Factorial design studies of antiretroviral drug-loaded stealth liposomal injectable: PEGylation, lyophilization and pharmacokinetic studies
详细信息 查看全文
- 作者：Beeravelli Sudhakar ; Mylangam Chaitanya Krishna…
- 关键词：Stealth liposomes ; Opsonization ; Stearic stability ; PEG ; 10000 ; DSPE ; Statistical optimization and mean residence time
- 刊名：Applied Nanoscience
- 出版年：2016
- 出版时间：January 2016
- 年：2016
- 卷：6
- 期：1
- 页码：43-60
- 全文大小：3,111 KB
- 刊物类别：Chemistry and Materials Science
- 刊物主题：Materials Science
Nanotechnology - 出版者：Springer Berlin / Heidelberg
- ISSN：2190-5517
文摘
The aim of the present study was to formulate and evaluate the ritonavir-loaded stealth liposomes by using 32 factorial design and intended to delivered by parenteral delivery. Liposomes were prepared by ethanol injection method using 32 factorial designs and characterized for various physicochemical parameters such as drug content, size, zeta potential, entrapment efficiency and in vitro drug release. The optimization process was carried out using desirability and overlay plots. The selected formulation was subjected to PEGylation using 10 % PEG-10000 solution. Stealth liposomes were characterized for the above-mentioned parameters along with surface morphology, Fourier transform infrared spectrophotometer, differential scanning calorimeter, stability and in vivo pharmacokinetic studies in rats. Stealth liposomes showed better result compared to conventional liposomes due to effect of PEG-10000. The in vivo studies revealed that stealth liposomes showed better residence time compared to conventional liposomes and pure drug solution. The conventional liposomes and pure drug showed dose-dependent pharmacokinetics, whereas stealth liposomes showed long circulation half-life compared to conventional liposomes and pure ritonavir solution. The results of statistical analysis showed significance difference as the p value is (<0.05) by one-way ANOVA. The result of the present study revealed that stealth liposomes are promising tool in antiretroviral therapy.