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Multi-effect hydroxyl pinacolone retinoate nano composition as well as preparation method and application thereof

A nano-composition and multi-effect hydroxyl technology, which is applied in the direction of drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problem of inability to fully exert functional active substances, low solubility of glycyrrhetinic acid, and difficulty in functional active substances. and other issues, to achieve the effect of increasing skin penetration, improving bioavailability, strong adhesion and biocompatibility

Active Publication Date: 2021-06-15
WUHAN BEST CARRIER NANO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, hydroxypinacolone retinoate is sensitive to light and heat, and it is easy to oxidize and degrade after being directly added to skin care products for a period of time, and its stability is poor, which not only reduces the efficacy of skin care products but also causes skin irritation; the amide structure of nicotinamide is easily It is oxidized to produce niacin, which is irritating to the skin; the solubility of glycyrrhetinic acid is very small, the addition amount is low, and it is easy to crystallize and precipitate
Furthermore, due to the skin's own barrier function, it is difficult for functional active substances to penetrate the stratum corneum to reach the deep structure of the skin to play a role, the bioavailability is low, and the efficacy of functional active substances cannot be fully exerted

Method used

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  • Multi-effect hydroxyl pinacolone retinoate nano composition as well as preparation method and application thereof
  • Multi-effect hydroxyl pinacolone retinoate nano composition as well as preparation method and application thereof
  • Multi-effect hydroxyl pinacolone retinoate nano composition as well as preparation method and application thereof

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preparation example Construction

[0058] The present invention also provides a preparation method of the multi-effect hydroxy pinacolone retinoate nanocomposite described in the above technical scheme, comprising the following steps:

[0059] mixing hydroxypinacolone retinoate, glycyrrhetinic acid, liquid lipids, emulsifiers, co-emulsifiers and polyols to obtain an oil phase;

[0060] Mixing nicotinamide and water to obtain an aqueous phase;

[0061] The water phase and the oil phase are mixed and emulsified and subjected to micronization treatment to obtain a micron-scale dispersion;

[0062] The micron-scale dispersion is subjected to nano-processing to obtain a multi-effect hydroxy pinacolone retinoic acid ester nano composition.

[0063] In the preparation method provided by the invention, the oil phase and the water phase are respectively prepared, and the solubility of the active ingredient is improved. The micronization and nanometerization treatments are carried out sequentially, which promotes the f...

Embodiment 1

[0076] 0.1% Hydroxypinacolone Retinoate, 10% Glycyrrhetinic Acid, 7% Caprylic Capric Triglyceride, 7% Cocoa Seed Butter, 10% Polyglyceryl-10 Stearate, 7% Polyglyceryl-10 Diisostearate, 16% diethylene glycol monoethyl ether, and 6% sorbitol are mixed, heated and dissolved in a water bath at 35°C to obtain an oil phase;

[0077] Add 0.5% nicotinamide to 36.4% purified water, heat and dissolve in a water bath at 35°C to obtain a water phase;

[0078] Add the water phase dropwise to the oil phase at a speed of 5 drops / second and keep stirring at a rotation rate of 400r / min. After the mixing is completed, high-speed shear emulsification is carried out at a rotation rate of 5000rpm for 8min to obtain a micron-sized dispersion ;

[0079] The micron-scale dispersion was subjected to high-pressure homogenization treatment at 35° C. and a pressure of 500 bar, circulated 5 times, and cooled to room temperature to obtain a nanocomposite.

[0080] The particle size of the above-mentioned...

Embodiment 2

[0082] 10% hydroxypinacolone retinoate, 0.1% glycyrrhetinic acid, 10% isononyl isononanoate, 5% isopropyl myristate, 10% polyoxyethylene hydrogenated castor oil, 8% cetearyl Lithyl alcohol polyether, 6% PPG-26-butanol-26, 6% ethoxydiethylene glycol oleate, 7% glycerin are mixed, heated and dissolved in a water bath at 40°C to obtain an oil phase;

[0083] Add 1% nicotinamide to 36.9% purified water, heat and dissolve in a water bath at 40°C to obtain a water phase;

[0084] Add the water phase dropwise to the oil phase at a speed of 4 drops / second and keep stirring at a rotation rate of 700r / min. After the mixing is completed, high-speed shear emulsification is performed at a rotation rate of 7000rpm for 6min to obtain a micron-sized dispersion ;

[0085] The micron-scale dispersion was subjected to high-pressure homogenization treatment at 40° C. and a pressure of 800 bar, circulated 3 times, and cooled to room temperature to obtain a nanocomposite.

[0086] The particle si...

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Abstract

The invention relates to the field of cosmetics, in particular to a multi-effect hydroxyl pinacolone retinoate nano composition which comprises hydroxyl pinacolone retinoate, nicotinamide, glycyrrhizic acid, an emulsifying agent, a co-emulsifying agent and polyhydric alcohol. The hydroxyl pinacolone retinoate accounts for 0.1-10% of of the total mass of the nano composition; the nicotinamide accounts for 0.1-10% of the total mass of the nano composition; and the glycyrrhizic acid accounts for 0.1-10% of the total mass of the nano composition. According to the nano composition disclosed by the invention, the hydroxyl pinacolone retinoate, the nicotinamide and the glycyrrhizic acid are wrapped in the nano composition, so that the stability of functional components is effectively improved. The three functional components of the nano composition are reasonably matched and synergistically interacted, penetrate through a skin barrier and enter deep skin tissues, the bioavailability is improved, the anti-aging, acne-removing and whitening effects are improved, and the nano composition is mild and non-irritant to skin and can be widely applied to cosmetics.

Description

technical field [0001] The invention relates to the technical field of cosmetics, in particular to a multi-effect hydroxy pinacolone retinoic acid ester nanocomposite and its preparation method and application. Background technique [0002] Retinoids generally refer to compounds with the main basic structure of vitamin A and their oxidative metabolites, which have significant effects in anti-aging, acne removal, and whitening. Most often, retinoids are converted to retinoic acid to act on the skin. Among them, all-trans retinoic acid is a common active form of retinoic acid, which can increase the expression of aquaporin 3 (AQP3) in normal human skin, increase the permeability of cell membrane water, participate in water secretion, absorption and cell Adjustment of internal and external balance. However, overexpression of AQP3 can increase transepidermal water loss, causing skin dryness and sensitivity. [0003] Studies have shown that hydroxypinacolone retinoate is a new...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/67A61K8/63A61K8/891A61K8/92A61K8/37A61K8/31A61K8/39A61K8/60A61K8/55A61K8/86A61K8/34A61Q19/00A61Q19/02A61Q19/08A61P17/10
CPCA61K8/671A61K8/675A61K8/63A61K8/891A61K8/922A61K8/37A61K8/375A61K8/31A61K8/39A61K8/602A61K8/553A61K8/86A61K8/34A61K8/342A61K8/345A61Q19/00A61Q19/02A61Q19/08A61P17/10A61K2800/56A61K2800/782A61K2800/5922A61K2800/413A61K2800/412A61K2800/805
Inventor 刘卫吴航航罗佳沈慧慧陈家玲王曦吕赛龙
Owner WUHAN BEST CARRIER NANO TECH
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