阅读说明：本技术 一种祛痘纳米脂质载体及制备方法 (Acne-removing nano lipid carrier and preparation method thereof ) 是由 徐梦漪 温子敏 章皓星 朱永闯 郭韵 陈杰生 于 2020-05-11 设计创作，主要内容包括：本发明涉及化妆品技术领域,尤其涉及一种祛痘纳米脂质载体及制备方法。这种祛痘纳米脂质载体按照质量份,包括祛痘活性物1-10份、碱1-10份、固体脂质5-30份、液体脂质5-20份、油包水型乳化剂1-10份以及水包油型乳化剂1-10份。本申请将祛痘活性物负载在三相分散体系的纳米脂质载体上,能很好地解决稳定性差、刺激性强的水溶性活性物的包覆问题,使其有效发挥祛痘功效。且制备仅需要油脂、去离子水及乳化剂,仅需要加热及均质即可以完成制备,其产物在安全性、可操作性上具有一定的优势。(The invention relates to the technical field of cosmetics, in particular to an acne-removing nano lipid carrier and a preparation method thereof. The acne-removing nano lipid carrier comprises, by mass, 1-10 parts of acne-removing active substances, 1-10 parts of alkali, 5-30 parts of solid lipid, 5-20 parts of liquid lipid, 1-10 parts of a water-in-oil emulsifier and 1-10 parts of an oil-in-water emulsifier. According to the application, the acne-removing active substance is loaded on the nano lipid carrier of the three-phase dispersion system, so that the problem of coating of the water-soluble active substance with poor stability and strong irritation can be well solved, and the acne-removing effect can be effectively exerted. The preparation only needs grease, deionized water and an emulsifier, and can be completed only by heating and homogenizing, and the product has certain advantages in safety and operability.)

1. An acne-removing nano lipid carrier is characterized in that: the acne-removing cream comprises, by mass, 1-10 parts of an acne-removing active substance, 1-10 parts of alkali, 5-30 parts of solid lipid, 5-20 parts of liquid lipid, 1-10 parts of a water-in-oil emulsifier and 1-10 parts of an oil-in-water emulsifier.

2. The acne-removing nano lipid carrier according to claim 1, wherein: the acne removing active substance is salicylic acid; according to the mass parts, the chitosan-urea composite material also comprises 1-10 parts of chitosan, 0.1-2 parts of urea peroxide, 5-20 parts of acetic acid, 3-8 parts of glycerol and 15-20 parts of cyclodextrin.

3. The acne-removing nano lipid carrier according to claim 1, wherein: the solid lipid comprises one or more of stearyl alcohol, glyceryl tribehenate, cholesterol, glyceryl trimyristate, palmitoyl stearoyl glyceride, glyceryl tristearate, glyceryl monostearate, behenyl alcohol, lauric acid, glyceryl stearate citrate, hydrogenated castor oil, palmitic acid, palmityl alcohol, cetearyl alcohol, fatty alcohol and fatty acid.

4. The acne-removing nano lipid carrier according to claim 1, wherein: the liquid lipid comprises one or more of caprylic/capric triglyceride, isopropyl palmitate, isopropyl myristate, liquid paraffin, isooctyl palmitate hexyl laurate, 2-octyl lauryl alcohol, oleic acid, linoleic acid, soybean oil and olive oil.

5. The acne-removing nano lipid carrier according to claim 1, wherein: the water-in-oil emulsifier comprises one or more of glycerate citrate, sucrose stearate, ABIL EM-90, P135, Span20, Span40, Span60, Span80, Brij 72, Brij 721 and A6.

6. The acne-removing nano lipid carrier according to claim 1, wherein: the oil-in-water emulsifier comprises one or more of sorbitan sesquioleate, SS, SSE-20, A25, Novel A, Tween20, Tween40, Tween60, Tween80 and K12.

7. A method for preparing the acne-removing nano lipid carrier according to any one of claims 1 to 6, wherein the carrier comprises the following components in percentage by weight: the method comprises the following steps:

heating, liquefying and mixing solid lipid, liquid lipid and water-in-oil emulsifier to obtain oil phase; dissolving the acne removing active substance and alkali in deionized water to obtain an internal water phase; dissolving an oil-in-water type emulsifier in deionized water to obtain an external water phase;

heating the inner water phase to the temperature of the oil phase, and adding the inner water phase into the oil phase under the homogeneous condition to obtain a coarse emulsion; reducing the temperature of the 5-10 DEG coarse emulsion, and adding the cooled coarse emulsion into an external water phase under a homogeneous condition to obtain an emulsion; and cooling the emulsion to normal temperature after magnetically stirring to obtain the acne-removing nano lipid carrier.

8. The preparation method of the acne-removing nano lipid carrier according to claim 7, wherein the carrier comprises the following components in percentage by weight: the acne removing active substance also needs to be pretreated, and comprises the following steps:

preparing acetic acid into an acetic acid solution with the volume fraction of 2%, and dissolving chitosan in the acetic acid solution to obtain a solution 1; a solution 2 obtained by dissolving urea peroxide in glycerol; dropwise adding the solution 2 into the solution 1 while stirring to obtain a solution 3;

dissolving salicylic acid and cyclodextrin in water to obtain a solution 4, slowly dripping the solution 3 into the solution 4, stirring for 5-8h, standing at 2-5 ℃ for 18-24h, then carrying out suction filtration, and drying the obtained filter cake to obtain the acne removing active substance after pretreatment.

9. The preparation method of the acne-removing nano lipid carrier according to claim 7, wherein the carrier comprises the following components in percentage by weight: the heating temperature of the oil phase is 60-85 ℃.

10. The preparation method of the acne-removing nano lipid carrier according to claim 7, wherein the carrier comprises the following components in percentage by weight: the homogenizing rotation speed is 15000-25000 rpm.

Technical Field

The invention relates to the technical field of cosmetics, in particular to an acne-removing nano lipid carrier and a preparation method thereof.

Background

Acne, also known as acne, is a chronic inflammatory skin disease that manifests itself well in the hair follicles and sebaceous glands of the face, chest and back. Typical lesions are manifested as acne, hills , pus marks, nodules and cysts. The occurrence of whelk is closely related to the major factors such as hypersecretion of sebum, blockage of pilosebaceous ducts, bacterial infection and inflammatory reaction. In general, the level of androgen, particularly testosterone, in a human body rapidly rises after the human body enters adolescence, so that the development of sebaceous glands is promoted and a large amount of sebum is produced; meanwhile, the abnormal keratinization of the pilosebaceous canal causes the canal to be blocked, sebum discharge is obstructed, and a keratosis plug is formed; a plurality of microorganisms in hair follicles, particularly propionibacterium acnes, multiply in a large number, and lipase produced by propionibacterium acnes decomposes sebum to produce free fatty acids; at the same time, chemotaxis inflammatory cells and mediators, and finally induce and aggravate inflammatory reaction. Acne seriously affects the appearance and confidence of people and has negative influence on the work and life of people, so the acne removal is one of the research focuses of cosmetics.

The most effective mechanism for removing acne is: the keratotic plug was first loosened and then the anaerobe acnes was exposed to oxygen to make it unable to grow.

The common active substance for removing acne is salicylic acid with molecular formula of C₇H₆O₃Is a plant willow bark extract, and is a natural anti-inflammatory drug. Salicylic acid can remove cutin, sterilize and diminish inflammation, so the acne removing cream is very suitable for treating acne caused by pore blockage, and international mainstream acne removing products contain salicylic acid, and the concentration of the salicylic acid is usually 0.5-2%. However, salicylic acid is highly irritating to the skin and mucous membranes and reacts with proteins in body tissues, thus having a corrosive effect. And salicylic acid can only loosen keratotic plug and can not introduce oxygen, so the acne removing effect is general.

And the other common active substance for removing acne is BPO benzoyl peroxide which has a large amount of oxygen and can emit oxygen against acne bacillus by being directly applied. However, it is highly irritating and has a problem of being easily allergic.

The nano-structure lipid carrier (NLC) is a novel carrier developed on the basis of a solid nano-lipid particle (SLN), and can overcome the defects of limited drug loading capacity of the SLN, easy leakage in the drug storage process, overhigh water content in dispersion liquid when the SLN exists in a water dispersion form and the like. The NLC replaces solid grease with a mixture of solid grease and liquid grease on the basis of SLN, so that the NLC has a more irregular defect type structure, more space is generated to accommodate more active substances, the coating rate of the NLC is effectively improved, the active substances are slowly released, and the irritation is reduced.

Disclosure of Invention

The invention aims to solve the problems and provides an acne-removing nano lipid carrier and a preparation method thereof.

The technical scheme for solving the problems is to provide an acne-removing nano lipid carrier which comprises, by mass, 1-10 parts of acne-removing active substances, 1-10 parts of alkali, 5-30 parts of solid lipid, 5-20 parts of liquid lipid, 1-10 parts of a water-in-oil emulsifier and 1-10 parts of an oil-in-water emulsifier.

Preferably, the acne-removing active is salicylic acid; according to the mass parts, the chitosan-urea composite material also comprises 1-10 parts of chitosan, 0.1-2 parts of urea peroxide, 5-20 parts of acetic acid, 3-8 parts of glycerol and 15-20 parts of cyclodextrin.

Preferably, the solid lipid comprises one or more of stearyl alcohol, glyceryl tribehenate, cholesterol, glyceryl trimyristate, palmitoyl stearoyl glyceride, glyceryl tristearate, glyceryl monostearate, behenyl alcohol, lauric acid, glyceryl stearate citrate, hydrogenated castor oil, palmitic acid, palmitic alcohol, cetostearyl alcohol, fatty alcohols and fatty acids.

Preferably, the liquid lipid comprises one or more of caprylic/capric triglyceride, isopropyl palmitate, isopropyl myristate, liquid paraffin, isooctyl palmitate hexyl laurate, 2-octyl lauryl alcohol, oleic acid, linoleic acid, soybean oil and olive oil.

Preferably, the water-in-oil emulsifier comprises one or more of glycerate citrate, sucrose stearate, ABIL EM-90, P135, Span20, Span40, Span60, Span80, Brij 72, Brij 721 and A6.

Preferably, the oil-in-water emulsifier comprises one or more of sorbitan sesquioleate, SS, SSE-20, A25, NovelA, Tween20, Tween40, Tween60, Tween80 and K12.

The invention also aims to provide a preparation method of the acne-removing nano lipid carrier, which comprises the following steps:

(1) heating, liquefying and mixing solid lipid, liquid lipid and water-in-oil emulsifier to obtain oil phase; dissolving the acne removing active substance and alkali in deionized water to obtain an internal water phase; dissolving an oil-in-water type emulsifier in deionized water to obtain an external water phase;

(2) heating the inner water phase to the temperature of the oil phase, and adding the inner water phase into the oil phase under the homogeneous condition to obtain a coarse emulsion; reducing the temperature of the 5-10 DEG coarse emulsion, and adding the cooled coarse emulsion into an external water phase under a homogeneous condition to obtain an emulsion; and cooling the emulsion to normal temperature after magnetically stirring to obtain the acne-removing nano lipid carrier.

Preferably, the anti-acne active is also subjected to a pre-treatment comprising the following steps:

a. preparing acetic acid into an acetic acid solution with the volume fraction of 2%, and dissolving chitosan in the acetic acid solution to obtain a solution 1; a solution 2 obtained by dissolving urea peroxide in glycerol; dropwise adding the solution 2 into the solution 1 while stirring to obtain a solution 3;

b. dissolving salicylic acid and cyclodextrin in water to obtain a solution 4, slowly dripping the solution 3 into the solution 4, stirring for 5-8h, standing at 2-5 ℃ for 18-24h, then carrying out suction filtration, and drying the obtained filter cake to obtain the acne removing active substance after pretreatment.

Preferably, the oil phase is heated to a temperature of 60-85 ℃.

Preferably, when the inner water phase is added into the oil phase, the homogenizing rotation speed is 15000-25000rpm, and the homogenizing time is 30-60 s.

Preferably, when the crude emulsion is added into the external water phase, the homogenizing rotation speed is 15000-25000rpm, and the homogenizing time is 1-5 min.

Preferably, the magnetic stirring speed is 500-.

The invention has the beneficial effects that:

1. the nano-lipid carrier is loaded with the acne-removing active substance, the structure of the nano-lipid carrier is similar to that of multiple emulsion W/O/W, the nano-lipid carrier is a three-phase dispersion system, the acne-removing active substance can be well dispersed in multiple phase components, lipid and emulsifier materials with good biocompatibility are adopted, the acne-removing active substance is embedded in particles or adsorbed on the surfaces of the particles, the nano-lipid carrier prepared by coating water-soluble active substances has good superiority, the coating problem of the water-soluble active substance with poor stability and strong irritation can be well solved, and the acne-removing effect can be effectively exerted.

2. The preparation only needs grease, deionized water and an emulsifier, and can be finished only by heating and homogenizing, and the product has certain advantages in safety and operability.

3. Salicylic acid and urea peroxide are used as acne-removing active substances, the urea peroxide is wrapped by a chitosan film to obtain a wrapping body 1, the wrapping body 1 is wrapped by a salicylic acid wall material to obtain a wrapping body 2, and then the wrapping body 2 is loaded on a nano lipid carrier, so that the effect is gradual, namely the keratotic plug is opened by the salicylic acid, and then oxygen is released by the urea peroxide to achieve an excellent acne-removing effect under double effects. Meanwhile, the chitosan film layer between the salicylic acid and the urea peroxide has the adhesion and combination effects of the salicylic acid and the urea peroxide, and can modify the salicylic acid and coat the urea peroxide to reduce the irritation of the salicylic acid and the urea peroxide.

4. During the decomposition process of the urea peroxide, urea is generated, and the urea can prevent chapping and improve the hydration of the cuticle, thereby softening the skin and further reducing the problems of skin desquamation and redness caused by the irritation of the acne removing active substances.

Drawings

Fig. 1 is a particle size distribution diagram of an acne-removing nano-lipid carrier in example 1.

Fig. 2 is a particle size distribution diagram of an acne-removing nano-lipid carrier in example 2.

Detailed Description

The following are specific embodiments of the present invention and are further described with reference to the accompanying drawings, but the present invention is not limited to these embodiments.