Elastic liposome composition containing sucrose-based surfactant and cosmetic composition containing the same

Abstract

The present invention provides an elastic liposome composition containing elastic liposomes, which contains lecithin and a sucrose-based surfactant esterified from sucrose and at least one stearic acid, and thus has excellent deformability, softness, skin permeability and effective ingredient capture efficiency, and can maintain a stable state for a long time. In addition, a cosmetic composition having excellent stability and skin permeability by containing the elastic liposome composition is provided.

Description

Technical Field

[0001] The present invention relates to an elastic liposome composition containing a sucrose-based surfactant and a cosmetic composition containing the same. Background Art

[0002] Human skin is composed of three layers: epidermis, dermis and subcutaneous fat, among which the epidermis is composed of basal layer, spinous layer, granular layer and stratum corneum. The stratum corneum is a structure in which keratinocytes are stacked layer by layer, and lipid components exist in the spaces between keratinocytes. At this time, it is reported that the percutaneous absorption route is more effective in penetrating lipid components located between keratinocytes of the skin than directly penetrating keratinocytes of the skin.

[0003] Therefore, attempts are being made to develop a skin absorption delivery system for active ingredients using liposomes with lipid components as the main component. In particular, liposomes are absorbed into the skin in a state where poorly soluble flavonoid substances are trapped inside, thereby effectively delivering poorly soluble, insoluble, etc. active ingredients to the skin. In response to this, the development of cosmetic compositions using liposomes is being actively carried out recently.

[0004] As an example, Korean Patent Publication No. 10-2003-0085941 discloses a liposome that captures flavonoids having anti-oxidation and anti-aging effects and a cosmetic composition containing the liposome. However, although the conventional liposome disclosed in the above patent has the advantage of being able to carry poorly soluble substances, etc., it has the problems of low capture efficiency of effective ingredients such as poorly soluble substances, low stability of the liposome, and low skin permeability of the liposome.

[0005] In order to solve the above problems, the use of elastic liposomes with high capture efficiency of active ingredients, excellent stability of liposomes, and elasticity or deformability is increasing. The above elastic liposomes are mainly composed of phospholipids forming a double layer and a surfactant as an elasticity-imparting component (edge ​​activator), and have elasticity and softness. That is, the elastic liposomes have deformability and can effectively pass through the stratum corneum, so the skin delivery efficiency of the active ingredients can be more excellent.

[0006] Most elastic liposomes are formed by phospholipids and surfactants with single carbon chains such as cholesterol, sodium cholate, span 80, octaoxyethylene laurate ether, or ionic surfactants such as sodium hexadecyl sulfate and cetylpyridinium chloride. As an example, Korean Publication Patent No. 10-2018-0013541 discloses elastic liposomes formed by surfactants such as sodium cholate. However, for elastic liposomes formed by the above-mentioned surfactants, deformability, softness, skin permeability, etc. are improved, but there is a problem of significantly reduced stability.

[0007] Therefore, there is a need to develop elastic liposomes that not only have excellent properties such as deformability, flexibility, skin permeability, and effective ingredient capture efficiency but also can maintain a stable state for a long time, and cosmetic compositions containing the same. Summary of the invention

[0008] Technical issues

[0009] The first object of the present invention is to provide an elastic liposome composition containing elastic liposomes having excellent deformability, softness, skin permeability and flavonoid capturing efficiency while maintaining a stable state for a long time.

[0010] A second object of the present invention is to provide a cosmetic composition which contains the elastic liposome composition and can effectively deliver flavonoids to the skin, thereby having an excellent skin improvement effect.

[0011] The purpose of the present invention is not limited to the above-mentioned technical problems, and other technical problems can be derived from the following description.

[0012] Problem Solving Methods

[0013] In order to achieve the above first object, the present invention provides an elastic liposome composition, which comprises lecithin and a sucrose-based surfactant esterified by sucrose and at least one stearic acid.

[0014] The sucrose-based surfactant may include one or more selected from the group consisting of sucrose monostearate, sucrose distearate, and sucrose tristearate.

[0015] The elastic liposome composition may include the lecithin and the sucrose-based surfactant in a weight ratio of 1:0.01 to 0.30.

[0016] The particle size of the elastic liposomes may be 70 to 200 nanometers.

[0017] The elastic liposome composition further comprises flavonoids, and the flavonoids may include one or more selected from the group consisting of quercetin, catechin, apigenin, myricetin, luteolin and fisetin.

[0018] In order to achieve the above second object, the present invention provides a cosmetic composition comprising an elastic liposome composition, wherein the elastic liposome composition comprises lecithin and a sucrose-based surfactant esterified with sucrose and at least one stearic acid.

[0019] Effects of the Invention

[0020] In the elastic liposome composition of the present invention, the elastic liposome has excellent deformability, softness, skin permeability and flavonoid capturing efficiency, and can also have excellent stability.

[0021] In particular, the elastic liposome composition of the present invention can achieve more excellent deformability, softness, skin permeability, flavonoid capture efficiency and stability because it contains lecithin and a sucrose-based surfactant esterified with sucrose and at least one stearic acid at a specific ratio.

[0022] In addition, the elastic liposome composition of the present invention can achieve more excellent deformability, softness, skin permeability, flavonoid capture efficiency and stability by containing a sucrose-based surfactant obtained by esterifying sucrose with 1 to 3 stearic acids as an elasticity-imparting component.

[0023] Since the cosmetic composition of the present invention contains elastic liposomes that trap poorly soluble flavonoids inside, the flavonoids can be effectively delivered to the skin, thereby achieving excellent skin improvement effects. In this case, the above-mentioned skin improvement effects refer to all skin improvement effects that can be achieved by flavonoids, and can typically refer to anti-oxidation, anti-aging, etc. BRIEF DESCRIPTION OF THE DRAWINGS

[0024] Figure 1 TEM images of the elastic liposome compositions of Comparative Example 1, Example 3, Example 7, and Example 11 according to Experimental Example 1 are shown.

[0025] Figure 2 This is a graph showing the changes in the skin permeation amount of quercetin over time in Example 3, Example 7, Example 11, Comparative Example 1, and the control group (1,3-butanediol) in Experimental Example 3.

[0026] Figure 3 It is a graph showing the quercetin content in the stratum corneum, the quercetin content in the skin (epidermis and dermis), and the quercetin content through the skin of Example 3, Example 7, Example 11, Comparative Example 1, and the control group (1,3-butanediol) after about 12 hours in Experimental Example 3. DETAILED DESCRIPTION

[0027] Hereinafter, embodiments of the present invention will be described in detail with reference to the accompanying drawings so that those skilled in the art can easily implement the present invention. However, the present invention can be implemented in various forms and is not limited to the embodiments described herein. Moreover, in order to clearly describe the present invention in the accompanying drawings, parts not related to the description are omitted.

[0028] The terms or words used in the specification and claims of the present invention should not be interpreted as limited to the ordinary or dictionary meanings, but should be interpreted as meanings and concepts consistent with the technical idea of ​​the present invention based on the principle that the inventor can appropriately define the concepts of the terms in order to describe his own invention in the best way.

[0029] Throughout the specification of the present invention, when a part “includes” a certain constituent element, it means that other constituent elements may also be included, rather than excluding other constituent elements, unless there is a special description to the contrary.

[0030] Throughout the specification of the present invention, "A and / or B" means A or B, or A and B.

[0031] The present invention is described in detail below, but the present invention is not limited thereto.

[0032] The present invention provides an elastic liposome composition.

[0033] In one embodiment of the present invention, an elastic liposome composition with excellent stability and skin permeability is provided, which comprises lecithin; and a sucrose-based surfactant esterified by sucrose and at least one stearic acid. Specifically, in this embodiment, a composition containing elastic liposomes entrapping flavonoids is provided, the composition comprising an elastic liposome composed of the following components: a phospholipid layer formed by a sucrose-based surfactant and lecithin, the sucrose-based surfactant being esterified by sucrose and at least one stearic acid; and flavonoids carried inside the above-mentioned phospholipid layer.

[0034] The elastic liposomes of this embodiment have excellent deformability, softness, skin permeability and flavonoid capture efficiency, and also have excellent stability.

[0035] In particular, the elastic liposome composition of this embodiment can achieve more excellent deformability, softness, skin permeability, flavonoid capture efficiency and stability because it contains lecithin and a sucrose-based surfactant esterified with sucrose and at least one stearic acid at a specific ratio.

[0036] In addition, the elastic liposome composition of this example can achieve more excellent deformability, softness, skin permeability, flavonoid capture efficiency and stability by containing a sucrose-based surfactant obtained by esterifying sucrose with 1 to 3 stearic acids as an elasticity-imparting component.

[0037] More specifically, in this Example, it was confirmed that the deformability, softness, skin permeability, flavonoid capture efficiency, and stability of elastic liposomes differ depending on the number of stearic acid chains attached or bound to sucrose.

[0038] For example, it was confirmed that when the sucrose-based surfactant was esterified with sucrose and 1 to 3 stearic acids, the above effect was enhanced. In particular, it was confirmed that when it was esterified with sucrose and two stearic acids, the above effect was further enhanced.

[0039] Phosphatidylcholine, as a phospholipid containing glycerophosphate, is one of the main components of biological membranes. Phosphatidylcholine is present in large quantities in egg yolk, soybean oil, liver, brain, etc. The above-mentioned phosphatidylcholine, together with the sucrose-based surfactant of the present embodiment, plays a role in improving the elasticity, softness and deformability of the elastic liposome of the present embodiment.

[0040] The sucrose-based surfactant, as an elasticity-imparting component (edge ​​activator), can impart elasticity, softness, and deformability to the elastic liposome of this embodiment. In particular, elastic liposomes are prone to deformation of the lipid membrane shape, so that, unlike general liposomes, even if the particle size becomes larger, it can easily pass through the narrow gaps between the stratum corneum. That is, elastic liposomes can capture more flavonoids inside than general liposomes, and can effectively deliver them to the skin.

[0041] The sucrose-based surfactant of this embodiment is formed by esterification of sucrose and at least one stearic acid.

[0042] For example, the sucrose-based surfactant of the present embodiment can be an ester compound of sucrose and 1 to 3 stearic acids. In the present embodiment, since the sucrose-based surfactant includes an ester compound of sucrose and 1 to 3 stearic acids, the deformability, softness, elasticity, flavonoid capture efficiency and stability of the elastic liposome can be further improved. In more detail, the above-mentioned sucrose-based surfactant can include one or more selected from the group consisting of sucrose monostearate, sucrose distearate and sucrose tristearate.

[0043] The sucrose monostearate may be obtained by monoesterification of sucrose and stearic acid.

[0044] The sucrose distearate may be obtained by diesterification of sucrose and stearic acid.

[0045] The sucrose tristearate may be obtained by triesterification of sucrose and stearic acid.

[0046] As another example, the sucrose-based surfactant of the present embodiment can be sucrose distearate, but is not limited thereto. In particular, when the sucrose-based surfactant of the present embodiment is sucrose distearate, the deformability, softness, elasticity, flavonoid capture efficiency and stability of the elastic liposome can be significantly improved.

[0047] The elastic liposome composition of this embodiment may contain the above-mentioned lecithin and the above-mentioned sucrose-based surfactant in a weight ratio of 1:0.01 to 0.30. If, when the elastic liposome composition of this embodiment does not contain the above-mentioned lecithin and the above-mentioned sucrose-based surfactant in a weight ratio of 1:0.01 to 0.30, the softness, elasticity, deformability, flavonoid capture efficiency and stability of the elastic liposome may be significantly reduced.

[0048] As another example, the elastic liposome composition of this embodiment may include the lecithin and the sucrose-based surfactant in a weight ratio of 1:0.02-0.20.

[0049] As another example, the elastic liposome composition of this embodiment may include the lecithin and the sucrose-based surfactant in a weight ratio of 1:0.05-0.15.

[0050] As another example, the elastic liposome composition of this embodiment may contain the above-mentioned lecithin and the above-mentioned sucrose-based surfactant in a weight ratio of 1:0.10 to 0.12. In particular, when the elastic liposome composition of this embodiment contains the above-mentioned lecithin and the above-mentioned sucrose-based surfactant in a weight ratio of 1:0.10 to 0.12, elastic liposomes having significantly excellent softness, elasticity, deformability, flavonoid capture efficiency and stability can be formed.

[0051] The flavonoids of this embodiment may include at least one selected from the group consisting of quercetin, catechin, apigenin, myricetin, luteolin and fisetin, but are not limited thereto.

[0052] For example, the flavonoid of this embodiment may be quercetin, but is not limited thereto.

[0053] Relative to 100 parts by weight of the total content of lecithin and surfactant, the content of flavonoids in this embodiment can be 0.00001 to 5.0 parts by weight, 0.0001 to 3.0 parts by weight, 0.001 to 1.0 parts by weight or 0.01 to 0.1 parts by weight, but is not limited thereto.

[0054] If, relative to 100 parts by weight of the total content of lecithin and surfactant, the content of flavonoids in this embodiment is less than 0.00001 parts by weight, there may be a problem that the skin improvement effects such as the antioxidant effect and the anti-aging effect caused by flavonoids are not significant. On the contrary, when the content of flavonoids in this embodiment exceeds 5 parts by weight relative to 100 parts by weight of the total content of lecithin and surfactant, the stability, skin permeability and flavonoid capture efficiency of elastic liposomes may be reduced.

[0055] The elastic liposome of this embodiment is formed from the above-mentioned flavonoids, lecithin and sucrose-based surfactant, and may have a particle size of 70 to 200 nanometers, but is not limited thereto.

[0056] If, when the elastic liposome of the present embodiment has a particle size of less than 70 nanometers, the capture efficiency of flavonoids is significantly reduced, and the properties of softness, elasticity, deformability, etc. may be reduced. On the contrary, when the elastic liposome of the present embodiment has a particle size of more than 200 nanometers, stability and skin permeability may be significantly reduced.

[0057] For example, the elastic liposome of this embodiment may have a particle size of 80 to 180 nanometers.

[0058] As another example, the elastic liposome of this embodiment may have a particle size of 90 to 160 nanometers.

[0059] As another example, the elastic liposome of the present embodiment may have a particle size of 100 to 130 nanometers. In particular, when the elastic liposome of the present embodiment has a particle size of 100 to 130 nanometers, the flavonoid capture efficiency is excellent, and the properties of softness, elasticity, variability, stability, skin permeability, etc. can be further improved.

[0060] The elastic liposome composition of this embodiment comprises flavonoids, lecithin, and a sucrose-based surfactant esterified by sucrose and at least one stearic acid. In particular, when i) lecithin is contained, ii) one or more selected from the group consisting of sucrose monostearate, sucrose distearate, and sucrose tristearate are contained as the sucrose-based surfactant, and iii) the lecithin and the sucrose-based surfactant are contained in a weight ratio of 1:0.01 to 0.30, a composition containing elastic liposomes having a particle size of 70 to 200 nanometers and having significantly excellent elasticity, deformability, softness, flavonoid capture efficiency and stability can be provided.

[0061] The elastic liposome composition of this embodiment may further contain known additives such as purified water and organic solvents.

[0062] The elastic liposome composition of this example can be applied to the skin itself, or can be applied to the skin in the form of being included in a cosmetic composition.

[0063] Furthermore, the present invention provides a cosmetic composition containing the elastic liposome composition.

[0064] The cosmetic composition of this embodiment may contain an elastic liposome composition, which contains lecithin; and a sucrose-based surfactant esterified by sucrose and at least one stearic acid to capture the elastic liposomes with flavonoids. Specifically, the cosmetic composition of this embodiment may contain an elastic liposome composition, which contains an elastic liposome composed of the following components: a phospholipid layer, which is formed by a sucrose-based surfactant and lecithin, and the sucrose-based surfactant is esterified by sucrose and at least one stearic acid; and flavonoids carried inside the above-mentioned phospholipid layer.

[0065] Since the cosmetic composition of this embodiment contains elastic liposomes having excellent deformability, softness, skin permeability, flavonoid capture efficiency, and excellent stability, the active ingredients can be effectively delivered to the skin. Therefore, the skin improvement effect of the cosmetic composition of this embodiment can be significantly improved.

[0066] In particular, the elastic liposome composition of this embodiment contains lecithin and a sucrose-based surfactant esterified with sucrose and at least one stearic acid in a specific ratio, and thus can form elastic liposomes with more excellent deformability, softness, skin permeability, flavonoid capture efficiency and stability.

[0067] In addition, the elastic liposome composition of this example contains a sucrose-based surfactant esterified with sucrose and 1 to 3 stearic acids as an elasticity-imparting component, thereby achieving elastic liposomes with more excellent deformability, softness, skin permeability, flavonoid capture efficiency and stability.

[0068] The cosmetic composition of this embodiment may contain 0.0001 to 50 wt % of the elastic liposome composition based on the total weight.

[0069] As another example, the cosmetic composition of this embodiment may include 0.001 to 40 wt % of the elastic liposome composition based on the total weight.

[0070] As another example, the cosmetic composition of this embodiment may include 0.01 to 30 wt % of the elastic liposome composition based on the total weight.

[0071] The cosmetic composition of this embodiment, in addition to the above-mentioned elastic liposome composition, may also contain one or more additional ingredients selected from the group consisting of thickeners, fatty substances, organic solvents, solubilizers, concentrators, gelling agents, softeners, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, emulsifiers, fillers, metal ion blocking agents, chelating agents, preservatives, vitamins, blocking agents, wetting agents, oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles and the remainder of water.

[0072] The cosmetic composition of this embodiment can be formed into a dosage form selected from the group consisting of softening lotion, nourishing lotion, astringent lotion, toner, emulsion, essence, ampoule, cream, massage cream, facial mask, primer, BB cream, foundation, powder, sunscreen, sunscreen lotion, sunscreen milk, cleansing foam, cleansing cream, cleansing water, shampoo, conditioner, conditioner, hair spray, hair serum, hair essence, body lotion, shower gel and body spray, but is not limited thereto.

[0073] The cosmetic composition of the present invention includes all the contents of the elastic liposome composition of the present invention described above.

[0074] The elastic liposome composition of the present invention and the cosmetic composition containing the same will be specifically described by the following examples, comparative examples and experimental examples. These examples are only used to illustrate the present invention, and therefore the scope of the present invention is not interpreted as being limited by these examples.

[0075] [Example]

[0076] Examples 1 to 12

[0077] 0.002 g of quercetin was mixed with 100 g of a mixture of lecithin and a sucrose-based surfactant in [unit: weight %] as shown in Table 1. At this time, the mixing weight ratio of lecithin and sucrose-based surfactant in Table 1 was sorted and recorded in Table 2, and the values ​​in Table 2 were rounded off to the fourth decimal place and displayed only to the third decimal place.

[0078] Next, the mixture of the mixed lecithin and the sucrose-based surfactant was mixed with quercetin, and then an organic solvent in which methanol and chloroform were mixed at a ratio of 10:10 (v / v%) was mixed thereto and dissolved.

[0079] Thereafter, the organic solvent was completely removed using a rotary evaporator to form a thin lipid film on the wall surface, which was then hydrated with purified water to form elastic liposomes.

[0080] The elastic liposomes were homogenized in glass beads and then ultrasonically disrupted for 15 minutes to make the particle size more uniform. Untrapped quercetin was then removed using a 0.45 μm syringe filter (Minisart CA26 mm, Germany) to obtain an elastic liposome composition.

[0081] [Table 1]

[0082] Lecithin Sucrose Monostearate Sucrose Distearate Sucrose tristearate Example 1 97.5 2.5 - - Example 2 95 5 - - Example 3 90 10 - - Example 4 80 20 - - Example 5 97.5 - 2.5 - Example 6 95 - 5 - Example 7 90 - 10 - Example 8 80 - 20 - Example 9 97.5 - - 2.5 Example 10 95 - - 5 Embodiment 11 90 - - 10 Example 12 80 - - 20

[0083] [Table 2]

[0084] Lecithin Sucrose Monostearate Sucrose Distearate Sucrose tristearate Example 1 1 0.026 - - Example 2 1 0.053 - - Example 3 1 0.111 - - Example 4 1 0.250 - - Example 5 1 - 0.026 - Example 6 1 - 0.053 - Example 7 1 - 0.111 - Example 8 1 - 0.250 - Example 9 1 - - 0.026 Example 10 1 - - 0.053 Embodiment 11 1 - - 0.111 Example 12 1 - - 0.250

[0085] Embodiment 13

[0086] Prepared in the same manner as Example 7, except that catechin was used instead of quercetin.

[0087] Embodiment 14

[0088] Prepared in the same manner as Example 7, except that apigenin was used instead of quercetin.

[0089] Embodiment 15

[0090] Prepared in the same manner as Example 7, except that myricetin was used instead of quercetin.

[0091] Example 16

[0092] The same preparation as Example 7 was performed except that luteolin was used instead of quercetin.

[0093] Embodiment 17

[0094] The same preparation as Example 7 was performed except that fisetin was used instead of quercetin.

[0095] [Comparative Example]

[0096] Comparative Examples 1 to 3

[0097] The same method as in Example 1 was carried out except that lecithin and sucrose monostearate were mixed at the weight ratio shown in Table 3 [Unit: weight ratio] and used.

[0098] [Table 3]

[0099] Lecithin Sucrose Monostearate Comparative Example 1 1 - Comparative Example 2 1 0.001 Comparative Example 3 1 0.4

[0100] Comparative Examples 4 to 6

[0101] Prepared in the same manner as Example 1, except that the surfactant of Table 4 was used instead of sucrose monostearate.

[0102] [Table 4]

[0103] Surfactants Comparative Example 4 PEG-100 stearate Comparative Example 5 Sucrose palmitate Comparative Example 6 Sucrose myristate

[0104] [Experimental example]

[0105] Experimental Example 1: Physical Property Measurement

[0106] In the elastic liposome compositions according to Examples 1 to 17 and Comparative Examples 1 to 6, the particle size (nm), zeta potential (Zeta potential, mV), quercetin encapsulation efficiency (Encapsulation Efficiency, %) and deformability (Deformability Index) of the elastic liposomes were evaluated, and the results are shown in Table 5.

[0107] At this time, the above-mentioned physical properties were measured according to the following methods.

[0108] (1) Particle size and zeta potential: Measured using Microtrac Flex (Microtrac, USA) using light scattering. The above average particle size is shown by cumulative analysis, and the distribution is explained by the contin method. At this time, the measurement conditions of particle size and zeta potential are as follows.

[0109] -Temperature: 25°C, Scattering angle: 165°, Light source: Argon laser

[0110] (2) Capture efficiency of quercetin : Take a certain amount of the elastic liposome composition of Examples 1 to 17 or Comparative Examples 1 to 6, then remove the uncaptured quercetin with a 0.45 μm syringe filter (Minisart CA 26 mm, Germany), and repeat the same operation 3 times to remove the uncaptured quercetin. Take 1 ml of the elastic liposome composition from which the uncaptured quercetin was removed, and mix 10 ml of ethanol therein to destroy the lipid membrane of the liposome.

[0111] Thereafter, the solvent was evaporated using a rotary evaporator, and then 1 mL of ethanol was added thereto, and the quercetin trapped in the elastic liposomes was quantitatively analyzed using a UV-vis spectrometer. At this time, the water bath temperature of the rotary evaporator was maintained at about 35°C.

[0112] In addition, a calibration curve of quercetin was prepared according to the concentration, the concentration of quercetin trapped in the liposome was calculated, and the "quercetin trapping efficiency of elastic liposomes" was calculated by Formula 1. On the other hand, for Examples 13 to 17, the trapping efficiencies of catechin, apigenin, myricetin, luteolin, and fisetin were measured and calculated instead of quercetin, and the results are shown in Table 5.

[0113] [Formula 1] Loading efficiency (%) = (TP) / Tx100

[0114] T: Initial concentration of quercetin added

[0115] P: Concentration of quercetin that does not pass through a 0.45 μm syringe filter

[0116] (3) Deformability:Measure the degree of elastic liposomes passing through artificial permeability barriers with a mini extruder. In more detail, a pressure of 0.2 MPa is applied to the elastic liposomes for 1 minute and 30 seconds, and then the amount of elastic liposomes released through a polycarbonate membrane with a hole of 0.08 μm is measured, and the particle size of the liposomes passing therethrough is measured. At this time, the elasticity of the elastic liposome membrane is proportional to the following formula 2.

[0117] [Formula 2] Deformability index = J Flux X(r v / r p ) 2

[0118] J Flux : The amount of elastic liposomes passing through the membrane

[0119] r v : Particle size of liposomes after extrusion

[0120] r p :The pore size of the membrane

[0121] [Table 5]

[0122]

[0123] Referring to Table 5, it can be seen that the elastic liposomes of this example are formed into particles with a size of 70 to 200 nanometers.

[0124] In addition, it can be seen that the elastic liposome of this example has a zeta potential similar to or lower than that of Comparative Example 1 corresponding to the general liposome. This means that the elastic liposome of this example has a state similar to or more stable than that of the general liposome.

[0125] In addition, it can be seen that the elastic liposomes of this example showed a higher "quercetin capture efficiency (%)" compared to Comparative Examples 1 to 6. In particular, when Examples 1 to 12 are compared, it can be seen that when sucrose distearate is included as a sucrose-based surfactant, the capture efficiency of quercetin is more excellent. In addition, in Examples 4 to 8, it can be seen that when the mixing weight ratio of lecithin and sucrose distearate is 1:0.111, the quercetin capture efficiency is the most excellent.

[0126] In addition, it can be seen that the elastic liposome of this example shows higher deformability than that of Comparative Examples 1 to 6. In particular, when Examples 1 to 12 are compared, it can be seen that when sucrose distearate is included as a sucrose-based surfactant, the deformability is more excellent. In addition, in Examples 4 to 8, it can be seen that when the mixing weight ratio of lecithin and sucrose distearate is 1:0.111, the deformability efficiency is most excellent.

[0127] Additionally, when comparing Example 7 with Examples 13 to 17, it can be seen that, in addition to quercetin, even when other types of flavonoids such as catechin, apigenin, myricetin, luteolin, and fisetin are used, elastic liposomes are formed into particle sizes of 70 to 200 nanometers and maintain characteristics such as low zeta potential, excellent effective ingredient capture efficiency (%), and excellent deformability.

[0128] In addition, TEM (transmission electron microscopy) images of the elastic liposome compositions of (A) Comparative Example 1, (B) Example 3, (C) Example 7, and (D) Example 11 are shown in Figure 1 middle.

[0129] See also Figure 1 It can be seen that the elastic liposomes of this embodiment have a particle size of about 70 to 200 nanometers.

[0130] Experimental Example 2: Stability Evaluation

[0131] The stability of Examples 1 to 12 and Comparative Examples 1 to 6 was evaluated, and the results are shown in Tables 6 and 7.

[0132] (1) Storage stability First, the particle size of the elastic liposome composition immediately after preparation was compared with the particle size (average value, unit: nanometer) of the elastic liposome composition after storage at about 4°C for 12 weeks, and the results are shown in Table 6. At this time, the particle size was measured by the same method as in Experimental Example 1.

[0133] [Table 6]

[0134] Just after preparation 12 weeks later (4℃) Example 1 81.2±2.2 85.0±2.5 Example 2 88.3±2.7 90.6±3.1 Example 3 98.0±3.0 100.1±3.5 Example 4 77.3±5.5 183.6±21.5 Example 5 99.3±2.6 101.2±3.1 Example 6 112.2±3.3 114.6±3.5 Example 7 125.3±2.6 128.6±3.3 Example 8 105.2±6.2 108.2±3.3 Example 9 122.9±3.1 128.4±3.5 Example 10 138.6±2.5 142.6±3.3 Embodiment 11 152.7±2.1 156.2±3.5 Example 12 158.2±3.6 193.1±20.2 Comparative Example 1 78.4±1.2 82.6±2.2 Comparative Example 2 72.2±0.2 99.4±1.1 Comparative Example 3 61.3±3.4 87.9±0.9 Comparative Example 4 52.4±1.2 83.6±2.1 Comparative Example 5 57.7±2.0 85.9±1.6 Comparative Example 6 59.2±1.1 90.1±4.2

[0135] As shown in Table 6, the elastic liposomes according to this embodiment have better stability than those of the comparative examples.

[0136] However, in the elastic liposome according to the present example, it can be seen that the stable state of the elastic liposome cannot be maintained for Examples 4 and 12 containing lecithin and a sucrose-based surfactant at a weight ratio of 1:0.250. That is, it means that when lecithin and a sucrose-based surfactant are contained at a weight ratio of 1:0.02 to 0.20, elastic liposomes in a more stable state can be formed.

[0137] In addition, it was confirmed that the elastic liposome according to this example and general liposomes have similar levels of stability.

[0138] (2) Acceleration stability : Accelerated stability test was performed using LUMiSizer (using space and time-resolved extinction profiles [STEP] technology). The instability of each elastic liposome was confirmed by measuring the transmittance, and the results are shown in Table 7 as the instability index. At this time, the instability index has a value between 0 and 1, 0 representing a stable state with no change in transmittance and 1 representing an unstable state with complete phase separation.

[0139] In the accelerated stability test, after the elastic liposome composition was subjected to pressure at about 1,500 rpm at 30° C. for 12 hours, the light transmittance was measured at intervals of 60 seconds to measure its instability index.

[0140] [Table 7]

[0141] Instability Index Instability Index Example 1 0.110±0.02 Comparative Example 1 0.100±0.02 Example 2 0.120±0.007 Comparative Example 2 0.607±0.24 Example 3 0.110±0.005 Comparative Example 3 0.542±0.11 Example 4 0.450±0.08 Comparative Example 4 0.710±0.31 Example 5 0.150±0.03 Comparative Example 5 0.657±0.22 Example 6 0.120±0.04 Comparative Example 6 0.612±0.39 Example 7 0.110±0.03 Example 8 0.410±0.09 Example 9 0.190±0.05 Example 10 0.180±0.05 Embodiment 11 0.150±0.03 Example 12 0.510±0.11

[0142] Referring to Table 7, it can be seen that, for this example, compared with the comparative example, the accelerated stability of the elastic liposome is excellent overall.

[0143] However, in the elastic liposome according to the present example, it can be seen that the accelerated stability of the elastic liposome is low for Examples 4, 8 and 12, which contain lecithin and a sucrose-based surfactant at a weight ratio of 1:0.250. That is, it is shown that when lecithin and a sucrose-based surfactant are contained at a weight ratio of 1:0.02 to 0.20, elastic liposomes in a more stable state can be formed.

[0144] In addition, it was confirmed that the elastic liposome according to this example and the general liposome had similar levels of accelerated stability.

[0145] Experimental Example 3: Skin permeability evaluation

[0146] Examples 1 to 12 and Comparative Examples 1 to 6 were evaluated for skin permeability, and the results thereof are shown in Table 8.

[0147] Skin permeability was evaluated using a Franz diffusion cell, and the permeation amount of quercetin per skin area was measured from 0 to 12 hours, and the final cumulative skin permeation amount of quercetin after about 12 hours was measured and shown in Table 8. At this time, the above-mentioned skin permeation test conditions were as follows.

[0148] -λmax(nm):258

[0149] -Detecting: UV-spectrometer

[0150] - Calibration curve: y = 0.0585x + 0.013

[0151] -Solvent: Receptor phase

[0152] - Slope: 0.0585

[0153] -y-intercept: 0.013

[0154] - Transepidermal area (cm 2 ):0.6362

[0155] - Sample amount applied per unit area (μg / cm 2 ):30.40

[0156] -Sample volume (dosage form): 0.2mL, 20μg, standard dosage form concentration (0.001g / 10mL)

[0157] - Infiltration solution (0h~12h): Take 0.3mL from 5mL

[0158] -Tape, Skin Solution: 7mL EtOH

[0159] In addition, an experiment was performed in which 1,3-butanediol was added instead of the elastic liposome as a control group.

[0160] [Table 8]

[0161]

[0162] It can be seen from Table 8 that, for this example, compared with Comparative Examples 1 to 6 and the control group, the skin permeability of the active ingredient is significantly improved.

[0163] In particular, from Examples 1 to 12 corresponding to the elastic liposomes according to the present embodiment and Comparative Example 1 which is a conventional liposome, the skin permeation amount of the active ingredient is significantly higher for the elastic liposomes than for the conventional liposomes, which means that the skin permeability of the elastic liposomes according to the present embodiment is significantly excellent.

[0164] On the other hand, it can be seen that although Examples 1 to 12 according to the present embodiment are excellent in skin permeability compared with the comparative example, the skin permeability is slightly reduced for Examples 4, 8 and 12 which do not contain lecithin and sucrose-based surfactants in a weight ratio of 1:0.02 to 0.20.

[0165] In addition, the changes in the skin permeation amount of quercetin corresponding to 1,3-butanediol of the control group and Comparative Example 1, Example 3, Example 7 and Example 11 over time are shown in Figure 2 middle.

[0166] See also Figure 2 It can be seen that Examples 3, 7 and 11 comprising the elastic liposomes prepared according to this Example show significantly superior skin permeation efficiency compared to Comparative Example 1 which is a general liposome. In particular, it can be seen from Examples 3, 7 and 11 that the skin permeation efficiency of Example 7 comprising sucrose distearate as a sucrose-based surfactant is significantly superior.

[0167] In addition, after about 12 hours, the amount of quercetin that penetrated the skin was quantified to measure the content (%), and it was divided into the amount present in the stratum corneum (Tape), the amount present in the skin (epidermis and dermis) (Skin) and the amount through the skin (Transdermal), and the results are shown in Figure 3 middle.

[0168] See also Figure 3 It can be seen that the total permeation amount of quercetin in Examples 3, 7 and 11 containing elastic liposomes is significantly higher than that in the control group or Comparative Example 1 containing general liposomes. That is, it can be seen that the skin permeation rate of flavonoids can be significantly improved when elastic liposomes are used compared with the use of general liposomes or simple solvents.

[0169] In addition, if Figure 2 As shown, referring to Examples 3, 7 and 11, it can be seen that the quercetin content of Example 7 is significantly higher, and it can be seen that when sucrose distearate with two stearic acids attached in the ester compound of sucrose and stearic acid is used, the skin permeability is significantly improved.

[0170] As described above, the description of the present invention is for illustration, and it will be appreciated by those skilled in the art that the present invention can be easily transformed into other specific forms without changing the technical concept or necessary features of the present invention. Therefore, it should be understood that the embodiments described above are exemplary and non-restrictive in all aspects. For example, each component described as a single type may also be implemented in a dispersed manner, and similarly, the components described as dispersed may also be implemented in a combined form.

[0171] The scope of the present invention is indicated by the claims described below rather than the detailed description above, and should be interpreted as including all changes or modifications derived from the meaning and scope of the claims and their equivalents within the scope of the present invention.

Claims

1. An elastic liposome composition, characterized in that: Include: Lecithin; and Sucrose-based surfactants including sucrose distearate, The elastic liposome composition comprises the lecithin and the sucrose-based surfactant in a weight ratio of 1:0.02 to 0.

15.

2. The elastic liposome composition according to claim 1, characterized in that The particle size of the elastic liposome is 70 to 200 nanometers.

3. The elastic liposome composition according to claim 1, characterized in that The elastic liposome composition further comprises flavonoids, The flavonoids include at least one selected from the group consisting of quercetin, catechin, apigenin, myricetin, luteolin and fisetin. A cosmetic composition comprising the elastic liposome composition according to claim 1.

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