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CN-122005352-A - High-stability retinol composite nano-liposome and preparation method thereof

CN122005352ACN 122005352 ACN122005352 ACN 122005352ACN-122005352-A

Abstract

The invention discloses a high-stability retinol composite nano liposome and a preparation method thereof, wherein the high-stability retinol composite nano liposome comprises glycerol, water, 2, 3-butanediol, caprylic/capric triglyceride, 1, 2-hexanediol, retinol, hydroxy pinacol retinoic acid ester and synergistically modified lipid, wherein the synergistically modified lipid consists of sodium stearoyl glutamate, polysorbate-20 and polyglycerol-4 oleate, and retinol and hydroxy pinacol retinoic acid ester are taken as retinoid active substances to be jointly wrapped in a nano liposome structure formed by self-assembly of the synergistically modified lipid. The preparation method comprises the steps of water phase preparation, oil phase preparation, mutual mixing, addition of synergistically modified lipid and dispersion treatment. The invention realizes the stable encapsulation of the dual retinoid active substances by the synergic modified liposome system, can effectively improve the stability and the utilization rate of the retinoid active substances, and reduces the irritation while ensuring the efficacy.

Inventors

  • MU CHUN
  • Gao Yudai
  • LU YINUAN
  • MING SI

Assignees

  • 有生之颜(深圳)生物科技有限公司

Dates

Publication Date
20260512
Application Date
20260209

Claims (10)

  1. 1. The high-stability retinol composite nanoliposome is characterized by comprising, by weight, 35-45 parts of glycerin, 25-40 parts of water, 5-15 parts of 2, 3-butanediol, 5-15 parts of caprylic/capric triglyceride, 1-4 parts of 1, 2-hexanediol, 0.5-2.0 parts of retinol, 0.5-2.0 parts of hydroxy pinacolone retinol ester and 2.7-9.0 parts of synergistically modified lipid, wherein the synergistically modified lipid is composed of sodium stearoyl glutamate, polysorbate-20 and polyglycerol-4 oleate, and the retinol and hydroxy pinacolone retinol are taken as retinoid active substances and are jointly wrapped in a nanoscale liposome structure formed by the synergistically modified lipid in a self-assembly manner.
  2. 2. The high-stability retinol composite nanoliposome according to claim 1 is characterized by comprising, by weight, 0.2-1.0 parts of sodium stearoyl glutamate, 200.5-2.0 parts of polysorbate, and 2.0-6.0 parts of polyglycerol-4 oleate.
  3. 3. The high-stability retinol composite nanoliposome according to claim 1 or 2, wherein the preparation method of the synergistically modified lipid comprises the following steps: (1) Weighing sodium stearyl glutamate, polysorbate-20 and polyglycerol-4 oleate; (2) Sequentially adding sodium stearyl glutamate, polysorbate-20 and polyglycerol-4 oleate into a solvent, and mixing under stirring to obtain a uniform lipid mixed system; (3) And performing dispersion treatment on the obtained lipid mixed system to obtain the synergistically modified lipid.
  4. 4. The high-stability retinol composite nanoliposome according to claim 3, wherein the reaction condition in the step (2) is that sodium stearyl glutamate, polysorbate-20 and polyglycerol-4 oleate are added into a solvent, and are mixed by adopting a mechanical stirring mode under the condition of 20-40 ℃, wherein the stirring speed is 300-1000 r/min, and the stirring time is 10-60 min.
  5. 5. The high-stability retinol composite nanoliposome according to claim 3, wherein the reaction condition of the step (3) is that the obtained lipid mixed system is treated by a high-shear dispersion mode, the dispersion temperature is 20-40 ℃, the dispersion rotating speed is 8000-20000 r/min, and the dispersion time is 5-30 min.
  6. 6. A preparation method of a high-stability retinol composite nanoliposome, which is characterized by comprising the following steps: s1, weighing glycerol, water, 2, 3-butanediol and 1, 2-hexanediol, and mixing under stirring to obtain a water phase system; s2, weighing caprylic/capric triglyceride, retinol and hydroxy pinacolone retinol, and mixing to obtain an oil phase system; S3, adding the oil phase system into the water phase system under the stirring condition, and mixing to obtain an initial mixed system; s4, adding the synergistically modified lipid into the initial mixed system, and continuing mixing to obtain a liposome precursor system; s5, performing dispersion treatment on the liposome precursor system to obtain the high-stability retinol composite nano-liposome.
  7. 7. The preparation method of the high-stability retinol composite nanoliposome according to claim 6, wherein the reaction condition of the step S1 is stirring and mixing at 20-40 ℃, the stirring time is 10-60 min, the stirring mode is mechanical stirring, the reaction condition of the step S2 is mixing at 20-40 ℃ and the mixing time is 5-30 min under the condition of light shielding.
  8. 8. The preparation method of the high-stability retinol composite nanoliposome according to claim 6, wherein the reaction condition in the step S3 is that an oil phase system is slowly added into a water phase system at 20-40 ℃ and mixed under stirring for 10-60 min.
  9. 9. The method for preparing the high-stability retinol composite nanoliposome according to claim 6, wherein the reaction condition in the step S4 is that the synergistically modified lipid is added into the initial mixed system at 20-40 ℃ and stirring is continued for 10-60 min.
  10. 10. The method for preparing the high-stability retinol composite nanoliposome according to claim 6, wherein the reaction condition in the step S5 is that a liposome precursor system is treated by adopting a high-shear dispersion mode, the dispersion temperature is 20-40 ℃, the dispersion rotating speed is 8000-20000 r/min, and the dispersion time is 5-30 min.

Description

High-stability retinol composite nano-liposome and preparation method thereof Technical Field The invention belongs to the technical field of cosmetic raw materials and active substance delivery, and particularly relates to a high-stability retinol composite nano liposome and a preparation method thereof. Background Aging is an inevitable process in the biological life cycle, and under the combined action of genetic factors and external environmental factors, the structures and functions of human tissues and organs gradually change in a degenerative manner. The skin is used as the largest organ of human body, has obvious aging performance, and is mainly characterized in the aspects of collagen content reduction, elasticity weakening, fine lines, wrinkle generation and the like. Therefore, it has been an important research direction in the cosmetic field to delay skin aging and improve skin condition. Retinol is used as vitamin A and its derivatives, and is widely used in anti-aging cosmetics because it can promote collagen synthesis, induce elastin and elastic collagen fiber generation. The retinol components commonly used in the prior art include retinol, retinaldehyde, retinoic acid esters, etc. However, retinol and its derivatives generally have a problem of poor stability, are highly sensitive to external factors such as light, oxygen, temperature and metal ions, and are easily degraded during storage and use, resulting in a decrease in the content of active ingredients. Meanwhile, the retinol has a narrow pH application range and certain phototoxicity, and is easy to generate oxidation reaction and free radical under the action of ultraviolet rays, so that the stability of the product is influenced, skin aging is possibly accelerated, and skin red swelling, itching, tightness and other stimulus reactions are possibly caused, so that the application of the retinol in cosmetics is limited to a certain extent. Various retinol derivatives have also been developed in the prior art in order to reduce irritation and improve the use experience. The hydroxy pinacolone retinoic acid ester is used as a novel retinoid component, the structure of the hydroxy pinacolone retinoic acid ester is composed of retinoic acid and pinacol, a traditional conversion path of ester-alcohol-aldehyde is jumped, the hydroxy pinacolone retinoic acid ester can be more rapidly converted into retinoic acid and is directly combined with an intracellular retinoic acid receptor, and the hydroxy pinacolone retinoic acid ester has the anti-aging effect of retinol and simultaneously has the characteristic of relatively mild. However, the compatibility of the components in the formula system is still limited, precipitation can still occur under bad storage or use environments, and the stability is still required to be further improved. To improve the stability and safety of retinol-like materials, liposome encapsulation is commonly used in the art for delivery. The liposome is used as a common active substance carrier, can isolate the influence of the external environment on active ingredients to a certain extent, and is helpful for improving skin permeability. However, at present, a liquid liposome system is generally adopted in the cosmetic field, and the system is still easy to cause the problems of liposome particle aggregation, active ingredient leakage and the like in the practical application process, so that the liposome structure is unstable, the encapsulation rate is reduced, and the utilization efficiency of retinol active ingredients and the overall performance of products are affected. Most products in the prior art only wrap single retinol ingredients, the action target point is relatively single, the requirements of quick acting and continuous slow release are difficult to be simultaneously considered, and the irritation risk still exists while the efficacy is ensured. Therefore, how to achieve synergistic delivery of multiple retinoid components while improving stability of retinoid actives and further improve structural stability and safety in use of liposome systems remains a technical problem to be solved in the art. Disclosure of Invention In order to overcome the problems that in the background technology, retinol active substances are poor in stability and easy to be degraded due to the influence of light, oxygen, temperature and the like, active ingredients are easy to leak, particles are gathered, the irritation is high, and the quick acting and sustained release are difficult to be compatible, the invention aims to provide a high-stability retinol composite nano-liposome and a preparation method thereof, wherein the high-stability retinol composite nano-liposome comprises glycerin, water, 2, 3-butanediol, caprylic/capric triglyceride, 1, 2-hexanediol, retinol, hydroxy pinacolone retinoate and synergistically modified lipid, the synergistic modified lipid is composed of sodium stearyl glutamate, polysorbate-20 and poly