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A kind of preparation method of transdermal tyrosinase inhibitor

A tyrosinase and inhibitor technology, applied in the field of preparation of transdermal tyrosinase inhibitors, can solve the problems of limited use effect, lack of targeting, low skin penetration rate, etc., and achieve good skin permeability Effect

Active Publication Date: 2021-01-26
GUANGXI UNIVERSITY OF TECHNOLOGY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the two disadvantages of low skin penetration and lack of targeting severely limit the cosmetic and clinical use of the above-mentioned tyrosinase inhibitors.

Method used

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  • A kind of preparation method of transdermal tyrosinase inhibitor
  • A kind of preparation method of transdermal tyrosinase inhibitor
  • A kind of preparation method of transdermal tyrosinase inhibitor

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Embodiment Construction

[0025] The present invention will be further described in detail below in conjunction with the accompanying drawings and embodiments.

[0026] 1. Specific examples

[0027] 1. Aminated zinc oxide quantum dots (NH 2 Synthesis of @ZnO)

[0028] A. Using the gel-sol method to synthesize zinc oxide quantum dots in alkaline ethanol solution: dissolve 0.41g of zinc acetate in 10ml of absolute ethanol, stir and react at 68°C for 1.5 hours, and then cool in an ice bath to obtain Zinc acetate solution; after dissolving 0.16g of sodium hydroxide in 5 mL of absolute ethanol, add it dropwise in the zinc acetate solution, and continue stirring the mixed solution until the solution is green fluorescent when observed under an ultraviolet lamp with a wavelength of 365nm, and then Add 10mL of n-heptane, let stand and then centrifuge to get the precipitate to obtain zinc oxide quantum dots;

[0029] The synthesized product was analyzed by X-ray diffraction, which figure 1 The X-ray spectrum...

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Abstract

The invention discloses a preparation method of a transdermal tyrosinase inhibitor. The method is characterized by comprising the following steps: (1) synthesizing zinc oxide quantum dots in an alkaliethanol solution by utilizing a gel-sol method, and then carrying out amination to obtain aminated zinc oxide quantum dots; (2) connecting BQ-788 with the aminated zinc oxide quantum dots to form BQ-788 / NH2@ZnO; (3) dissolving ellagic acid and N,N'-carbonyldiimidazole in N,N'-dimethyl formamide, stirring for 2 hours at a room temperature and then adding into the N,N'-dimethyl formamide solution containing BQ-788 / NH2@ZnO, performing reaction for 7 hours at a room temperature under nitrogen protection, and cleaning for 3 times separately with anhydrous ethanol and deionized water so as to obtain the transdermal tyrosinase inhibitor BQ-788 / EA@ZnO. The transdermal tyrosinase inhibitor BQ-788 / EA@ZnO has the advantages of high transdermal rate and specially-targeted melanocytes.

Description

technical field [0001] The invention relates to a tyrosinase inhibitor, in particular to a preparation method of a transdermal tyrosinase inhibitor. Background technique [0002] Melanin is a natural pigment produced by melanocytes, which can absorb ultraviolet rays and prevent photodamage. However, the excessive deposition of melanin will affect the appearance of human skin, and more seriously, it will induce melanoma. The production process of melanin is divided into two steps. The first step: L-tyrosine is catalyzed by tyrosinase to generate L-dopa, and then dopa is catalyzed by tyrosinase to generate dopaquinone; the second step: dopa Quinones generate melanin via two non-enzymatic pathways. It can be seen that tyrosinase is the key rate-limiting enzyme for the formation of melanin. When tyrosinase is overexpressed, it will lead to a large amount of melanin deposition, leading to diseases related to pigment disorders. Therefore, the use of high-efficiency and low-tox...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/54A61K47/52A61K31/366A61P17/00A61K8/49A61K8/27A61Q19/02C01G9/02B82Y40/00B82Y30/00B82Y20/00
CPCA61K8/27A61K8/4926A61K8/498A61K31/366A61K2800/782A61K2800/805A61Q19/02B82Y20/00B82Y30/00B82Y40/00C01G9/02C01P2002/72C01P2002/82C01P2002/88C01P2004/04C01P2004/64
Inventor 黄啸易彩霞陈春肖祖丽龚星全郑曦石秀兰
Owner GUANGXI UNIVERSITY OF TECHNOLOGY
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