Encapsulated compositions and cosmetic or pharmaceutical compositions comprising liquid crystal particles and methods for producing them - Patents.com

Abstract

Provided is an encapsulation composition comprising liquid crystal particles, each of which comprises a core and a liquid crystal shell, the core containing an active ingredient, and the liquid crystal shell containing a fatty alcohol, a first surfactant, and an optional lipid. Also provided is a cosmetic or pharmaceutical composition comprising the encapsulation composition. Also provided is a method for preparing the encapsulation composition.

Description

[Technical Field]

[0001] The present disclosure relates generally to the encapsulation of active ingredients, and more particularly to liquid crystal encapsulation systems and methods. More particularly, the present disclosure relates to encapsulation compositions comprising liquid crystal particles, cosmetic or pharmaceutical compositions comprising the encapsulated compositions, and methods for producing the same. [Background technology]

[0002] Cosmetics generally contain complex mixtures of various ingredients, including but not limited to water, oils, surfactants, pigments, preservatives, etc., used in different cosmetic compositions, including but not limited to lotions, creams, emulsions, gels, sprays, etc., with different efficacies, including but not limited to whitening, anti-wrinkle, and sunscreen. Active ingredients can be introduced to support the aforementioned efficacies.

[0003] Some active ingredients may limit the development of cosmetic formulations, such as limiting the delivery of the required texture or feel when applied to the skin of a user. For example, diethylaminohydroxybenzoylhexylbenzoate and ethylhexyl triazone are ultraviolet (UV) filters widely used in sunscreen products, especially those with high sun protection factors (SPF). However, these types of UV filters may cause an oily feel on the skin of a user, especially because the high loading of filters is contained in sunscreen products. Generally, oil is added as a solvent to dissolve these UV filters, which causes an oily feel when applied to the skin and limits the flexibility of cosmetic formulations.

[0004] Some active ingredients, such as retinol or its derivatives, can have potential side effects upon application, such as redness, irritation, peeling, sun sensitivity, etc. Furthermore, retinol is sensitive to oxidation and has poor water solubility.

[0005] Pharmaceutical compositions generally contain complex mixtures of various ingredients. It is also desirable to encapsulate pharmaceutically active ingredients to provide improved properties.

[0006] Encapsulation systems can be provided to encapsulate active ingredients to reduce or eliminate side effects, improve texture or feel when applied to the skin, or preserve the beneficial properties of the active ingredient during storage. Although various encapsulation systems, such as solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and liquid crystal encapsulation, are known in the art, it would be desirable to provide a liquid crystal encapsulation system with improvements over the prior art, such as longer durability and stability, lower burst release and leakage of the cored active, greater compatibility with formulation systems, higher encapsulation capacity, and / or a simpler or more cost-effective production process.

[0007] The present application provides at least one of the above improvements. Summary of the Invention

[0008] In one aspect, the present application provides an encapsulation composition comprising liquid crystal particles, each of the liquid crystal particles comprising a core and a liquid crystal shell, the core containing an active ingredient, and the liquid crystal shell containing a fatty alcohol, a first surfactant, and an optional lipid.

[0009] According to one embodiment, the first surfactant may be a gemini surfactant, preferably a gemini amphiphilic surfactant. More preferably, the first surfactant may be sodium dilauramidoglutamide lysine (DLGL). The first surfactant may be present in an amount ranging from 0.1 to 20% by weight, preferably from 0.1 to 10% by weight, and more preferably from 0.1 to 5% by weight of the encapsulated composition. According to one embodiment, the fatty alcohol may be selected from the group consisting of myristyl alcohol, cetyl alcohol, cetyl / stearyl alcohol, stearyl alcohol, arachyl alcohol, behenyl alcohol, and mixtures thereof. The fatty alcohol may be present in an amount ranging from 0.1 to 50% by weight, preferably from 1 to 20% by weight, and more preferably from 1 to 10% by weight of the encapsulated composition. According to one embodiment, the active ingredient is generally lipophilic. The active ingredient may be present in an amount ranging from 1 to 70% by weight, preferably from 5 to 65% by weight, and more preferably from 5 to 60% by weight of the encapsulated composition. Preferably, the active ingredient is selected from the group consisting of lipophilic ultraviolet (UV) filters, retinol and its derivatives, and mixtures thereof.

[0010] According to one embodiment, the active ingredient may be a lipophilic ultraviolet (UV) filter, which may range from 1 to 70% by weight, preferably 5 to 60% by weight, of the encapsulated composition. Preferably, the lipophilic UV filter is selected from the group consisting of ethylhexyl triazone, diethylamino hydroxybenzoyl hexyl benzoate, bis-ethylhexyloxyphenol methoxyphenyl triazine, and mixtures thereof.

[0011] According to one embodiment, the active ingredient may be retinol and / or its derivatives, which may range from 1 to 70% by weight, preferably 5 to 60% by weight of the encapsulated composition.

[0012] According to one embodiment, the first surfactant may be in the range of 0.1-20% by weight, preferably 0.1-10% by weight, more preferably 0.1-5% by weight of the encapsulated composition, the fatty alcohol may be in the range of 0.1-50% by weight, preferably 1-20% by weight, more preferably 1-10% by weight of the encapsulated composition, and / or the active ingredient may be in the range of 1-70% by weight, preferably 5-60% by weight of the encapsulated composition.

[0013] According to one embodiment, the encapsulation composition can be formed by mixing a first mixture containing a polyol, a first surfactant, and water with a second mixture containing an active ingredient, a fatty alcohol, and an optional lipid, and liquid crystal particles are formed during mixing.

[0014] The polyol may be selected from polyols having two or more hydroxyl groups and 3 to 12, preferably 3 to 6, carbon atoms in the molecule. Preferably, the polyol is selected from the group consisting of glycerin, 1,2-propanediol, 1,3-propanediol, 1,4-butanediol, 1,3-butylene glycol, dipropylene glycol, 1,2-pentanediol, 2-methyl-pentane-2,4-diol, 1,2-hexanediol, sorbitol, 1,2-octanediol, and mixtures thereof. More preferably, the polyol is glycerin, sorbitol, or mixtures thereof. The polyol may be present in an amount ranging from 10 to 80% by weight, preferably from 20 to 60% by weight, of the encapsulated composition.

[0015] Water may range from 1 to 10% by weight of the encapsulated composition.

[0016] According to one embodiment, the lipid may be selected from the group consisting of triglycerides, hydrocarbons, esters, fatty acids, waxes, sphingolipids, phospholipids, cholesterol, and mixtures thereof. The lipid may range from 0 to 70% by weight of the encapsulated composition.

[0017] According to one embodiment, the weight ratio of the second mixture to the first mixture may range from 0.1 to 10, preferably from 0.2 to 5.

[0018] The second mixture may be in the form of a solid, semi-solid, paste, or liquid paste at 25 degrees Celsius.

[0019] According to one embodiment, the polyol may include glycerin, the first surfactant may include sodium dilauramidoglutamide lysine, the active ingredient may include diethylaminohydroxybenzoyl hexyl benzoate and / or ethylhexyl triazone, and the fatty alcohol may include behenyl alcohol.

[0020] According to one embodiment, the liquid crystal shell may contain lipids and the active ingredient may include retinol and / or its derivatives.

[0021] In another aspect, the present application provides a cosmetic or pharmaceutical composition comprising the encapsulated composition of the present application.

[0022] According to one embodiment, the cosmetic or pharmaceutical composition may further comprise a second surfactant to control the particle size of the liquid crystal particles. Preferably, the particle size of the liquid crystal particles in the presence of the second surfactant is within the range of 10 nm to 300 μm, preferably 50 nm to 100 μm, and more preferably 200 nm to 100 μm. The second surfactant may be selected from the group consisting of fatty acid esters of glycerol, fatty acid esters of sorbitol, fatty acid ethoxylates, and mixtures thereof. For example, the second surfactant may be polyglyceryl-3 methylglucose distearate.

[0023] The second surfactant may be in the range of 0.5 to 10 wt %, preferably 1 to 10 wt %, more preferably 1 to 5 wt % of the total amount of the encapsulated composition, the at least one second surfactant, and any other ingredients in the cosmetic or pharmaceutical composition.

[0024] In a further aspect, the present application provides a method for preparing the encapsulated composition of the present application, comprising: a) providing a first mixture comprising a polyol, a first surfactant, and water, and a second mixture comprising an active ingredient, a fatty alcohol, and an optional lipid; b) optionally mixing the first mixture and / or mixing the second mixture; c) mixing the first mixture with the second mixture at a temperature equal to or greater than the melting point of the fatty alcohol; d) cooling the resulting mixture of step c) to room temperature to provide an encapsulated composition.

[0025] In one embodiment, the mixing of the first mixture is carried out at a temperature above the melting point of the fatty alcohol, and the mixing of the second mixture is carried out at a temperature above the melting point of the fatty alcohol.

[0026] In one embodiment, combining the first mixture and the second mixture comprises adding the second mixture to the first mixture.

[0027] The liquid crystal (LC) encapsulation of the present application can reduce or eliminate the amount of solvent required to dissolve active ingredients such as UV filters by encapsulating the UV filters in the core. Therefore, a solvent-free liquid crystal can be provided, since no solvent is required to dissolve the active ingredients. Therefore, a more concentrated active ingredient can be encapsulated in the core. Therefore, a high SPF value can be delivered along with a desired sensory feel on the skin.

[0028] Retinol and its derivatives can have potential side effects upon application, such as redness, irritation, peeling, and sun sensitivity. Furthermore, retinol is sensitive to oxidation and has poor water solubility. The liquid crystal encapsulation of the present application can reduce or eliminate such undesirable effects.

[0029] The liquid crystal encapsulation system and method of the present application are suitable for use at high temperatures. The liquid crystal particles of the present application become more durable over time. In the present application, high liquid crystal particle size control can be easily achieved through the addition of a second surfactant and proper mixing. [Brief explanation of the drawings]

[0030] For a more complete understanding of the present disclosure, reference is now made to the following descriptions taken in conjunction with the accompanying drawings, in which: [Figure 1] FIG. 1 is a schematic diagram of a liquid crystal particle according to the present application. [Figure 2] FIG. 2 shows a schematic representation of liquid crystal particles containing a core active substance after application to the skin according to the present application. [Figure 3] FIG. 3 is a photomicrograph of the cosmetic composition of Example 1 before stability testing. [Figure 4] FIG. 4 is a photomicrograph of the comparative cosmetic composition of Example 2 prior to stability testing. [Figure 5] FIG. 5 is a micrograph of the cosmetic composition of Example 1 after a stability test (freeze-thaw test). [Figure 6] FIG. 6 is a micrograph of the cosmetic composition of Example 1 after a stability test (50° C.). DETAILED DESCRIPTION OF THE INVENTION

[0031] The present application relates to the encapsulation of an active ingredient by a liquid crystal shell. The active ingredient encapsulated by the liquid crystal shell can be in the form of particles. Thus, the present application provides an encapsulation composition comprising liquid crystal particles, each of which comprises a core and a liquid crystal shell encapsulating the core, the core containing an active ingredient, and the liquid crystal shell containing a fatty alcohol, a first surfactant, and an optional lipid. Thus, the liquid crystal particles according to the present application comprise a core encapsulated by a liquid crystal shell.

[0032] The term "optional" means that lipids can either be present or absent in the shell. When lipids are absent in the shell, it means that no lipids are used in preparing the encapsulation composition.

[0033] According to one embodiment, the core contains an active ingredient and an optional lipid, and the liquid crystal shell contains a fatty alcohol, a first surfactant, and an optional lipid, and the lipid in the core and the liquid crystal shell are the same.

[0034] The liquid crystal particles formed in the present invention can be characterized by a Maltese cross. The appearance of a Maltese cross under a polarized microscope is a typical characteristic of the formation of a liquid crystal structure.

[0035] "Active ingredient" refers to compounds, substances, molecules, and mixtures used in cosmetics to produce a beneficial effect, or compounds, substances, molecules, and mixtures that have a therapeutic effect. In some cases, for cosmetic products, it may be desirable for the active ingredient to be delivered to the epidermis and deeper skin layers in order to interact with or protect them.

[0036] The active ingredient encapsulated by the liquid crystal shell can be any lipophilic active ingredient. Preferably, the active ingredient is selected from those with low compatibility with cosmetic compositions or those with potential side effects such as redness, irritation, or peeling upon application, and must be encapsulated before being incorporated into the cosmetic composition. Preferably, the active ingredient is selected from the group consisting of lipophilic ultraviolet (UV) filters, retinol and its derivatives, and mixtures thereof. The active ingredient can range from 1 to 70% by weight, preferably 5 to 60% by weight, of the encapsulated composition.

[0037] The first surfactant may be a gemini surfactant, preferably a gemini amphiphilic surfactant. "Gemini surfactants" are generally known in the art. Gemini surfactants may have a dimeric structure consisting of two hydrophobic chains and two hydrophilic head groups connected by a spacer at or near the head groups. According to a preferred embodiment, the first surfactant may be dilauramidoglutamide lysine sodium (DLGL).

[0038] The first surfactant may range from 0.1 to 20% by weight of the encapsulated composition, preferably from 0.1 to 10% by weight, more preferably from 0.1 to 5% by weight.

[0039] In the present application, any fatty alcohol can be used as long as it does not adversely affect the formation of the liquid crystal structure described herein. According to one embodiment, the fatty alcohol can be selected from the group consisting of myristyl alcohol, cetyl alcohol, cetyl / stearyl alcohol, stearyl alcohol, arachyl alcohol, and behenyl alcohol, and any combination thereof.

[0040] According to one embodiment, the at least one fatty alcohol can be selected depending on the desired texture / sensational feel of the cosmetic composition. For example, the inclusion of behenyl alcohol can provide a stronger texture to the cosmetic composition, while cetyl alcohol can provide a lower viscosity to the cosmetic composition.

[0041] The fatty alcohol may range from 0.1 to 50% by weight of the encapsulated composition, preferably from 1 to 20% by weight, more preferably from 1 to 10% by weight.

[0042] Lipids are well known in the art, and lipids commonly used in cosmetics can be used in the present application. According to one embodiment, the lipids used in the present application can be selected from the group consisting of triglycerides, hydrocarbons, esters, fatty acids, waxes, sphingolipids, phospholipids, cholesterol, and mixtures thereof. In the present application, the lipid can be in the range of 0 to 70% by weight of the encapsulated composition.

[0043] The present application also provides a method for preparing the above-described encapsulated composition. This method may include: a) providing a first mixture containing a polyol, a first surfactant, and water; and a second mixture containing an active ingredient, a fatty alcohol, and an optional lipid; b) optionally mixing the first mixture and / or the second mixture; c) mixing the first mixture and the second mixture together at a temperature equal to or higher than the melting point of the fatty alcohol; and d) cooling the resulting mixture of step c) to room temperature to provide an encapsulated composition. The term "optionally" means that step b) is either present or absent in this method. When step b) is present, the method includes steps a), b), c), and d); and when step b) is absent, the method includes steps a), c), and d).

[0044] "Room temperature" in this application means a temperature of about 25°C.

[0045] The water used in the first mixture can be any water that can be used in cosmetic or pharmaceutical compositions, including, but not limited to, deionized water, purified water, etc. The water can range from 1 to 10% by weight of the encapsulated composition.

[0046] The first surfactant, fatty alcohol, and active ingredient used in this method are the same as those described in the encapsulated composition above.

[0047] The polyol of the present application can be any polyol having two or more hydroxyls and 3 to 12, preferably 3 to 6, carbon atoms in the molecule. In one embodiment, the polyol used in this method can be selected from the group consisting of glycerin, 1,2-propanediol (propylene glycol), 1,3-propanediol (e.g., ZEMEA™ sold by Duponte Tate & Lyle), 1,4-butanediol, 1,3-butylene glycol, dipropylene glycol, 1,2-pentanediol, 2-methyl-pentane-2,4-diol (e.g., Diolane), 1,2-hexanediol, sorbitol, 1,2-octanediol, dipropylene glycol propyl ether (e.g., Dowanol™ DPnP sold by Dow Chemicals), and dipropylene glycol isobornyl ether (e.g., Pribelance™ Clear sold by CARB), and mixtures thereof. Preferably, the polyol is glycerin, sorbitol, and mixtures thereof. The polyol may range from 10 to 80% by weight of the encapsulated composition, preferably from 20 to 60% by weight (i.e., by weight of the total amount of the first mixture and the second mixture).

[0048] Heat may be applied to mix the first mixture and / or the second mixture, and the heating temperature must be at least equal to or higher than the melting point of the fatty alcohol used in the second mixture.In a preferred embodiment, the first mixture is mixed at a temperature equal to or higher than the melting point of the fatty alcohol, and the second mixture is mixed at a temperature equal to or higher than the melting point of the fatty alcohol.When a mixture of fatty alcohols is used, the heating temperature must be equal to or higher than the melting point of the fatty alcohol with the highest melting point in the mixture.

[0049] Heat can be provided by any heating means commonly known in the art, and the means of heating is not particularly limited.

[0050] In a preferred embodiment, mixing the first mixture and the second mixture together comprises adding the second mixture to the first mixture, preferably under heating and mixing, to raise the temperature to above the melting point of the fatty alcohol.

[0051] Any suitable mixing means known in the art, such as mixing with stirring, can be used in this method. Any suitable mixing method acceptable in cosmetic or pharmaceutical production can be utilized. Those skilled in the art can select and adjust the mixing means according to, for example, the particle size of the liquid crystal particles to be obtained in the encapsulated composition.

[0052] In one embodiment, the resulting mixture of step c) may be allowed to cool naturally in step d).

[0053] According to one embodiment, the first surfactant may be present in an amount ranging from 0.1 to 20% by weight, preferably from 0.1 to 10% by weight, and more preferably from 0.1 to 5% by weight of the encapsulated composition. The fatty alcohol may be present in an amount ranging from 0.1 to 50% by weight, preferably from 1 to 20% by weight, and more preferably from 1 to 10% by weight of the encapsulated composition. The active ingredient may be present in an amount ranging from 1 to 70% by weight, preferably from 5 to 60% by weight of the encapsulated composition. The polyol may be present in an amount ranging from 10 to 80% by weight, preferably from 20 to 60% by weight, and the water may be present in an amount ranging from 1 to 10% by weight of the encapsulated composition.

[0054] Those skilled in the art can easily select the ratio between the first mixture and the second mixture. For example, this ratio can be adjusted according to the level of the active ingredient to be incorporated into the encapsulated composition. In one embodiment, the weight ratio of the second mixture to the first mixture can be in the range of 0.1 to 10, preferably 0.2 to 5.

[0055] It should be understood that the weight percentages of the ingredients are based on the weight of the encapsulated composition, ie, based on the combination of the first mixture and the second mixture.

[0056] It should be understood that the second mixture can take a variety of forms, including but not limited to, a solid, semi-solid, paste, or liquid paste at 25 degrees C. This form may depend primarily on the fatty alcohol and lipid, if any, selected.

[0057] Surprisingly, it has been found in the present application that the liquid crystal particles according to the present application are more stable than liquid crystal particles known in the art.

[0058] The method of the present application is simple and therefore has low requirements for equipment, and can reduce energy consumption because the method of the present application does not require high-energy-consuming mixing procedures such as ultrasound and high-pressure homogenization.

[0059] The present application provides a liquid crystal encapsulation technology that can reduce or eliminate the amount of solvent required to dissolve one or more lipophilic active ingredients by encapsulating the active ingredient in a core.

[0060] According to an embodiment, the active ingredient in the core may include a UV filter, preferably a lipophilic UV filter. The lipophilic UV filter may be one commonly used in the cosmetic field. For example, the lipophilic UV filter may be ethylhexyl triazone (e.g., UVINUL T150), diethylaminohydroxybenzoylhexylbenzoate (e.g., UVINUL A PLUS GRANULAR), or bis-ethylhexyloxyphenol methoxyphenyl triazine (e.g., TINOSORB S). According to the present application, the lipophilic UV filter may be used as the active ingredient to deliver a high SPF value along with a desirable sensory feel when applied to the skin. The lipophilic UV filter may be present in a range of 1 to 70% by weight, preferably 5 to 65% by weight, and more preferably 5 to 60% by weight, of the encapsulated composition. According to one embodiment, the lipophilic UV filter may be present in a range of 20 to 70% by weight, preferably 30 to 65% by weight, and more preferably 40 to 65% by weight of the encapsulated composition.

[0061] According to one embodiment, the active ingredient in the core may include retinol and / or its derivatives. Retinol is a synthetic derivative of vitamin A, a fat-soluble vitamin commonly found in carrots, eggs, and potatoes. It is a very popular skin care ingredient for addressing many skin concerns, such as fine lines, pigmentation, and acne. However, retinol has several potential side effects upon application, such as redness, irritation, peeling, and sun sensitivity. Furthermore, retinol is sensitive to oxidation and has poor water solubility. The encapsulated composition of the present application, including liquid crystal particles, can encapsulate retinol in the core to maintain retinol properties during storage, enhance its physiological efficacy, and eliminate retinol side effects. Retinol and its derivatives may range from 1 to 70% by weight, preferably 5 to 60% by weight, of the encapsulated composition.

[0062] According to one embodiment, the liquid crystal shell in the liquid crystal particles contains a lipid while the core contains retinol or a derivative thereof.

[0063] The liquid crystal encapsulation technology of the present application has broader applicability than conventional liquid crystal encapsulation technologies. For example, the liquid crystal encapsulation technology of the present application is suitable for use at high temperatures (up to 80-90 degrees Celsius, depending on the melting point of the active ingredient being encapsulated). Therefore, active ingredients with high melting points can be more easily incorporated into cosmetic compositions. Furthermore, the liquid crystal particles are more durable over time than liquid crystal particles prepared by conventional liquid crystal encapsulation technologies.

[0064] The encapsulated compositions according to the present application may contain liquid crystal particles that are solvent-free because they do not require a solvent to dissolve the active ingredient, and therefore the core of the liquid crystal particles may contain higher levels of the active ingredient.

[0065] The present application further provides a cosmetic or pharmaceutical composition comprising the encapsulated composition of the present application.

[0066] In this application, a cosmetic or pharmaceutical composition comprising an encapsulated composition means that the encapsulated composition is used in the preparation of the cosmetic or pharmaceutical composition. Those skilled in the art will understand that the encapsulated composition is mixed with other ingredients in the cosmetic or pharmaceutical composition during the preparation of the cosmetic or pharmaceutical composition, and that the liquid crystal particles in the encapsulated particles are mixed with other ingredients in the cosmetic or pharmaceutical composition. Generally, the liquid crystal particles are dispersed in the cosmetic or pharmaceutical composition.

[0067] In this application, "cosmetic composition" means a composition for affecting or beautifying the appearance of the face, skin, hair, nails, or other keratinous material. Cosmetic compositions are well known in the art.

[0068] The cosmetic compositions of the present application can be formulated into various forms, such as lotions, creams, emulsions, gels, sprays, and the like.

[0069] The level of the encapsulated composition of the present application in the cosmetic composition can be readily selected and determined by one skilled in the art according to the level of active ingredients to be incorporated into the cosmetic composition.

[0070] The cosmetic composition of the present application may contain various ingredients commonly used in cosmetic products that are known in the art. Specifically, these ingredients can be selected and combined according to the form of the cosmetic composition and / or the desired properties or characteristics of the cosmetic composition. By way of example, these ingredients may include, but are not limited to, one or more of antioxidants, chelating agents, colorants, emollients, emulsifiers, fragrances, moisturizers, lubricants, preservatives, stabilizers, surfactants, viscosity modifiers, or any combination thereof. The amounts of the ingredients can be easily selected and adjusted by those skilled in the art. For example, the ingredients can be used at levels commonly used in cosmetic products.

[0071] Alternatively or in addition, the cosmetic composition of the present application may contain at least one additional active ingredient in addition to the active ingredient contained in the encapsulated composition described above. The additional active ingredient may be an ingredient commonly known in cosmetics and may be selected according to the desired effect provided by the cosmetic composition. For example, the additional active ingredient may be selected from radical scavengers, ultraviolet absorbers, vitamins, peeling active ingredients, retinoids, anti-acne active ingredients, tanning active ingredients, anti-inflammatory active ingredients, antimicrobial active ingredients, antifungal active ingredients, skin whitening agents, skin activators, skin healing agents, moisturizing active ingredients, and mixtures thereof.

[0072] The amount of the additional active ingredient can be readily selected and adjusted by one skilled in the art, for example, the additional active ingredient can be used at a level generally employed in cosmetic products to provide the desired effect.

[0073] According to a preferred embodiment, the cosmetic composition may further contain a second surfactant. The particle size of the liquid crystal particles can be further adjusted or controlled by the second surfactant. Preferably, the particle size of the liquid crystal particles is controlled to within a range of 10 nm to 300 μm, preferably 50 nm to 100 μm, and more preferably 200 nm to 100 μm, by the presence of the second surfactant. The second surfactant may be selected from the group consisting of fatty acid esters of glycerol, fatty acid esters of sorbitol, fatty acid ethoxylates, and mixtures thereof. For example, the second surfactant may be polyglyceryl-3 methylglucose distearate. The second surfactant may be present in an amount ranging from 0.5 to 10% by weight, preferably from 1 to 10% by weight, and more preferably from 1 to 5% by weight, of the total amount of the encapsulated composition, the at least one second surfactant, and any other components in the cosmetic composition. According to one embodiment, the second surfactant may be incorporated into the cosmetic composition during its preparation.

[0074] The cosmetic composition of the present application can be obtained by mixing the encapsulated composition of the present application with all other ingredients in the cosmetic composition (including the second surfactant, if present). The encapsulated composition of the present application can be added to a third mixture under mixing to provide the cosmetic composition. The third mixture can contain all other ingredients in the cosmetic composition except for the encapsulated composition. Any suitable mixing method acceptable in cosmetic production can be used as long as it can provide a cosmetic composition. Those skilled in the art can easily select and adjust the type and / or speed of mixing. High-energy-consuming mixing procedures, such as ultrasonication and high-pressure homogenization, can be used, but are not required. According to one embodiment, high-energy-consuming mixing procedures are not used in the preparation of the cosmetic composition of the present application.

[0075] According to a preferred embodiment, the cosmetic composition of the present application comprises a polyol selected from the group consisting of glycerin, sorbitol, and mixtures thereof. The first surfactant is dilauramidoglutamide lysine sodium, the encapsulated active ingredient is selected from the group consisting of diethylaminohydroxybenzoylhexylbenzoate, ethylhexyl triazone, and mixtures thereof, the fatty alcohol is behenyl alcohol, and the second surfactant is polyglyceryl-3 methylglucose distearate. In another preferred embodiment, the cosmetic composition of the present application comprises glycerin or sorbitol as the polyol, dilauramidoglutamide lysine sodium as the first surfactant, diethylaminohydroxybenzoylhexylbenzoate and ethylhexyl triazone as the encapsulated active ingredients, behenyl alcohol as the fatty alcohol, polyglyceryl-3 methylglucose distearate as the second surfactant, and ethylhexyl methoxycinnamate as an additional UV filter.

[0076] In this application, "pharmaceutical composition" means a composition containing an active ingredient having a therapeutic effect. Pharmaceutical compositions are well known in the art. The pharmaceutical compositions of this application can be formulated into various dosage forms such as syrups, capsules, tablets, solutions, suspensions, ointments, and gels.

[0077] The level of the encapsulated composition of the present application in a pharmaceutical composition can be readily selected and determined by one skilled in the art according to the level of active ingredient to be incorporated into the pharmaceutical composition.

[0078] The pharmaceutical composition according to the present application may also contain pharmaceutically acceptable ingredients, including, but not limited to, carriers, excipients, disintegrants, buffers, emulsifiers, suspending agents, soothing agents, stabilizers, preservatives, antiseptics, physiological saline, etc. Those skilled in the art can select such additional ingredients according to the dosage form of the pharmaceutical composition.

[0079] The pharmaceutical composition according to the present application can be manufactured using methods generally known in the relevant technical field. Those skilled in the art can easily select a suitable manufacturing method according to the dosage form of the pharmaceutical composition.

[0080] It should be understood that the inclusion of polyol in the present application can promote the formation of liquid crystal structure in the first surfactant (e.g., sodium dilauramidoglutamide lysine) and at least one fatty alcohol (e.g., behenyl alcohol).In addition, the active ingredient can be encapsulated as a core material, and the active ingredient can be more easily retained on the user's skin upon application.

[0081] FIG. 1 is a schematic diagram of a liquid crystal particle according to the present application, showing the encapsulation of a core active substance through the liquid crystal structure. As shown in FIG. 1, the core (1) is encapsulated by a liquid crystal shell (2), which is surrounded by a continuous phase (3), such as the continuous phase of a cosmetic composition. FIG. 2 is a schematic diagram of a liquid crystal particle according to the present application, which includes a core active substance, after application to skin. The continuous phase disappears after the cosmetic composition of the present application is applied to skin. Thus, the liquid crystal particle with the active ingredient in the core (1) remains on the skin, and the core (1) is surrounded by the liquid crystal shell (2).

[0082] The following examples are provided to further illustrate the present application. [Example]

[0083] Example 1 The encapsulated compositions of the present application were prepared by propeller mixing the ingredients in Mix 1 at 85°C until uniform, propeller mixing the ingredients in Mix 2 at 85°C until uniform, adding Mix 2 to Mix 1 while propeller mixing until uniform, and cooling to room temperature. The first and second mixtures are shown in the table below.

[0084] [Table 1]

[0085] Mixture 3 was mixed at 85°C until uniform and cooled to room temperature. The encapsulation composition was added to Mixture 3 by slow homogenization at 2000-3000 rpm until uniform to provide a cosmetic composition (sunscreen emulsion).

[0086] Comparative Example 2

[0087] [Table 2]

[0088] A comparative composition was prepared by propeller mixing the ingredients in Mix 1 at 85°C until uniform, propeller mixing the ingredients in Mix 2 at 85°C until uniform, adding Mix 2 to Mix 1 while propeller mixing until uniform, and cooling to room temperature. Mix 3 was added to the comparative composition by slow homogenization at 2000-3000 rpm until uniform to provide a comparative cosmetic composition (sunscreen emulsion).

[0089] Example 3 Stability Test Stability tests were conducted for Examples 1 and 2 over a period of one month. The liquid crystal structure was confirmed by polarizing microscope. The microscope used was a Leica DM2500. As can be seen from the table below, the liquid crystal structure for the cosmetic composition of Example 1 still exists after stability tests at room temperature, 50°C, and five cycles of freeze-thawing (from room temperature to -20°C). The equipment used for the stability tests at room temperature and 50°C is a Binder incubator BF240, and the equipment used for the freeze-thawing test is a Haier refrigerator DW-40L278. The liquid crystal structure for the cosmetic composition of Example 2 gradually disappeared during the stability test. This indicates that a stronger liquid crystal structure can be obtained in this application compared to conventional liquid crystal technology.

[0090] [Table 3]

[0091] As shown in Figures 3 and 4, the cosmetic composition of Example 1 exhibits more liquid crystal particles (Figure 3), while far fewer liquid crystal particles are observed in the comparative cosmetic composition of Example 2, which uses traditional liquid crystal technology (Figure 4). The thicker, fuller Maltese cross in Figure 3 indicates a stronger liquid crystal structure.

[0092] After the extreme stability test (50°C, freeze-thaw), the liquid crystal particles in the cosmetic composition of Example 1 were still observable, while the liquid crystal particles were no longer present in the comparative cosmetic composition of Example 2, as shown in Figures 5 and 6.

[0093] Although the present disclosure and its advantages have been described in detail, it should be understood that various changes, substitutions, and alterations can be made therein without departing from the spirit and scope of the present disclosure, as defined by the appended claims. Moreover, the scope of this application is not intended to be limited to the particular embodiments of the processes, machines, manufacture, compositions of matter, means, methods, and steps described herein. As one skilled in the art will readily understand from this disclosure, any existing or later-developed processes, machines, manufacture, compositions of matter, means, methods, or steps that perform substantially the same function or achieve substantially the same results as the corresponding embodiments described herein can be utilized in accordance with the present disclosure. Accordingly, the appended claims are intended to include within their scope such processes, machines, manufacture, compositions of matter, means, methods, or steps.

Claims

1. An encapsulation composition comprising liquid crystal particles, each of the liquid crystal particles comprising a core and a liquid crystal shell, the core containing an active ingredient, and the liquid crystal shell containing a fatty alcohol, a first surfactant, and an optional lipid.

2. 2. The encapsulated composition of claim 1, wherein the first surfactant is a gemini surfactant, preferably a gemini amphiphilic surfactant, more preferably sodium dilauramidoglutamide lysine (DLGL), and / or the first surfactant is in the range of 0.1 to 20%, preferably 0.1 to 10%, more preferably 0.1 to 5% by weight of the encapsulated composition.

3. 2. The encapsulated composition of claim 1, wherein the fatty alcohol is selected from the group consisting of myristyl alcohol, cetyl alcohol, cetyl / stearyl alcohol, stearyl alcohol, arachyl alcohol, behenyl alcohol, and mixtures thereof, and / or the fatty alcohol ranges from 0.1 to 50%, preferably 1 to 20%, more preferably 1 to 10% by weight of the encapsulated composition.

4. 10. The encapsulated composition of claim 1, wherein the active ingredient is lipophilic and ranges from 1 to 70%, preferably 5 to 65%, more preferably 5 to 60% by weight of the encapsulated composition, and preferably the active ingredient is selected from the group consisting of lipophilic ultraviolet (UV) filters, retinol and its derivatives, and mixtures thereof.

5. 2. The encapsulated composition of claim 1, wherein the active ingredient is a lipophilic ultraviolet (UV) filter, and the lipophilic ultraviolet (UV) filter ranges from 1 to 70% by weight of the encapsulated composition, preferably 5 to 65% by weight, preferably 5 to 60% by weight, and preferably the lipophilic ultraviolet (UV) filter is selected from the group consisting of ethylhexyl triazone, diethylamino hydroxybenzoyl hexyl benzoate, bis-ethylhexyloxyphenol methoxyphenyl triazine, and mixtures thereof.

6. 2. The encapsulated composition of claim 1, wherein the active ingredient is selected from the group consisting of retinol and its derivatives, and the retinol and its derivatives are in the range of 1 to 70% by weight, preferably 5 to 60% by weight of the encapsulated composition.

7. 10. The encapsulated composition of claim 1, wherein the encapsulated composition is formed by combining a first mixture comprising a polyol, the first surfactant, and water with a second mixture comprising the active ingredient, the fatty alcohol, and the optional lipid.

8. 2. The encapsulated composition of claim 1, wherein the polyol is a polyol having two or more hydroxyls and 3 to 12, preferably 3 to 6, carbon atoms in the molecule, preferably selected from the group consisting of glycerin, 1,2-propanediol, 1,3-propanediol, 1,4-butanediol, 1,3-butylene glycol, dipropylene glycol, 1,2-pentanediol, 2-methyl-pentane-2,4-diol, 1,2-hexanediol, sorbitol, 1,2-octanediol, and mixtures thereof, preferably the polyol is glycerin, sorbitol, and mixtures thereof, and / or the polyol is in the range of 10 to 80% by weight, preferably 20 to 60% by weight of the encapsulated composition.

9. 10. The encapsulated composition of claim 1, wherein the lipid is selected from the group consisting of triglycerides, hydrocarbons, esters, fatty acids, waxes, sphingolipids, phospholipids, cholesterol, and mixtures thereof, and / or the lipid ranges from 0 to 70% by weight of the encapsulated composition.

10. The encapsulated composition of claim 1, wherein the weight ratio of the second mixture to the first mixture ranges from 0.1 to 10, preferably from 0.2 to 5.

11. 7. The encapsulated composition of claim 6, wherein the second mixture is in the form of a solid, semi-solid, paste, or liquid paste at 25 degrees Celsius.

12. 8. The encapsulated composition of claim 7, wherein the polyol comprises glycerin, the first surfactant comprises sodium dilauramidoglutamide lysine, the active ingredient comprises diethylaminohydroxybenzoyl hexyl benzoate and / or ethylhexyl triazone, and the fatty alcohol comprises behenyl alcohol.

13. The encapsulated composition of claim 1 , wherein the liquid crystal shell contains the lipid and the active ingredient comprises retinol and / or a derivative thereof.

14. A cosmetic or pharmaceutical composition comprising an encapsulated composition according to any one of claims 1 to 13.

15. 15. The cosmetic or pharmaceutical composition according to claim 14, wherein the system further comprises a second surfactant and the particle size of the liquid crystal particles is in the range of 10 nm to 300 μm, preferably 50 nm to 100 μm, more preferably 200 nm to 100 μm.

16. 16. The cosmetic or pharmaceutical composition of claim 15, wherein the second surfactant is selected from the group consisting of fatty acid esters of glycerol, fatty acid esters of sorbitol, fatty acid ethoxylates, and mixtures thereof.

17. 17. The cosmetic or pharmaceutical composition of claim 15 or 16, wherein the second surfactant is in the range of 0.5 to 10 wt %, preferably 1 to 10 wt %, more preferably 1 to 5 wt % of the total amount of the encapsulated composition, the at least one second surfactant, and any other ingredients in the cosmetic or pharmaceutical composition.

18. A method for preparing the encapsulated composition of any one of claims 1 to 14, comprising: a) providing a first mixture comprising a polyol, a first surfactant, and water, and a second mixture comprising an active ingredient, a fatty alcohol, and an optional lipid; b) optionally mixing the first mixture and / or mixing the second mixture; c) mixing the first mixture with the second mixture at a temperature equal to or greater than the melting point of the fatty alcohol; d) cooling the resulting mixture of step c) to room temperature to provide said encapsulated composition.

19. 20. The method of claim 18, wherein the mixing of the first mixture is performed at a temperature above the melting point of the fatty alcohol and the mixing of the second mixture is performed at a temperature above the melting point of the fatty alcohol.

20. 20. The method of claim 18, wherein combining the first mixture with the second mixture comprises adding the second mixture to the first mixture.

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