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Hair growth microneedle patch containing androgen receptor protein targeted complex as well as preparation method and application of hair growth microneedle patch

An androgen receptor and protein target technology, applied in the field of biomedical materials, can solve the problems of needle tip dermal tissue blockage, inability to accurately control drug dosage, lack of drug loading capacity, etc., to induce hair regeneration, accelerate the growth period, and safe effect

Active Publication Date: 2022-08-05
ZHEJIANG UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Common microneedles include solid microneedles, hollow microneedles, and soluble microneedles, etc. Among them, solid microneedles lack drug-loading capacity, and generally require pretreatment of the skin to form micropores before applying drugs. The operation is more cumbersome. And it is impossible to precisely control the amount of medicine that enters the skin
Hollow microneedles have small holes on the axis of the needle that are similar to traditional injection functions, similar to microinjection, but the preparation process is complicated, and the needle tip is easily blocked by dermal tissue, making it impossible to release the drug

Method used

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  • Hair growth microneedle patch containing androgen receptor protein targeted complex as well as preparation method and application of hair growth microneedle patch
  • Hair growth microneedle patch containing androgen receptor protein targeted complex as well as preparation method and application of hair growth microneedle patch
  • Hair growth microneedle patch containing androgen receptor protein targeted complex as well as preparation method and application of hair growth microneedle patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051]

[0052] The present embodiment provides a preparation method of a soluble hair growth microneedle patch, comprising:

[0053] 1. Preparation of androgen receptor protein targeting complex:

[0054] Compound 2 (2.0g, 1.0eq.) was dissolved in 20mL N,N-dimethylformamide, ice bath, sodium hydride (60%, 0.56g, 1.5eq.) was added, stirred for 0.5h, compound 1 ( 1.45g, 1.0eq.) was dissolved in 10mL N,N-dimethylformamide, dropped into the above reaction solution, reacted at room temperature until the reaction of the raw materials was complete, the reaction solution was concentrated, and purified by column chromatography (V 石油醚 / V 乙酸乙酯 =6 / 1) to obtain 3.1 g of white solid, yield 95%, UPLC-MS: m / z 351.15 [M+H] + ;

[0055] Compound 3 (1.0 g, 1.0 eq.) was dissolved in 12 mL of dichloromethane, 4 mL of trifluoroacetic acid was added, under argon protection, the reaction was performed at room temperature until the reaction of the raw materials was complete, the pH was adjusted...

Embodiment 2

[0069]

[0070] The present embodiment provides a preparation method of a soluble hair growth microneedle patch, comprising:

[0071] 1. Preparation of androgen receptor protein targeting complex:

[0072] Compound 2 (2.0g, 1.0eq.) was dissolved in 20mL N,N-dimethylformamide, ice bath, sodium hydride (60%, 0.56g, 1.5eq.) was added, stirred for 0.5h, compound 1 ( 1.45g, 1.0eq.) was dissolved in 10mL N,N-dimethylformamide, dropped into the above reaction solution, reacted at room temperature until the reaction of the raw materials was complete, the reaction solution was concentrated, and purified by column chromatography (V 石油醚 / V 乙酸乙酯 =6 / 1) to obtain 3.1 g of a white solid with a yield of 95%. UPLC-MS: m / z 351.15 [M+H] + ;

[0073] Compound 3 (1.0 g, 1.0 eq.) was dissolved in 12 mL of dichloromethane, 4 mL of trifluoroacetic acid was added, under argon protection, the reaction was performed at room temperature until the reaction of the raw materials was complete, the pH ...

Embodiment 3

[0084] This embodiment provides a method for preparing a soluble microneedle patch. The difference between this embodiment and Embodiment 1 is that step 1 in this embodiment is to synthesize the salt of the androgen receptor protein targeting complex.

[0085] In this embodiment, a solid-state soluble microneedle patch is finally obtained by mixing the androgen receptor protein targeting complex with the polymer solution. The solid-state soluble microneedle patch has a mild preparation process, does not require extreme conditions, is simple to prepare, and can be stored at room temperature in a dry environment, thereby effectively realizing the transdermal delivery of the androgen receptor protein targeting complex.

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Abstract

The invention discloses a hair growth micro-needle patch containing an androgen receptor protein targeted complex, which is characterized in that the hair growth micro-needle patch comprises a sheet-shaped backing and soluble micro-needle bodies which are arranged on the sheet-shaped backing and contain the androgen receptor protein targeted complex; the soluble microneedle body comprises one or more of an androgen receptor protein targeting complex, a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a geometric stereomer thereof, a tautomer thereof, an ester thereof, a prodrug thereof, a solvate thereof, a metabolite thereof, a nitrogen oxide thereof or a deuterated compound thereof. The invention also discloses a preparation method of the hair-growing micro-needle patch containing the androgen receptor protein targeted complex and application of the hair-growing micro-needle patch in preparation of a medicine for treating androgen-derived alopecia. The hair-growing micro-needle patch provided by the invention has the advantages of safe effect, high efficiency and convenience in use.

Description

technical field [0001] The invention belongs to the technical field of biomedical materials, and in particular relates to a hair growth microneedle patch containing an androgen receptor protein targeting complex and a preparation method and application thereof. Background technique [0002] Androgenetic alopecia (AGA) is the most common pathological type of hair loss in clinic. Both men and women can suffer from it. It is characterized by progressive miniaturization of hair follicles, which is manifested as a receding forehead hairline, or a gradual thinning and loss of hair on the top, and a progressive decrease in hair density, which eventually leads to hair loss and seriously affects the patient's mental health. Surveys show that the prevalence of males in my country is about 21.3%, and the prevalence of females is about 6.0%. In recent years, with the rapid development of society, the competition has become more and more fierce, and people's mental pressure has increase...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/496C07D401/14A61K47/66A61P5/28A61P17/14
CPCA61K9/0021A61K47/665C07D401/14A61K31/496A61P5/28A61P17/14Y02P20/55
Inventor 高建青秦冲王茹萱钟腾江
Owner ZHEJIANG UNIV
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