CN111249185A - Nano lipid carrier for embedding idebene and preparation method and application thereof - Google Patents

Nano lipid carrier for embedding idebene and preparation method and application thereof Download PDF

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CN111249185A
CN111249185A CN202010197258.0A CN202010197258A CN111249185A CN 111249185 A CN111249185 A CN 111249185A CN 202010197258 A CN202010197258 A CN 202010197258A CN 111249185 A CN111249185 A CN 111249185A
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idebene
lipid carrier
nano lipid
embedding
surfactant
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陈宝祺
庞文心
潘颀钧
李秋涛
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Shanghai Gelan Cosmetics Co ltd
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Shanghai Gelan Cosmetics Co ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55—Phosphorus compounds
    • A61K8/553—Phospholipids, e.g. lecithin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/14—Liposomes; Vesicles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/345—Alcohols containing more than one hydroxy group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/35—Ketones, e.g. benzophenone
    • A61K8/355—Quinones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/56—Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms

Abstract

The invention provides a nano lipid carrier for embedding idebene and a preparation method and application thereof, and relates to the technical field of cosmetics. The nano lipid carrier provided by the invention comprises the following components in percentage by mass: 10-30% of Hawaii bean oil; 5-15% of palm wax; 1-5% of idebene; 6-10% of a surfactant; 1-5% of polyol; 0.5-1.5% of lecithin; the balance of water. According to the invention, the idebene is coated by the combination of macadamia oil, palm wax, a surfactant, a polyalcohol and lecithin, so that the provided nano lipid carrier for embedding the idebene has the advantages of good stability, high embedding rate, high drug loading capacity and good skin absorbability, and can be well applied to cosmetics. The invention provides a preparation method of an idebene-embedded nano lipid carrier, which adopts a thermal high-pressure homogenization technology and can effectively realize the stable embedding of the nano lipid carrier on the idebene.

Description

Nano lipid carrier for embedding idebene and preparation method and application thereof
Technical Field
The invention relates to the technical field of cosmetics, and particularly relates to an idebene-embedded nano lipid carrier, and a preparation method and application thereof.
Background
With the progress of society and the continuous improvement of living standard, people pay more attention to skin maintenance and care, maintenance products on the market are numerous, the maintenance products are rich in active ingredients, and the functions of repairing, moisturizing or moistening can be realized. Idebenone (Idebenone) is a fat-soluble orange substance, is a new generation antioxidant, and is applied to partial maintenance products in recent years. The antioxidant effect of the idebene is superior to that of levorotatory C, vitamin A, vitamin E and coenzyme Q10, and the idebene becomes one of popular components of the anti-aging health care product.
How to slow down the release of active ingredients in the care product, avoid instability and promote the active ingredients to be really transferred to the bottom layer of skin is always the key point of developing the care product, and the carrier is a good choice for embedding the active ingredients. The carrier in the prior art mainly comprises a microcapsule, an emulsion and a microemulsion, wherein the microcapsule can be prepared into the microemulsion, a composite emulsion and solid particles, can be well combined with an excipient and is easy to manufacture in a large scale; although the liposome has the effects of protecting the active compound in the vesicle against chemical degradation and regulating the release of the active compound, the application of the liposome is affected by the problems of difficult storage, rapid leakage of the substance in the vesicle, unstable structure due to the action of the hydrophilic substance in the vesicle and the double-layer membrane, unstable encapsulation of the substance in the vesicle, unstable substance in the vesicle and the like. In recent years, nanostructured lipid carriers are developed and applied, and the carriers have many excellent characteristics and are expected to replace traditional carriers and microcapsules. However, the research on the nanostructure lipid carrier is relatively less, and the research on coating the idebene with the nanostructure liposome is not reported.
Disclosure of Invention
In view of the above, the present invention aims to provide an idebene-embedded nano lipid carrier, and a preparation method and an application thereof. The nano lipid carrier for embedding the idebene provided by the invention has the advantages of good stability, high embedding rate, high drug loading capacity and good skin absorbability, and can be well applied to cosmetics.
In order to achieve the above object, the present invention provides the following technical solutions:
the invention provides an idebene-embedded nano lipid carrier, which comprises the following components in percentage by mass:
Figure BDA0002418073600000011
Figure BDA0002418073600000021
the balance of water.
Preferably, the surfactant is a non-ionic surfactant; the non-ionic surfactant is one or more of Tween 80, Poloxamer 188 and decyl glucoside.
Preferably, the polyol comprises 1, 2-pentanediol and/or 1, 2-hexanediol.
Preferably, the lecithin is soybean lecithin.
The invention provides a preparation method of the idebene-embedded nano lipid carrier in the scheme, which comprises the following steps:
(1) mixing and heating macadamia oil, palm wax and ideben to obtain an oil phase;
(2) mixing and heating water, polyalcohol, a surfactant and lecithin to obtain a water phase;
(3) adding the oil phase into the water phase to obtain a mixed phase;
(4) pre-emulsifying and homogenizing the mixed phase under high pressure in sequence to obtain a nano lipid carrier embedded with the idebene;
the step (1) and the step (2) have no time sequence limitation.
Preferably, the heating temperature in the step (1) and the heating temperature in the step (2) are independently 85-90 ℃.
Preferably, the temperature of the mixed phase in the step (3) is 85-90 ℃.
Preferably, the pre-emulsification in the step (4) is performed by using an emulsifying machine; the rotation speed of the pre-emulsification is 5000-15000 rpm, and the pre-emulsification time is 3-10 min.
Preferably, the high-pressure homogenization in the step (4) is performed by using a high-pressure homogenizer; the pressure of the high-pressure homogenizing is 300-800 bar, and the cycle time is 4-8 times.
The invention provides an application of the idebene-embedded nano lipid carrier in the scheme or the idebene-embedded nano lipid carrier prepared by the preparation method in the technical scheme in cosmetics.
The invention provides an idebene-embedded nano lipid carrier, which comprises the following components in percentage by mass: 10-30% of Hawaii bean oil; 5-15% of palm wax; 1-5% of idebene; 6-10% of a surfactant; 1-5% of polyol; 0.5-1.5% of lecithin; the balance of water. According to the invention, the idebene is coated by the combination of macadamia oil, palm wax, a surfactant, a polyalcohol and lecithin, so that the provided nano lipid carrier for embedding the idebene has the advantages of good stability, high embedding rate, high drug loading capacity and good skin absorbability, and can be well applied to cosmetics.
The invention provides a preparation method of an idebene-embedded nano lipid carrier, which adopts a thermal high-pressure homogenization technology and can effectively realize the stable embedding of the nano lipid carrier on the idebene.
Drawings
FIG. 1 is a DSC chart of sample No. 1;
FIG. 2 is a DSC plot of sample No. 2;
FIG. 3 is a DSC plot of sample No. 3;
FIG. 4 is a DSC plot of sample No. 4;
FIG. 5 is a DSC plot of sample No. 5;
FIG. 6 is a DSC plot of sample No. 6;
FIG. 7 is a DSC chart of sample No. 7;
FIG. 8 is a DSC chart of sample No. 8;
FIG. 9 is a DSC chart of sample No. 9;
FIG. 10 is a graph of the digoxibenzene assay;
FIG. 11 is a graph showing the relationship between the relative flux (Y) and the concentration (C) of samples No.10 to No. 13.
Detailed Description
The invention provides an idebene-embedded nano lipid carrier, which comprises the following components in percentage by mass:
Figure BDA0002418073600000031
the balance of water.
The idebene-embedded nano lipid carrier provided by the invention comprises 10-30% by mass of Hawaii soybean oil, and preferably 25% by mass of Hawaii soybean oil. The macadamia nut oil contains minerals, proteins and polyunsaturated fatty acids, and mainly contains oleic acid, palmitoleic acid, linoleic acid, linolenic acid and triglyceride, wherein the oleic acid has moisturizing and anti-aging effects; palmitoleic acid is an essential fatty acid, has skin-friendly and high skin moistening effects, and is an indispensable component for delaying skin and cell aging; the triglyceride is mainly unsaturated fatty acid unit, and the oil has good maintenance effect. Hawaii bean oil is cheap and easy to obtain, and the components of the oil are similar to those of grease secreted by sebaceous glands in vivo, and main fatty acid contained in the oil has the characteristic of protection. The source of the Hawaii soybean oil is not particularly required in the invention, and a commercially available product well known to those skilled in the art can be adopted.
The idebene-embedded nano lipid carrier provided by the invention comprises 5-15% of palm wax by mass percentage, and preferably 10% of palm wax by mass percentage. The palm wax can adjust the consistency of oily products, increase the skin luster and has the effect of softening and moistening the skin. The source of the palm wax is not particularly critical to the present invention and commercially available products well known to those skilled in the art may be used.
The nano lipid carrier for embedding the idebene comprises 1-5% of the idebene, and preferably 3-5% of the idebene by mass percentage. Adiantum (C)19H30O5The structure is shown as formula A) is a new generation antioxidant, which is composed of coenzyme Q10 (C)59H90O4The structural formula is shown as formula B), but the molecule of the antioxidant is 60 percent smaller than that of Q10, and the penetrating power to skin is better, so that the antioxidant effect is more obvious; q10 is converted from oxidation resistance to autooxidation under anoxic conditions to produce free radicals, which is not the risk of idebene; under the comparison standard of mass concentration of 1%, the antioxidant effect of the idebenone is better than that of levorotatory C, vitamin A, vitamin E and coenzyme Q10. The present invention does not require any particular source for the idebene and may employ commercially available or self-prepared products.
Figure BDA0002418073600000041
The idebene-embedded nano lipid carrier provided by the invention comprises 6-10% of a surfactant, preferably 8-10% by mass. In the present invention, the surfactant is preferably a nonionic surfactant; the non-ionic surfactant is preferably one or more of Tween 80, Poloxamer 188 and decyl glucoside. The surfactant adopted by the invention has good emulsifying effect, wherein Poloxamer 188 can form a three-dimensional effect, thereby avoiding particle agglomeration; decyl glucoside is a mild nonionic type co-surfactant, is synthesized by glucose prepared from corn and coconut and fatty acid alcohol, can be compatible with any surfactant, has higher foaming stability and good wetting property, can improve the conditioning effect of a cationic surfactant, also has the function of maintaining the moisture balance of the skin and preventing the skin from being dry and astringent, and has the characteristics of easy biodegradation, extreme mildness, no irritation, low toxicity and the like because the surfactant is derived from saccharides. The source of the surfactant is not particularly required in the present invention, and commercially available products well known in the art may be used.
The idebene-embedded nano lipid carrier provided by the invention comprises 1-5% of polyol by mass percentage, and preferably 2%. In the present invention, the polyhydric alcohol preferably includes 1, 2-pentanediol and/or 1, 2-hexanediol; the 1, 2-pentanediol or 1, 2-hexanediol is a small molecular material, has good moisturizing effect and has the functions of lubrication, bacteriostasis and the like. The source of the polyol is not particularly critical to the present invention and commercially available products well known in the art may be used.
The idebene-embedded nano lipid carrier provided by the invention comprises 0.5-1.5% of lecithin by mass percentage, and preferably 1-1.5%. In the present invention, the lecithin is preferably soybean lecithin. The lecithin can promote the recovery of cells and keep the cells active, the lecithin is mainly composed of B-vitamin choline and also contains linoleic acid and inositol, and the lecithin is an ester and also has the function of an emulsifier. The source of the lecithin is not particularly required in the present invention, and a commercially available product well known in the art may be used.
The idebene-embedded nano lipid carrier provided by the invention comprises the balance of water in percentage by mass. The water is not particularly required in the present invention, and water well known in the art may be used.
According to the invention, the idebene is coated by the combination of macadamia oil, palm wax, a surfactant, a polyalcohol and lecithin, so that the provided nano lipid carrier for embedding the idebene has the advantages of good stability, high embedding rate, high drug loading capacity and good skin absorbability.
The invention provides a preparation method of an idebene-embedded nano lipid carrier, which comprises the following steps:
(1) mixing and heating macadamia oil, palm wax and ideben to obtain an oil phase;
(2) mixing and heating water, polyalcohol, a surfactant and lecithin to obtain a water phase;
(3) adding the oil phase into the water phase to obtain a mixed phase;
(4) pre-emulsifying and homogenizing the mixed phase under high pressure in sequence to obtain a nano lipid carrier embedded with the idebene;
the step (1) and the step (2) have no time sequence limitation.
According to the invention, Hawaii soybean oil, palm wax and idebene are mixed and heated to obtain an oil phase. In the invention, the heating temperature is preferably 85-90 ℃. In the invention, the Hawaii soybean oil and the palm wax are preferably mixed and heated to the required temperature, and then the idebene is added into the mixture for mixing. The present invention does not require any particular time for the mixing, and the william oil, the carnauba wax, and the idebene can be sufficiently dissolved and mixed.
According to the invention, water, polyalcohol, a surfactant and lecithin are mixed and heated to obtain a water phase. In the invention, the heating temperature is preferably 85-90 ℃. The invention has no special requirement on the sequence of mixing the water, the polyalcohol, the surfactant and the lecithin, and the water, the polyalcohol, the surfactant and the lecithin can be mixed in any sequence. The time for the mixing is not particularly required in the present invention, and the water, the polyol, the surfactant and the lecithin can be sufficiently dissolved and mixed.
After the oil phase and the water phase are obtained, the oil phase is added into the water phase to obtain a mixed phase. In the invention, the temperature of the mixed phase is preferably 85-90 ℃.
After the mixed phase is obtained, the mixed phase is sequentially pre-emulsified and homogenized under high pressure to obtain the nano lipid carrier embedded with the idebene. In the present invention, the pre-emulsification is preferably performed using an emulsifying machine; the rotation speed of the pre-emulsification is preferably 5000-15000 rpm, more preferably 8000rpm, and the time of the pre-emulsification is preferably 3-10 min, more preferably 5 min. In the present invention, the high-pressure homogenization is preferably performed using a high-pressure homogenizer; the pressure of the high-pressure homogenization is preferably 300-800 bar, more preferably 700bar, and the cycle number is preferably 4-8 times, more preferably 5 times. After high-pressure homogenization, the emulsion obtained is preferably cooled; the cooling is preferably natural cooling; and cooling to obtain the idebene-embedded nano lipid carrier.
The preparation method provided by the invention adopts a hot high-pressure homogenization technology, and can effectively realize the stable embedding of the nano lipid carrier on the idebene.
The invention provides an application of the idebene-embedded nano lipid carrier in cosmetics. The nano lipid carrier provided by the invention has the advantages of good stability, high embedding rate, high drug loading rate and good skin absorbability, and can be well applied to cosmetics.
The idebene-embedded nano lipid carrier provided by the invention, the preparation method and the application thereof are described in detail by combining with the examples below, but the invention is not to be construed as being limited by the scope of the invention.
Example 1
The idebene-embedded nano lipid carrier comprises the following components in percentage by mass as shown in Table 1, and is prepared by the following steps:
(1) heating macadamia oil and carnauba wax to 90 ℃ at constant temperature, adding idebene, and dissolving macadamia oil, carnauba wax and idebene to obtain an oil phase;
(2) heating water, 1, 2-pentanediol, a surfactant and soybean lecithin to 90 ℃ at constant temperature, and dissolving to obtain a water phase;
(3) adding the oil phase into the water phase, and keeping the temperature at 90 ℃ to obtain a mixed phase;
(4) pre-emulsifying the mixed phase by using an emulsifying machine, wherein the rotating speed of the emulsifying machine is 8000rpm, and the pre-emulsifying time is 5 min; and feeding the pre-emulsified sample into a high-pressure homogenizer, pressurizing to an operating pressure of 700bar in the high-pressure homogenizer, circulating for 5 times, and naturally cooling to room temperature to obtain the nano lipid carrier embedded with the idebene.
Examples 2 to 9
The difference between the nano lipid carrier for embedding idebene and the nano lipid carrier in the example 1 is that the components and the corresponding mass percentage content are shown in the table 1.
Table 1 Each component and corresponding mass percentage content in examples 1-9
Figure BDA0002418073600000071
Figure BDA0002418073600000081
The particle diameter, the interface potential, the crystallinity and the embedding rate of the idebene-embedded nano lipid carriers (No.1 to No.9) prepared in examples 1 to 9 were measured:
(1) particle size detection
The size and distribution of the particle size are important for the stability of the system, and Table 2 shows the average particle size data of the nano lipid carriers (NO. 1-NO. 9) for 1-56 days. As shown in Table 2, the average particle size of the prepared idebene-embedded nano lipid carrier stored for 1 day is 161-919 nm, and the particle size change is stable after 56 days.
TABLE 2 mean particle size data for idebene-embedded nano-lipid carriers at different storage times
Figure BDA0002418073600000082
(2) Interface potential detection
The interfacial potential can be used to evaluate the physical stability of lipid carrier, and generally, the interfacial potential above-30 mV means that the system is in a stable state and the aggregation of particles is low, mainly because of the electrostatic repulsion between colloidal particles. Table 3 shows the data of the interface potential of the nano lipid carriers (NO. 1-NO. 9) for 1-56 days. As can be seen from Table 3, the interface potential of each sample remained above-30 mV after long-term storage, indicating that each sample was maintained in a steady state.
TABLE 3 interfacial potential data for idebene-embedded nano-lipid carriers at different storage times
Figure BDA0002418073600000091
(3) Crystallinity detection
Firstly, freeze-drying a sample to remove water,then, the mixture is analyzed by a DSC/TGA thermal analyzer; the enthalpy value of the sample can be obtained from a DSC analysis chart, the enthalpy value of the palm wax is 16.10J/g, and the enthalpy value (Delta H) of the samplesample) And the enthalpy value (. DELTA.H) of the palm waxpure) The degree of crystallinity CI can be determined with formula I:
Figure BDA0002418073600000092
in the formula I,. DELTA.HsampleAnd Δ HpureRespectively, the enthalpies of fusion of the dispersed phase of the lipid carrier and the lipid phase.
FIGS. 1 to 9 are DSC graphs of samples No.1 to No.9, respectively, and it can be seen from FIGS. 1 to 9 that each sample has a single peak showing good compatibility among the components.
Table 4 shows the crystallinity data of samples No.1 to No.9, and it can be seen from Table 4 that the crystallinity of samples No.1 to No.9 is between 13.75 to 67.50%, and the drug-loading capacity of the active substance in the samples is about 32.5 to 86%.
TABLE 4 crystallinity data for samples No.1 to No.9
Sample (I) Mp(℃) △H(J/g) CI(％)
Palm wax 66.67 16.10 100
NO.1 58.94 2.214 13.75
NO.2 53.32 10.87 67.51
NO.3 53.16 8.54 53.04
NO.4 58.98 3.254 20.21
NO.5 53.96 9.713 60.33
NO.6 56.89 6.121 38.01
NO.7 59.62 9.935 61.70
NO.8 58.75 6.858 42.59
NO.9 58.17 8.727 54.20
(4) Detection of embedding Rate
The embedding rate was analyzed by UV/visible spectrophotometer, and calibration lines were prepared at five spots of concentrations of 1ppm, 10ppm, 25ppm, 100ppm, and 500ppm, as shown in FIG. 10, R20.9998, indicating that the calibration curve is referable; detecting the absorbance of the sample by using an ultraviolet/visible light spectrophotometer, substituting the obtained absorbance into a Y value of a detection line to obtain the concentration of the sample, and calculating the embedding rate by using a formula II:
the inclusion ratio (%) - (addition concentration-sample concentration)/addition concentration × 100% formula ii.
Table 5 shows the embedding rate data of samples No.1 to No.9, and Table 5 shows that the samples No.1 to No.9 can realize 61.48 to 81.20 percent of effective embedding, and the embedding rate is high.
TABLE 5 entrapment Rate data for samples NO1 through NO9
Figure BDA0002418073600000101
Figure BDA0002418073600000111
Examples 10 to 13
The difference between the nano lipid carrier for embedding idebene and the nano lipid carrier in the embodiment 1 is that the components and the corresponding mass percentage content are shown in the following table 6:
table 6 shows the components and the corresponding mass percentages in examples 10 to 13
Figure BDA0002418073600000112
(1) The particle size, interface potential, crystallinity and embedding rate of the idebene-embedded nano lipid carriers (No.10 to No.13) prepared in examples 10 to 13 were measured (stored for one day), and the results are shown in table 7:
TABLE 7 data on particle size, interface potential, crystallinity, embedding rate of samples No.10 to No.13
Figure BDA0002418073600000113
Figure BDA0002418073600000121
(2) Transdermal absorption tests were performed on the idebene-embedded nano-lipid carriers (No.10 to No.13) prepared in examples 10 to 13:
the concentration of idebene was analyzed using 50nm VMWP membranes (Millipore) to simulate human skin, and the concentration was converted to diffusion flux as shown in Table 8, for four sets of experiments, each for 8hr, with samples taken every 2 hours. 8hr of experiment showed that the concentration (C) was 7.646X 10-4～8.892×10-3The relative flux (Y) between M is 409-5702 mu g/cm2And the calculated diffusion flux (J)A) At 204.5-1255.4 mu g/h cm2In the meantime. The diffusion coefficient obtained is of the order of 10, as shown by the semi-infinite solid diffusion mode-6m2And about/s. Therefore, the prepared nano lipid carrier for embedding the idebene has a good skin absorption effect.
TABLE 8 results of percutaneous absorption of samples No.10 to No.13
Figure BDA0002418073600000122
Figure BDA0002418073600000131
Furthermore, the relative flux (Y) is plotted against the concentration (C), as shown in fig. 11, which shows a linear relationship indicating the effect of the uniformity of the diffusion in the thin film, although the concentration and the condition are different for each group.
The embodiment shows that the idebene-embedded nano lipid carrier provided by the invention has the advantages of good stability, high embedding rate, high drug loading capacity and good skin absorbability, and thus can be well applied to cosmetics.
The foregoing is only a preferred embodiment of the present invention, and it should be noted that, for those skilled in the art, various modifications and decorations can be made without departing from the principle of the present invention, and these modifications and decorations should also be regarded as the protection scope of the present invention.

Claims (10)

1. The nano lipid carrier for embedding the idebene is characterized by comprising the following components in percentage by mass:
Figure FDA0002418073590000011
2. the idebene-embedded nano lipid carrier according to claim 1, characterized in that the surfactant is a non-ionic surfactant; the non-ionic surfactant is one or more of Tween 80, Poloxamer 188 and decyl glucoside.
3. The idebene-embedded nano lipid carrier according to claim 1, characterized in that the polyol comprises 1, 2-pentanediol and/or 1, 2-hexanediol.
4. The idebene-embedded nano lipid carrier according to claim 1, wherein the lecithin is soybean lecithin.
5. The method for preparing the idebene-embedded nano lipid carrier according to any one of claims 1 to 4, which comprises the following steps:
(1) mixing and heating macadamia oil, palm wax and ideben to obtain an oil phase;
(2) mixing and heating water, polyalcohol, a surfactant and lecithin to obtain a water phase;
(3) adding the oil phase into the water phase to obtain a mixed phase;
(4) pre-emulsifying and homogenizing the mixed phase under high pressure in sequence to obtain a nano lipid carrier embedded with the idebene;
the step (1) and the step (2) have no time sequence limitation.
6. The method according to claim 5, wherein the temperature of the heating in the step (1) and the heating in the step (2) are independently 85 to 90 ℃.
7. The method according to claim 5, wherein the temperature of the mixed phase in the step (3) is 85 to 90 ℃.
8. The method according to claim 5, wherein the pre-emulsification in the step (4) is performed using an emulsifying machine; the rotation speed of the pre-emulsification is 5000-15000 rpm, and the pre-emulsification time is 3-10 min.
9. The method according to claim 5, wherein the high-pressure homogenization in the step (4) is performed using a high-pressure homogenizer; the pressure of the high-pressure homogenizing is 300-800 bar, and the cycle time is 4-8 times.
10. Use of the idebene-embedded nano lipid carrier according to any one of claims 1 to 4 or the idebene-embedded nano lipid carrier prepared by the preparation method according to any one of claims 5 to 9 in cosmetics.
CN202010197258.0A 2020-03-19 2020-03-19 Nano lipid carrier for embedding idebene and preparation method and application thereof Pending CN111249185A (en)

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CN115363970A (en) * 2022-09-22 2022-11-22 广州金御化妆品有限公司 Water-soluble idebene liposome solution and preparation method thereof
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