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基于透明质酸的纳米晶体水凝胶用于增强药物的局部递送:案例研究。

Hyaluronic acid based nanocrystals hydrogels for enhanced topical delivery of drug: A case study.

机构信息

Jiangxi University of Traditional Chinese Medicine, 1688 MEILING Avenue, Nanchang 330004, China.

Department of Pharmaceutics, 94th Hospital of People's Liberation Army, Nanchang, China.

出版信息

Carbohydr Polym. 2018 Dec 15;202:64-71. doi: 10.1016/j.carbpol.2018.08.112. Epub 2018 Aug 28.

Abstract

The objective of this study is to use a carbohydrate polymer hyaluronic acid (HLA) as matrix to design novel transdermal nanogel loading poorly soluble drug nanocrystals. Baicalin nanocrystals (BCA-NC) were prepared by coupling homogenization technology and spray-drying technology. The morphology, the rheological behavior and transdermal permeation studies of HLA based BCA-NC-gel were evaluated. The results demonstrated that the BCA-NC could be successfully prepared in terms of trehalose after spray-drying. The trehalose could prevent the aggregation of BCA-NC during spray-drying. It was discovered that, the BCA-NC-gel with 1% HLA possessed the favorable gelatin capacity and thinning shear rheological property. In vitro transdermal permeation studies of BCA-NC-gel/HLA studies indicated a marked increase in the skin permeation of BCA. And the transdermal flux of BCA-NC-gel with 1% HLA were 20.65-fold higher (p < 0.01) than that of coarse BCA-gel, which could be attributed to particles size reduction of BCA-NC and bioadhesive property of HLA. And the morphology characterization of BCA-NC-gel/HLA demonstrated that BCA-NC could be imprisoned into the gel network of HLA, which might prevent it from aggregation in gel. In conclusion, HLA based nanogel system is a promising carrier for effectively transdermal delivery of poorly soluble drug.

摘要

本研究旨在利用碳水化合物聚合物透明质酸(HLA)作为基质,设计新型载药透皮纳米凝胶。采用高压均质法和喷雾干燥法制备黄芩苷纳米晶体(BCA-NC)。评价了基于 HLA 的 BCA-NC-凝胶的形态、流变行为和透皮渗透研究。结果表明,喷雾干燥后可成功制备海藻糖载黄芩苷纳米晶体。海藻糖可防止喷雾干燥过程中 BCA-NC 的聚集。发现 1%HLA 的 BCA-NC-凝胶具有良好的凝胶能力和变薄剪切流变特性。BCA-NC-凝胶/HLA 的体外透皮渗透研究表明,BCA 的皮肤渗透明显增加。并且 1%HLA 的 BCA-NC-凝胶的透皮通量比粗 BCA-凝胶高 20.65 倍(p<0.01),这可能归因于 BCA-NC 的粒径减小和 HLA 的生物黏附特性。BCA-NC-凝胶/HLA 的形态学特征表明,BCA-NC 可以被囚禁在 HLA 的凝胶网络中,这可能防止其在凝胶中聚集。总之,基于 HLA 的纳米凝胶系统是一种有前途的载体,可有效透皮递送电镜下不易溶解的药物。

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