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基于醋酸纤维素的固体分散体基质纳米颗粒中难溶性抗病毒药物的溶出度增强

Enhanced dissolution of poorly soluble antiviral drugs from nanoparticles of cellulose acetate based solid dispersion matrices.

作者信息

Mazumder Sonal, Dewangan Ashish Kumar, Pavurala Naresh

机构信息

Department of Chemical Engineering, Birla Institute of Science and Technology, Pilani, Rajasthan 333031, India.

Oak Ridge Associated Universities, Food and Drug Administration, Silver Spring, MD, USA.

出版信息

Asian J Pharm Sci. 2017 Nov;12(6):532-541. doi: 10.1016/j.ajps.2017.07.002. Epub 2017 Jul 8.

Abstract

Polysaccharide-based polymers were used to produce nanoparticles of poorly soluble antiviral drugs using a rapid precipitation process. The structure-property relationships of four novel cellulose acetate-based polymers were studied for their solubility enhancement of poorly soluble drugs. Particles were purified by dialysis, and dried powders were recovered after freeze-drying. The particle diameters were 150-200 nm. The target drug loading in the particles was 25 wt%, and the drug loading efficiencies were 80-96%. The effects of the formulation process and nanoparticle properties on drug solubility were investigated. All nanoparticles afforded increased solubility and faster release compared to pure drugs. Drug release was a function of the relative hydrophobicity (or solubility parameters) of the polymers.

摘要

基于多糖的聚合物被用于通过快速沉淀法制备难溶性抗病毒药物的纳米颗粒。研究了四种新型醋酸纤维素基聚合物的结构-性能关系,以提高难溶性药物的溶解度。颗粒通过透析纯化,并在冷冻干燥后回收干粉。粒径为150-200nm。颗粒中的目标载药量为25wt%,载药效率为80-96%。研究了制剂工艺和纳米颗粒性质对药物溶解度的影响。与纯药物相比,所有纳米颗粒都提高了溶解度并实现了更快的释放。药物释放是聚合物相对疏水性(或溶解度参数)的函数。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/708e/7032198/7d47993de08c/ajps449-ga-5001.jpg

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