Nano lipid carrier microneedle for treating alopecia and application of nano lipid carrier microneedle

A nano-lipid carrier and micro-needle technology, which is applied in the medical field, can solve the problems of lack of hair loss drugs, etc., and achieve the effects of increasing skin penetration and retention, improving targeting, and increasing targeting effects

Active Publication Date: 2020-06-26
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, male patients with alopecia treated with oral finasteride have adverse reactions such as loss of libido and impotence.
[0005] Therefore, there is still a lack of drugs that can effectively treat alopecia clinically.

Method used

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  • Nano lipid carrier microneedle for treating alopecia and application of nano lipid carrier microneedle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 Preparation of finasteride nano-lipid carrier

[0017] This embodiment includes the following raw materials by mass percentage:

[0018] Finasteride 10 mg

[0019] Glyceryl monostearate 810 mg

[0020] Squalene 90 mg

[0021] Poloxamer 188 200 mg

[0022] water 10ml

[0023] The preparation method of this embodiment:

[0024] A. According to the prescription ratio, at 78°C, glyceryl monostearate and squalene were dissolved by magnetic stirring to form a transparent and clear solution; the prescribed amount of finasteride was added to the above solution to dissolve;

[0025] B. According to the prescription ratio, add Poloxamer 188 to 78°C water to dissolve;

[0026] C. At 78°C, add solution A dropwise to the solution described in step B, and keep stirring until a uniform and stable white suspension is formed.

Embodiment 2

[0028] (1) Preparation of finasteride nano-lipid carrier microneedles

[0029] This embodiment includes the following raw materials by mass percentage:

[0030] Tip matrix:

[0031] Finasteride Nano Lipid Carrier Lyophilized Powder 16%

[0032] Sodium hyaluronate (molecular weight 34 KD) 40%

[0033] the rest is water

[0034] Base matrix:

[0035] Dextran 40 10%

[0036] Sodium hyaluronate (molecular weight 34 KD) 10%

[0037] Sodium hyaluronate (molecular weight 200 KD~ 400 KD) 10%

[0038] the rest is water

[0039] The preparation method of this embodiment:

[0040] A, take the finasteride nano-lipid carrier in Example 1 and freeze-dry to obtain a white powder;

[0041] B. According to the prescription ratio, take 4 g of sodium hyaluronate (molecular weight 34 KD) and disperse it in 10 mL of water, stir until it is fully dissolved, add the lyophilized powder of finasteride nano-lipid carrier in the prescription ratio, and stir until it is evenly mixed , inject th...

Embodiment 3

[0079] Example 3. In vitro transdermal experiment of finasteride nano-lipid carrier microneedle

[0080] After the microneedles were prepared according to Examples 1 and 2, the transdermal effect of the microneedles was investigated.

[0081] Transdermal test method: SD rats were anesthetized with 1 mL of 20% urethane, sacrificed by cervical dislocation, shaved off the abdominal hair, and depilated with depilatory cream. Rinse well with saline and store in -20 °C freezer. Before use, thaw with normal saline, and blot the surface moisture with filter paper. The abdominal skin of the rat was fixed between the donor and receiver cisterns. The process of the transdermal experiment was consistent with the above-mentioned isolated pig skin transdermal experiment.

[0082] After 24 hours of the transdermal experiment, the rat skin was removed from the diffusion cell, the surface was washed with water, the residual drug was removed with methanol, the skin was cut into pieces, 1 mL ...

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PUM

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Abstract

The invention provides a nano lipid carrier microneedle for treating alopecia. The nano lipid carrier microneedle comprises: a) a needle tip portion, and b) a base portion, wherein the needle tip portion comprises a finasteride nano lipid carrier and a needle tip matrix; and the base portion comprises a base matrix. The invention further provides application of the nano lipid carrier microneedle in preparation of a drug for treating androgen-derived alopecia. The nano lipid carrier microneedle can improve the retention amount of finasteride in hair follicles and a hair follicle targeting effect, and promotes hair follicle development and hair growth by inhibiting 5 alpha-reductase and / or stimulating hair follicle stem cells.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a nano-lipid carrier microneedle for promoting the treatment of hair loss and an application thereof. Background technique [0002] The pathogenesis of androgenetic alopecia is not yet clear, and it is mostly related to excessive secretion of androgen, which often manifests as excessive scalp fat overflow. The course of androgenetic alopecia lasts for several years, which affects the patient's quality of life and physical and mental health. Hair growth is closely related to hormones, and different parts of the hair have different sensitivity to androgen. In patients with alopecia, there is often more androgen receptor expression in scalp hair follicles, enhancing the sensitivity of dermal papilla cells to androgens. After the androgen testosterone in the body acts on the androgen receptor in the hair follicle, it forms a more active dihydrotestosterone under the action of 5α-red...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/58A61K47/06A61K47/14A61K47/36A61P17/14
CPCA61K9/0021A61K31/58A61K47/06A61K47/14A61K47/36A61P17/14
Inventor 徐月红曹思思王艺璇
Owner SUN YAT SEN UNIV
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