prepared according to Examples 1 and 2 above were bottled into glass vials, sealed, and stored in a 25°C incubator for 7 days. Afterward, the presence of precipitate was visually determined, and compositions in which a precipitate was observed were judged to be suspensions. To confirm the sol-gel characteristics, 45 o The appearance was determined by tilting it and leaving it for 10 minutes.
[0134] For the polymerized copolymer, the molecular weight of the hydrophobic block and the ratio of the molecular weights of the hydrophobic block and the hydrophobic block were calculated as the difference between the molecular weight of the total copolymer and the molecular weight of the hydrophilic block (methoxypolyethylene glycol) used in the synthesis.
[0135] Preparation Example Molecular Weight (g / mol) Hydrophilic Block:Hydrophilic Block Appearance Precipitate Copolymer Hydrophilic Block Hydrophilic Block Hydrophilic Block Example 1 Example 2 Example 1 Example 2 Preparation Example 4 3,500 2,000 1,500 1.33:1 Sol-Gel -- Preparation Example 6 2,500 2,000 500 4:1 Sol-Gel -- Preparation Example 8 6,000 4,000 2,000 2:1 Gel-Gel -- Preparation Example 10 4,500 4,000 500 8:1 Sol-Sol -- Preparation Example 11 5,500 4,000 1,500 2.67:1 Sol-Gel -- Preparation Example 18 550 400 150 2.67:1 Sol-Sol -- Preparation Example 21 800 550 250 2.2:1 Sol-Sol --
[0136] As shown in Table 1 above, it was confirmed that among the compositions prepared according to Examples 1 and 2, the compositions containing the methoxypolyethylene glycol-polycaprolactone copolymer of Preparation Examples 4, 6, 8, 10, 11, 18, and 21 have a sol or gel formulation.
[0137] In particular, it can be seen that a copolymer having a polymerization ratio of hydrophilic biocompatible polymer and hydrophobic biocompatible polymer of 1:1 to 10:1 and a molecular weight of 1,000 to 10,000 g / mol has excellent physicochemical properties and characteristics.
[0138] Experimental Example 2: Evaluation of the properties of the composition according to the concentration of the amphiphilic biocompatible polymer
[0139] The properties according to the concentration of the compositions containing the methoxypolyethylene glycol-polycaprolactone copolymers of Preparation Examples 4, 8, 10, and 11 prepared according to the above Example 5 were compared, and the results are shown in Table 2 and Figure 2 below.
[0140] Appearance by Concentration 5% 10% 20% 25% 30% 40% Preparation Example 4 Soluble Soluble Soluble Soluble Gel Soluble Gel Soluble Preparation Example 8 Soluble Soluble Gel Soluble Gel Soluble Preparation Example 10 Soluble Soluble Soluble Gel Soluble Gel Soluble Preparation Example 11 Soluble Soluble Soluble Soluble Soluble Gel Soluble
[0141] As shown in Table 2 and Figure 2 above, it was confirmed that all compositions containing the methoxypolyethylene glycol-polycaprolactone copolymer of Preparation Example 4, Preparation Example 8, Preparation Example 10, and Preparation Example 11 at a concentration of 5% to 40% maintained a sol or gel form.
[0142] Accordingly, it can be seen that the composition of the present invention has excellent properties that allow it to be formulated into topical skin preparations such as powders, hydrogels, emulsions, ointments, and creams when the concentration of the hydrophilic biocompatible polymer and the hydrophobic biocompatible polymer copolymer is 5% to 40%.
[0143] Experimental Example 3: Evaluation of viscosity of a composition containing an amphiphilic biocompatible polymer according to temperature change
[0144] Compositions containing the methoxypolyethylene glycol-polycaprolactone copolymers of Preparation Examples 4, 8, 10, and 11 prepared according to the above Examples 1 and 3 were filled into glass containers and immersed in constant temperature water baths set to temperatures of 5°C, 20°C, 25°C, 30°C, and 35°C for 20 minutes, respectively, and then the viscosity was measured using a viscometer (VISCO B, ATAGO).
[0145] It was confirmed that the viscosity of the compositions containing the methoxypolyethylene glycol-polycaprolactone copolymers of Preparation Examples 4, 8, 10, and 11 prepared according to Examples 1 and 3 decreased as the temperature increased.
[0146] Therefore, it can be seen that the composition comprising the hydrophilic biocompatible polymer and the hydrophobic biocompatible polymer copolymer of the present invention has excellent properties that can be formulated into topical skin preparations such as powders, hydrogels, and emulsions.
[0147] Experimental Example 4: Particle Size Analysis of Amphiphilic Biocompatible Polymers
[0148] To measure the particle size of the compositions prepared according to Examples 1 and 2 above, they were classified into a group in which a precipitate is formed and a group in which a sol or gel is formed without forming a precipitate. The particle size of the compositions containing the methoxypolyethylene glycol-polycaprolactone copolymer that formed a precipitate was measured by laser diffraction and scattering using a Mastersizer 2000 (Manufacturer: MALVERN). The compositions containing the methoxypolyethylene glycol-polycaprolactone copolymer of Examples 4, 8, 10, and 11 prepared according to Example 1, which were in the form of a sol and gel without forming a precipitate, were measured by dynamic light scattering using an ELSZ-1000 (Manufacturer: OTSUKA ELECTRONICS). The results are shown in Table 4 below.
[0149] Distinction Appearance Average Particle Size (μm) Example 1 Preparation Example 4 Gel 0.857 Preparation Example 8 Gel 0.345 Preparation Example 10 Sol 0.756 Preparation Example 11 Sol 0.754
[0150] As shown in Table 4 above, it was confirmed that the compositions containing the methoxypolyethylene glycol-polycaprolactone copolymers of Preparation Examples 4, 8, 10, and 11, prepared according to Examples 1 and 2 in the form of sol and gel in which no precipitate is formed, have a small size of 10 μm or less.
[0151] Therefore, it can be seen that the composition containing the amphiphilic biocompatible polymer of the present invention has excellent properties that allow it to be formulated into topical skin preparations such as powders, hydrogels, and emulsions.
[0152] Experimental Example 5: Confirmation of the morphology of an amphiphilic biocompatible polymer
[0153] The composition of Example 1 using the copolymer of Preparation Example 8 was photographed using a scanning electron microscope (SEM).
[0154] It was confirmed that the amphiphilic biocompatible polymer in the composition of the example self-assembled to form microvesicles with a particle size of about 100 nm.
[0155] Experimental Example 6: Evaluation of Collagen RNA (Col1A1) Expression Levels
[0156] The amount of collagen mRNA (Col1A1) expression in human skin fibroblasts was evaluated for the cosmetic composition of Example 6.
[0157] Human skin fibroblasts (NHDF, Normal Human Dermal Fibroblast) at 1.0 x 10⁶ per well in a 6-well culture plate 6After dispensing into individual cells, the cells were cultured for 24 hours. After washing with phosphate-buffered saline (PBS), the composition of Example 6 was added at a concentration of 1 v / v% to a medium (EMEM, 1% P / S) that does not contain fetal bovine serum (FBS), followed by 48 hours of starvation. The untreated group was treated with PBS at the same concentration instead of the composition of Example 6. RNA was extracted from the cells according to a prescribed method using Total RNA extraction reagent (Takara Bio Inc, Japan). Spark ® The concentration of extracted RNA was measured using a Nanoquant plate with a Multimode Microplate Reader (TECAN, Swiss). The concentration of extracted RNA was measured after measuring the blank with DEPC (diethyl pyrocarbonate) treated water. cDNA synthesis was performed using Transcript ® All-in-One First Strand cDNA Synthesis SuperMix for qPCR (TransGen Biotech Co., LTD, China) with SimpliAmp TM The procedure was performed using a thermal cycler (Thermo Fisher Scientific, USA) according to the prescribed method. TB Green was used for quantitative PCR. ® Premix Ex Taq TM II (Takara Bio Inc, Japan) and the QuantStudio 3 Real-Time PCR system (Thermo Fisher Scientific, USA) were used. Relative mRNA expression values were 2 (ΔΔCt) It was determined using the method and is shown in Figure 1.
[0158] Figure 1 is a graph of the mRNA expression levels of collagen type I in human skin fibroblasts. Referring to Figure 1, the analysis of the relative expression levels of collagen mRNA (Col1A1) showed that when the composition of Example 6 was treated at a concentration of 1 v / v%, the expression level was 23.83% higher compared to the untreated group.
[0159] Experimental Example 7: Evaluation of Collagen Production Efficacy
[0160] Considering that various factors related to the elasticity of fibroblasts in the dermis change when the skin is exposed to ultraviolet rays, the content of procollagen (PIP, Procollagen type I C-peptide), collagenase (MMP-1, Matrix etalloproteinase-1), and elastase was evaluated in skin fibroblasts following UVB (ultraviolet B) irradiation and treatment with the composition of Example 6.
[0161] During intracellular collagen production, procollagen peptide chains form from mRNA and adopt a triple helix structure to form procollagen molecules. As procollagen is a precursor to collagen, the presence of collagen can be determined by measuring the PIP content in skin fibroblasts. If skin fibroblasts are stimulated and the secretion of MMP-1 increases, collagen degradation may be accelerated. If the content of MMP-1 decreases upon treatment with the test substance, it can be confirmed that the test substance prevents collagen degradation in a concentration-dependent manner. Elastase is an enzyme that degrades elastin, which affects skin elasticity; if skin fibroblasts are stimulated and the secretion of elastase increases, the degradation of elastin may be accelerated. If the content of elastase decreases upon treatment with the test substance, it can be confirmed that the test substance prevents elastin degradation in a concentration-dependent manner.
[0162] The content of PIP, MMP-1, and elastase was evaluated for the untreated group (no UVB irradiation), negative control group (UVB irradiation), positive control group (UVB irradiation and treatment with 1 μM retinoic acid (RA)), and experimental group (UVB irradiation and treatment with the composition of Example 6 at volume-based concentrations of 0.16%, 0.63%, and 2.50%, respectively).
[0163] Human skin fibroblasts (Hs68) at 2.5 x 10 wells per 35 nm cell culture dish 5 After dispensing into individual tubes, the samples were incubated for 24 hours. After washing with PBS, the samples were starved for 24 hours in FBS-free medium (DMEM, 1% P / S). After removing the medium, 1 mL of PBS was added, and UVB was applied at 15 mJ / cm² to the negative control, positive control, and experimental groups. 2 The intensity was investigated. In a new medium not containing FBS, 1 μM of retinoic acid was applied to the positive control group, and the composition of Example 6 was applied to the experimental group at concentrations of 0.16 vol%, 0.63 vol%, and 2.50 vol%, respectively, and cultured for 48 hours.
[0164] The culture medium was recovered, and the content of procollagen, collagenase, and elastase was measured according to the protocol using respective ELISA kits (Abcam, USA). Absorbance was measured at 450 nm using a microplate spectrophotometer (Bio Tek, USA), and the standard curve (R 2 The content of each factor was calculated using ≥0.90 to obtain the graphs of Figures 2 to 4.
[0165] The above experimental results are shown in Figures 2 to 4 below. Figure 2 is a graph of the content of PIP in human skin fibroblasts (Hs68) according to treatment with the composition. Figure 3 is a graph of the content of MMP-1 in human skin fibroblasts according to treatment with the composition. Figure 4 is a graph of the content of elastase in human skin fibroblasts according to treatment with the composition.
[0166] Referring to Figure 2, the PIP content in the experimental group increased as the treatment concentration of the composition of Example 6 increased, reaching 564.97 ng / mL when treated with 2.50 volume% of the composition of Example 6. The experimental group showed a higher PIP content than the untreated group, negative control group, and positive control group; specifically, the 2.50% treatment group of the composition of Example 6 showed an increase in content of 58.17% compared to the untreated group, 142.27% compared to the negative control group, and 30.53% compared to the positive control group. Through this, it was confirmed that the composition of the present invention can promote collagen production in a concentration-dependent manner.
[0167] Referring to Figure 3, the MMP-1 content was found to be 4077.26 pg / mL when the composition of Example 6 was treated at a concentration of 2.50%. Specifically, the MMP-1 content in the group treated with 2.50% of the composition of Example 6 was 24.88% lower than that of the negative control group. Through this, it was confirmed that the composition of the present invention can inhibit the secretion of collagen-degrading enzymes.
[0168] Referring to Figure 4, the elastase content in the experimental group decreased as the treatment concentration increased, reaching 752.75 pg / mL when the composition of Example 6 was treated at a concentration of 2.50%. Specifically, in the group treated with 2.50% of the composition of Example 6, the elastase content was 1.04% lower than the untreated group, 19.63% lower than the negative control group, and 20.39% lower than the positive control group. Through this, it was confirmed that the composition of the present invention can inhibit elastase secretion.
[0169] Experimental Example 8: Histological analysis of skin tissue structure and collagen density
[0170] An artificial skin tissue model was treated with the composition of Example 6 at a concentration of 2.50%, and H&E (hematoxylin & eosin) and MT stained samples were analyzed using an optical microscope.
[0171] Artificial skin tissue models (Neoderm) for all groups except the untreated group ® -ED, TEGO SCIENCE, Korea) UVB 50 mJ / cm 2 Irradiation was performed once a day for a total of 8 days at an intensity. For the positive control group, 1 mL of culture medium (FBS 10%) containing 1 μM of retinoic acid was added to a 12-well plate, and for the test group, 2.50% of the composition of Example 6 was added. Subsequently, the artificial skin tissue model was mounted in the 12-well plate and cultured for 8 days, replacing the medium with fresh medium every 2 days. After 8 days, the artificial skin tissue was harvested and fixed in 10% formaldehyde to produce a paraffin block.
[0172] For H&E staining analysis, slides were prepared by sectioning paraffin blocks to a thickness of 3 μm, followed by a hydration process and staining with H&E staining solution. Subsequently, structural and morphological changes in the artificial skin tissue sections were observed using an optical microscope (Zeweiss, Germany).
[0173] For MT staining analysis, paraffin blocks were sectioned to a thickness of 3 μm to prepare slides, hydrated, stained with Biebrich Scarlet-Acid Fuchsin solution for 5 minutes, washed, and then stained again with phosphotungsten / phosphomolybdic acid for 5 minutes. Subsequently, changes in collagen density in the cross-sections of artificial skin tissue were observed using an optical microscope (Zeweiss, Germany).
[0174] Figure 5 shows H&E stained optical microscope images (X100 magnification) of an artificial skin tissue model according to treatment with the composition. Referring to Figure 5, the negative control group showed a thickened stratum corneum and irregular tissue arrangement within the dermis compared to the untreated group. The positive control group and the test group showed a thinner stratum corneum and regular tissue arrangement within the dermis compared to the negative control group, and UVB-induced damage was alleviated.
[0175] Figure 6 shows MT stained optical microscope images (X100 magnification) of an artificial skin tissue model according to the composition treatment. To analyze collagen density, cross-sections of MT-stained artificial skin tissue were photographed using an optical microscope. The color (RGB) channels of the original image captured using the Image J (The National Institutes of Health, USA) program were deconvolved and separated into monochromatic images to analyze collagen density (%).
[0176] Figure 7 is a graph of collagen density according to the composition treatment in an artificial skin tissue model. Referring to Figure 7, it was found that the collagen density of the test group was significantly improved by more than 156% compared to the negative control group.
[0177] Experimental Example 9: Evaluation of Pore Reduction Effect on Human Skin
[0178] The number of pores and pore area were evaluated according to the treatment with the composition of Example 6 alone and the treatment with microneedles in combination.
[0179] Among female volunteers aged 35 to 49 who appear to have enlarged pores or uneven skin texture, (1) those who are pregnant, breastfeeding, or planning to become pregnant within 6 months; (2) those with psychiatric disorders or infectious skin diseases; (3) those with skin diseases, skin allergies, sensitive or hypersensitive skin, or atopic dermatitis; (4) those who have been using topical skin preparations containing antibacterial agents, immunosuppressants, or steroids, or treatments for chronic skin diseases on the test site for more than 1 month to treat skin diseases; (5) those who are severely irritated or allergic to cosmetics, medicines, or sun exposure; (6) those who have used cosmetics or medicines with the same or similar efficacy on the test site within 3 months prior to the start of the study; (7) those who have received dermatological procedures (Botox, fillers, hair removal, laser treatment, other skin care, etc.) on the test site within 6 months; (8) those taking contraceptives, antihistamines, or anti-inflammatory drugs; and (9) those participating in the same study Evaluations were conducted on 21 selected subjects recruited after excluding those for whom 3 months had not elapsed since participation. All evaluations were performed after the subjects washed their faces and adapted for 30 minutes under constant temperature and humidity conditions (22±2℃, 50±5%).
[0180] 2.5 g of the composition of Example 6 was evenly applied to the entire face of the recruited subjects. The subjects' faces were divided into left and right sides; the left side was treated with the composition of Example 6 alone, while the right side was treated with the composition of Example 6 followed by the combined application of 0.5 mm microneedles for approximately 2 minutes. The above treatments were performed on all subjects a total of four times at one-week intervals. Skin pore images were taken before treatment, one week after treatment, and four weeks after treatment to measure the number and area of pores. Skin pore imaging was performed using Antera 3D, which enhances pore visualization capabilities, allows for the quantification of related characteristics such as density and granularity, and enables the measurement of various pore-related parameters. ®CS (Miravex Limited, Ireland) was used. Antera 3D ® The skin surface was captured in high resolution using CS and converted into a 3D image. Changes in skin condition were analyzed and quantified using an internal algorithm on the converted image. The left and right cheek areas were photographed before treatment, 1 week after treatment, and 4 weeks after treatment to analyze the number of pores and the average pore area, which are skin pore analysis parameters.
[0181] Figure 8 is a graph of the number of pores on the skin according to treatment with the composition alone and treatment with microneedles in combination.
[0182] Figure 9 is a graph of the average pore area of the skin according to treatment with the composition alone and treatment with microneedles in combination.
[0183] FIG. 10 shows Antera 3D on skin pores treated with the composition alone. ® This is a CS image.
[0184] Fig. 11 shows Antera 3D on skin pores according to combined treatment with the composition and microneedles. ® This is a CS image.
[0185] Referring to Figure 8, the average number of pores of the subjects decreased by 5.54% after 1 week and 22.03% after 4 weeks when treated with the composition of Example 6 alone, and by 18.58% after 1 week and 36.55% after 4 weeks when treated with microneedles in combination.
[0186] Referring to Figure 9, the average pore area of the subjects decreased by 1.94% after 1 week and 10.02% after 4 weeks when treated with the composition of Example 6 alone, and by 7.14% after 1 week and 18.82% after 4 weeks when treated with microneedles in combination.
[0187] Through this, it was confirmed that the composition of the present invention has the effect of reducing the number of pores and shrinking the pore area, and that the effect of reducing the number of pores and shrinking the pore area is further increased when treated in combination with microneedles.
Claims
1. A hydrophilic biocompatible polymer block formed from a hydrophilic biocompatible polymer and a hydrophobic biocompatible polymer block formed from a hydrophobic biocompatible polymer, and an amphiphilic biocompatible polymer having a molecular weight of 500 g / mol to 15,000 g / mol, A cosmetic composition for improving skin elasticity or shrinking pores, wherein the molecular weight ratio of the hydrophilic biocompatible polymer block and the hydrophobic biocompatible polymer block is 1:1 to 10:
1.
2. In Paragraph 1, A cosmetic composition for improving skin elasticity or shrinking pores, wherein the molecular weight ratio of the hydrophilic biocompatible polymer block and the hydrophobic biocompatible polymer block is 2:1 to 5:
1.
3. In Paragraph 1, A cosmetic composition for improving skin elasticity or shrinking pores, wherein the polymerization ratio of the hydrophilic biocompatible polymer and the hydrophobic biocompatible polymer is 1:1 to 15:
1.
4. In Paragraph 1, A cosmetic composition for improving skin elasticity or shrinking pores, wherein the polymerization ratio of the hydrophilic biocompatible polymer and the hydrophobic biocompatible polymer is 2:1 to 8:
1.
5. In Paragraph 1, A cosmetic composition for improving skin elasticity or shrinking pores, wherein the molecular weight of the amphiphilic biocompatible polymer is 3,000 to 9,000 g / mol.
6. In Paragraph 1, A cosmetic composition for improving skin elasticity or shrinking pores, comprising 0.001 volume% to 50 volume% of the above-mentioned amphiphilic biocompatible polymer.
7. In Paragraph 1, The above-mentioned amphiphilic biocompatible polymer forms vesicles within the composition, a cosmetic composition for improving skin elasticity or shrinking pores.
8. In Paragraph 7, A cosmetic composition for improving skin elasticity or shrinking pores, wherein the particle size of the above-mentioned vesicle is 30 μm or less.
9. In Paragraph 7, A cosmetic composition for improving skin elasticity or shrinking pores, wherein the particle size of the above-mentioned vesicle is 1 μm or less.
10. In claim 1, the melting point (T) of the amphiphilic biocompatible polymer m A cosmetic composition for improving skin elasticity or shrinking pores, having a temperature of 35℃ to 65℃.
11. In Paragraph 1, A cosmetic composition for improving skin elasticity or shrinking pores, wherein the above-mentioned hydrophilic biocompatible polymer block is formed from at least one hydrophilic biocompatible polymer selected from the group consisting of polyethylene glycol, polyvinyl alcohol, polyvinylpyrrolidone, poly(N-isopropylacrylamide), hyaluronic acid, dextran, derivatives thereof, and copolymers thereof.
12. In Paragraph 1, A cosmetic composition for improving skin elasticity or reducing pores, wherein the above-mentioned hydrophobic biocompatible polymer block is formed from at least one hydrophobic biocompatible polymer selected from the group consisting of polycaprolactone, polylactic acid, polyglycolic acid, poly(3-hydroxybutyrate), polydioxanone, derivatives thereof, and copolymers thereof.
13. In Paragraph 1, A cosmetic composition for improving skin elasticity or reducing pores, wherein the amphiphilic biocompatible polymer is a block copolymer in which the hydrophobic biocompatible polymer block is bonded to one end of the hydrophilic biocompatible polymer block.
14. In Paragraph 1, A cosmetic composition for improving skin elasticity or shrinking pores, wherein the amphiphilic biocompatible polymer is formed by polymerizing a monomer of the hydrophobic biocompatible polymer at one end of the hydrophilic biocompatible polymer block.
15. In Paragraph 1, The above-mentioned amphiphilic biocompatible polymer is a methoxypolyethylene glycol-polycaprolactone copolymer, a cosmetic composition for improving skin elasticity or shrinking pores.
16. In Paragraph 1, A cosmetic composition for improving skin elasticity or shrinking pores, further comprising at least one selected from the group consisting of amino acids, vitamins, moisturizing ingredients, and whitening ingredients.
17. In Paragraph 1, A cosmetic composition for improving skin elasticity or shrinking pores, provided in at least one formulation selected from the group consisting of toner, essence, serum, ampoule, mist, lotion, cream, gel, balm, oil, mask pack, stick, primer, and foundation.