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用于从灵芝中分离出的三萜类化合物经皮给药以治疗冻伤的纳米凝胶。

Nanogel for dermal application of the triterpenoids isolated from Ganoderma lucidum (GLT) for frostbite treatment.

作者信息

Shen Cheng-ying, Xu Ping-hua, Shen Bao-de, Min Hong-yan, Li Xiao-rong, Han Jin, Yuan Hai-long

机构信息

a Department of Pharmacy , 302 Military Hospital , Beijing , China.

出版信息

Drug Deliv. 2016;23(2):610-8. doi: 10.3109/10717544.2014.929756. Epub 2014 Jun 25.

DOI:10.3109/10717544.2014.929756
PMID:24963753
Abstract

OBJECTIVE

The purpose of this study was to formulate stable Ganoderma lucidum (GLT) nanogels suitable for topical delivery with a view to improve the therapeutic effect for frostbite.

METHODS

GLT nanosuspensions were formulated using the high-pressure homogenization technique and then suitably gelled for characterized. In order to confirm the advantages of GLT nanogel for dermal application, skin permeation studies in vitro and pharmacodynamic evaluation in vivo were studied and compared with GLT-carbopol gel.

RESULTS

The particle size analysis and SEM studies revealed that GLT nanosuspensions were still stably kept their particle size after suitably gelled by carbopol preparation. The drug content, pH, and spreadability of the GLT nanogel was found to be 99.23 ± 1.8%, 6.07 ± 0.1, and 26.42 (g·cm)/s, which were within acceptable limits. In vitro permeation studies through rat skin indicated that the amount of GLT permeated through skin of GLT nanogel after 24 h was higher than GLT-carbopol gel, and GLT nanogel increased the accumulative amount of GLT in epidermis five times than GLT-carbopol gel. No oedema and erythema were observed after administration of GLT nanogel on the rabbits' skin. Pharmacodynamic study showed that GLT nanogel was more effective than GLT-carbopol gel in treatment of frostbite.

CONCLUSION

The GLT nanogel possess superior therapeutic effect for frostbite compared with the GLT-carbopol gel, which indicates that nanogels are eligible for the use as a suitable nanomedicine for dermal delivery of poorly soluble drugs such as GLT.

摘要

目的

本研究旨在制备适用于局部给药的稳定灵芝纳米凝胶(GLT),以提高冻伤的治疗效果。

方法

采用高压均质技术制备GLT纳米混悬液,然后进行适当凝胶化并表征。为了证实GLT纳米凝胶在皮肤应用方面的优势,进行了体外皮肤渗透研究和体内药效学评价,并与GLT-卡波姆凝胶进行比较。

结果

粒径分析和扫描电镜研究表明,GLT纳米混悬液经卡波姆制剂适当凝胶化后,粒径仍保持稳定。GLT纳米凝胶的药物含量、pH值和铺展性分别为99.23±1.8%、6.07±0.1和26.42(g·cm)/s,均在可接受范围内。大鼠皮肤体外渗透研究表明,GLT纳米凝胶给药24小时后透过皮肤的GLT量高于GLT-卡波姆凝胶,且GLT纳米凝胶使表皮中GLT的累积量比GLT-卡波姆凝胶增加了五倍。在兔皮肤给药GLT纳米凝胶后未观察到水肿和红斑。药效学研究表明,GLT纳米凝胶在治疗冻伤方面比GLT-卡波姆凝胶更有效。

结论

与GLT-卡波姆凝胶相比,GLT纳米凝胶对冻伤具有更好的治疗效果,这表明纳米凝胶有资格用作适用于皮肤递送难溶性药物(如GLT)的纳米药物。

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