Jiangxi University of Traditional Chinese Medicine, 1688 MEILING Avenue, Nanchang 330004, China.
Department of Pharmaceutics, 94th Hospital of People's Liberation Army, Nanchang, China.
Carbohydr Polym. 2018 Dec 15;202:64-71. doi: 10.1016/j.carbpol.2018.08.112. Epub 2018 Aug 28.
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.
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。