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抗HIV纳米乳剂配方:优化及体内外评价

Anti HIV nanoemulsion formulation: optimization and in vitro-in vivo evaluation.

作者信息

Kotta Sabna, Khan Abdul Wadood, Ansari Shahid H, Sharma Rakesh Kumar, Ali Javed

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi 110062, India.

Department of Pharmacognosy & Phytochemistry, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi 110062, India.

出版信息

Int J Pharm. 2014 Feb 28;462(1-2):129-34. doi: 10.1016/j.ijpharm.2013.12.038. Epub 2013 Dec 25.

Abstract

The objective of the present work is to develop a dose adjustable nanotechnology based liquid formulation of efavirenz with improved bioavailability for HIV therapy. Nanoemulsion of efavirenz was developed using phase inversion composition method with the help of ternary phase diagram. Globule size of the o/w nanoemulsion was studied with the help of dynamic light scattering and further confirmed with TEM analysis. Optimized formulations were subjected for in vitro dissolution studies and in vivo studies were done in rats to calculate pharmacokinetics parameters and compared with efavirenz suspension. TEM results revealed that the globule size of optimized formulation was less than 30 nm. In vitro release profile showed more than 80% release within 6 h which was highly significant (p>0.05) and pharmacokinetic studies also proved a promising in vivo absorption profile when compared to the efavirenz suspension. The developed nanoemulsion proved to be an effective dose adjustable formulation of efavirenz for pediatric HIV therapy.

摘要

本研究的目的是开发一种基于纳米技术的依非韦伦液体剂型,其剂量可调节,生物利用度提高,用于HIV治疗。借助三元相图,采用相转变组成法制备了依非韦伦纳米乳剂。通过动态光散射研究了o/w纳米乳剂的液滴大小,并通过透射电子显微镜(TEM)分析进一步证实。对优化后的制剂进行体外溶出度研究,并在大鼠体内进行研究以计算药代动力学参数,并与依非韦伦混悬液进行比较。TEM结果显示,优化制剂的液滴大小小于30nm。体外释放曲线显示,6小时内释放超过80%,具有高度显著性(p>0.05),药代动力学研究也证明,与依非韦伦混悬液相比,其体内吸收情况良好。所开发的纳米乳剂被证明是一种用于儿童HIV治疗的有效的、剂量可调节的依非韦伦制剂。

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