Transdermal delivery nano-preparation, and preparation method and application thereof

A nano-formulation and drug delivery technology, applied in the field of medicine, can solve the problems of unfavorable pigmentation treatment, single drug action link, little effect, etc., and achieve the effect of inhibiting excessive melanin secretion and improving pigmentation treatment effect.

Inactive Publication Date: 2014-07-30
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Pigmentation affects the facial appearance of patients, which in turn affects their work and social interaction
With the improvement of living standards, people pay more and more attention to the treatment of freckles. Various freckle products and treatment techniques emerge in an endless stream. However, they often cost a lot but have little effect.
[0003] To sum up the current drug or cosmetic preparations for the treatment of pigmentation, there are mainly the following problems: ①The dosage forms are mainly traditional creams, which are difficult to penetrate through the stratum corneum
The stratum corneum barrier is the biggest obstacle for transdermal drug delivery, and it is also the bottleneck that restricts the development of new transdermal drug delivery systems; The toxicity of drugs produced by keratinocytes makes the regulation of keratinocytes to melanocytes disordered, which is not conducive to the treatment of pigmentation; ③The link of drug action is single
At present, the treatment drugs for pigmentation are mainly to inhibit the initial rate-limiting enzyme of melanin production—tyrosinase activity, but pigmentation is caused by the excessive production of melanin by melanocytes caused by changes in the microenvironment in the body. Therefore, the treatment of pigmentation is not enough to only target intracellular melanin production, but also pay attention to the regulation and treatment of the microenvironment of melanocytes

Method used

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  • Transdermal delivery nano-preparation, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of nanoparticles for transdermal administration of kojic acid dipalmitate double-modified by agoutin and oleic acid

[0028] 1. Preparation of Oleic Acid Chitosan Complex

[0029] Accurately weigh 0.8g chitosan, add 30ml pH4.7 dilute hydrochloric acid and stir to dissolve, add 1g 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC). Weigh oleic acid (OA) according to a certain feeding ratio, and dissolve it in 20ml of ethanol. The above two solutions were mixed, stirred magnetically at 400r / min, and reacted at room temperature for 48h until the reaction was complete. The final reaction solution was placed in a dialysis bag and dialyzed for 48 hours to remove the remaining EDC and water-soluble by-products. The dialysate was freeze-dried to obtain the oleic acid-chitosan complex.

[0030] 2. Preparation of kojic acid dipalmitate-loaded oleic acid-chitosan composite nanoparticles (OA-KD NPs)

[0031] Take 50 mg of oleic acid chitosan complex and d...

Embodiment 2

[0034] Example 2 In vivo drug efficacy evaluation of transdermal administration of kojic acid dipalmitate double-modified by agoutin and oleic acid

[0035] 1. Establishment of Pigmentation Mouse Model

[0036] Thirty-six healthy C57BL mice were randomly divided into 6 groups, 6 in each group. A proper amount of depilatory cream was applied to the back of the mice. After standing for 5 minutes, the depilatory cream was washed off, and an appropriate amount of depilatory liquid was applied. The UVB ultraviolet lamp (9W) was irradiated the next day. ), 30 minutes a day. On the 7th day of irradiation, the drug was administered at the irradiation site and one ear of the mice.

[0037] 2. In vivo anti-pigmentation efficacy evaluation

[0038] The five experimental groups were ① negative control group (modeling by irradiation but no administration); ② oleic acid chitosan nanoparticles loaded with kojic acid dipalmitate (OA-KD NPs); ③ agouti-loaded kojic acid oleic acid chitosan n...

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Abstract

The invention discloses a transdermal delivery nano-preparation, containing kojic dipalmitate, a polymer material, agouti protein and oleic acid, wherein the polymer material is formed into a nano-preparation carrier; the agouti protein and oleic acid are modified on the surface of the carrier; and the kojic dipalmitate is loaded in the carrier. The invention also discloses a preparation method and application of the transdermal delivery nano-preparation. The transdermal delivery nano-preparation disclosed by the invention is capable of effectively penetrating through the cuticle and also can be located at the melanocyte of the epidermis stratum basale; and besides, the transdermal delivery nano-preparation has good stain treatment effect and is suitable for treating hyperpigmentation diseases such as chloasma, freckle and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a transdermal nano-preparation loaded with kojic acid dipalmitate double-modified by agoutin and oleic acid, and a preparation method and application thereof. Background technique [0002] Pigmentation is the increase in the amount of melanin in the skin caused by the influence of ultraviolet rays, hormones in the body, inflammatory reactions and other factors on the human skin, so that the local color on the appearance of the skin becomes dark. Pigmentation affects the facial appearance of patients, which in turn affects their work and social interaction. With the improvement of living standards, people pay more and more attention to the treatment of freckles. Various freckle products and treatment techniques emerge in an endless stream, but often cost a lot but have little effect. [0003] To sum up the current pharmaceutical or cosmetic preparations for the treatment of pigm...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/19A61K38/00A61K47/48A61K47/36A61K8/64A61K8/73A61K8/49A61K8/02A61P17/00A61Q19/02A61K31/351
Inventor 高静钟延强高申储藏涂晔张玮黄景彬王晓宇张敏袁飞林亚玲孙治国刘俊杰
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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