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Transfersome-exosome membrane fusion preparation with transdermal enhancement effect as well as preparation method and application thereof

A technology of enhancement and exosomes, which is applied in the field of biomedicine, can solve problems such as difficulty in ensuring the stability and effectiveness of multiple whitening ingredients, poor drug loading effects, and insufficient carrier advantages, etc., to achieve good development and application prospects, Improve the effect of poor self-stability and excellent transdermal effect

Pending Publication Date: 2021-10-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Decreased synthesis and increased loss of collagen in fibroblasts in the dermis will lead to aging phenomena such as sagging and fine lines in the skin. Increased melanin synthesis by melanocytes in the basal layer will cause problems such as dark yellow and spots. However, most skin care products on the market contain ingredients It is single and mainly composed of chemical components. Due to the limitation of the stratum corneum of the skin, it only stays on the surface of the skin, and it is difficult to penetrate into the deep layer of the skin to play a role on specific cells, causing waste and affecting the actual use effect of the user.
[0003] As far as skin care products are concerned, if the active ingredients exist alone, they are easily affected by pH, oxidation, and interaction with other ingredients, resulting in reduced self-efficacy
CN202010292807.2 provides an essence with whitening and freckle-removing functions, which contains a variety of whitening compositions combining Chinese and Western: Mimeng flower extract (0.1-10%), sealwort extract (0.1-10%), magnolia extract extract (0.1-10%), Moutan bark extract (0.1-10%), phloretin (0.05-2%), 4-n-butylresorcinol (0.01-0.3%), vitamin C or its Derivatives (0.05-2%), niacinamide (0.05-2%), vitamin E (0.03-1%), etc., in addition to containing 5-20% moisturizers, 1-5% skin conditioning agents, 0.1-5 % solubilizer, 0.1-1% thickener, 0.02-2% preservative, but the carrier advantage is not obvious enough, it is difficult to guarantee the stability and effectiveness of multiple whitening ingredients
CN104083318A provides a whitening skin care product and its preparation method, wherein the whitening ingredients only account for 0.5-1.5%, and there are problems such as limited penetration effect, and there is still a lot of room for improvement in the whitening effect
[0004] Emerging medical aesthetic methods such as micro-needle, water light needle and other physical methods can deliver active ingredients to the deeper skin to a certain extent, but they will cause skin damage such as bleeding and irritation. After use, the repair cycle is long and there are many precautions, so it is not suitable for long-term , Repeated use, causing a lot of inconvenience to beauty lovers
Umbilical cord-derived mesenchymal stem cell exosomes can restore the activity of skin fibroblasts and promote collagen regeneration through various cytokines. field application

Method used

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  • Transfersome-exosome membrane fusion preparation with transdermal enhancement effect as well as preparation method and application thereof
  • Transfersome-exosome membrane fusion preparation with transdermal enhancement effect as well as preparation method and application thereof
  • Transfersome-exosome membrane fusion preparation with transdermal enhancement effect as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Preparation of a transfersome-exosome membrane fusion preparation with enhanced transdermal effect:

[0045] (1) Extraction, separation and purification of exosomes from mesenchymal stem cells:

[0046] in DMEM containing 10% fetal bovine serum at 37°C in 5% CO 2 Human umbilical cord-derived mesenchymal stem cells were cultured to the 4th passage under the conditions, and the cells adhered to the wall and grew to 90% of the culture dish (about 1×10 7 1), replace with serum-free DMEM medium and continue to culture at 37°C for 24h, collect the medium, use an ultra-high-speed centrifuge at 4°C, 2000g for 10min to remove cell debris, take the supernatant through a 0.22μm filter membrane, and centrifuge at 100000g After 70 minutes, exosomes were obtained and stored at -80°C for later use;

[0047] (2) Preparation of small molecule peptide transfer body:

[0048] Weigh oligopeptide-1 (5mg), dissolve it with 5mL PBS (pH7.4), and use it as a hydration solution for later use....

Embodiment 2

[0056] Preparation of a transfersome-exosome membrane fusion preparation with enhanced transdermal effect:

[0057] (1) Extraction, separation and purification of exosomes from mesenchymal stem cells, as in Example 1;

[0058] (2) Preparation of small molecule peptide transfer body:

[0059] Weigh tripeptide-1 (4mg), dissolve it with 5mL PBS, and set aside. Weigh EPC (44 mg), cholesterol (6 mg), Tween 80 (8 mg) in a 100 mL eggplant-shaped bottle, add 5 mL of absolute ethanol to dissolve it ultrasonically, form a film under reduced pressure at 25 ° C to remove the organic solvent, dry it in vacuum overnight, add three Peptide-1 in PBS solution 5mL, rotate and hydrate at 25°C and 120rpm for 20min to obtain a transfersome suspension, use a dialysis bag (mW=30kD) to dialyze overnight to remove unencapsulated free peptide in the transfersome suspension , to obtain the transfersome solution, which was stored at 4°C for future use;

[0060] (3) Preparation of transfersome-exosome ...

Embodiment 3

[0066] Preparation of a transfersome-exosome membrane fusion preparation with enhanced transdermal effect:

[0067] (1) Extraction, separation and purification of exosomes from mesenchymal stem cells, as in Example 1;

[0068] (2) Preparation of small molecule peptide transfer body:

[0069] Weigh tripeptide-1 (5mg), dissolve it with 5mL PBS, and set aside. Weigh SPC (87.50mg), cholesterol (12.50mg), Tween 80 (8mg), sodium deoxycholate (7mg) in a 100mL eggplant-shaped bottle, add 5mL absolute ethanol to dissolve it ultrasonically, and remove it under reduced pressure at 25°C to form a film Organic solvent, vacuum-dry overnight, add 5 mL of PBS solution containing tripeptide-1, rotate and hydrate at 25°C, 120 rpm for 20 min to obtain a transfersome suspension, and use a dialysis bag (mW=30kD) to dialyze overnight to remove the transfersome mixture. The unencapsulated free peptide in the suspension was obtained as a transfersome solution, which was stored at 4°C for later use;...

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Abstract

The invention discloses a transfersome-exosome membrane fusion preparation with a transdermal enhancement effect as well as a preparation method and the application thereof. The preparation method of the preparation comprises the following steps: extracting and separating mesenchymal stem cell exosome; preparing a small molecule peptide-loaded carrier; constructing a transdermal peptide modified transfersome-exosome membrane fusion carrier loaded with small molecule peptide; preparing plant essential oil gel; and obtaining a transfersome-exosome membrane fusion preparation with the transdermal enhancement effect. The prepared transfersome-exosome membrane fusion preparation can remarkably improve the drug loading capacity of small molecule peptide, has higher deformability and more excellent transdermal effect compared with traditional lipidosome, and has synergistic effect with plant essential oil with transdermal effect to better promote penetration of functional beautifying components into the deep skin. Multiple beautifying effects of tightening skin, recovering skin vitality and the like are expected to be achieved through simple smearing, and the cosmetic is convenient to use, safe, free of pain and non-irritant to skin and has huge application market and development prospects in the medical market.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a transfer body-exosome membrane fusion preparation with enhanced transdermal effect, a preparation method and application thereof. Background technique [0002] The skin is the largest organ of the human body, and the stratum corneum is responsible for resisting external aggression, and thus blocks the absorption of many skin care ingredients. Decreased synthesis and increased loss of collagen in fibroblasts in the dermis will lead to aging phenomena such as sagging and fine lines in the skin. Increased melanin synthesis by melanocytes in the basal layer will cause problems such as dark yellow and spots. However, most skin care products on the market contain ingredients It is single and mainly composed of chemical components. Due to the limitation of the stratum corneum of the skin, it only stays on the surface of the skin, and it is difficult to penetrate into the deep la...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K38/18A61K38/08A61K38/06A61K36/61A61K47/64A61K47/46A61K47/44A61K8/14A61K8/55A61K8/63A61K8/64A61K8/92A61K8/99A61P17/00A61P17/16A61P17/18A61P29/00A61P31/04A61Q19/02B82Y5/00B82Y40/00
CPCA61K8/99A61K8/64A61K8/553A61K8/63A61K8/922A61K8/14A61Q19/02A61K47/6911A61K47/46A61K9/0014A61K47/64A61K47/44A61K36/61A61K38/06A61K38/08A61K38/1808A61P17/16A61P17/00A61P29/00A61P31/04A61P17/18B82Y5/00B82Y40/00A61K2800/5922A61K2300/00Y02A50/30
Inventor 李斯文尚美彤李钰
Owner CHINA PHARM UNIV
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