Development and optimisation of atorvastatin calcium loaded self-nanoemulsifying drug delivery system (SNEDDS) for enhancing oral bioavailability: in vitro and in vivo evaluation

被引：34
作者：
Kassem, Abdulsalam M. [1 ]
Ibrahim, Hany M. [1 ]
Samy, Ahmed M. [1 ]
机构：
[1] Al Azhar Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo, Egypt
来源：
JOURNAL OF MICROENCAPSULATION | 2017年 / 34卷 / 03期
关键词：
Atorvastatin calcium; self-nanoemulsifying drug delivery system (SNEDDS); optimisation; fatty liver; bioavailability; BOX-BEHNKEN DESIGN; WATER MICROEMULSIONS; NONIONIC SURFACTANT; SAS PROCESS; FORMULATION; NANOPARTICLES; PHARMACOKINETICS; DISSOLUTION; ABSORPTION; ORIDONIN;
D O I：
10.1080/02652048.2017.1328464
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
The objective of this study was to develop and optimise self-nanoemulsifying drug delivery system (SNEDDS) of atorvastatin calcium (ATC) for improving dissolution rate and eventually oral bioavailability. Ternary phase diagrams were constructed on basis of solubility and emulsification studies. The composition of ATC-SNEDDS was optimised using the Box-Behnken optimisation design. Optimised ATC-SNEDDS was characterised for various physicochemical properties. Pharmacokinetic, pharmacodynamic and histological findings were performed in rats. Optimised ATC-SNEDDS resulted in droplets size of 5.66 nm, zeta potential of -19.52mV, t(90) of 5.43 min and completely released ATC within 30 min irrespective of pH of the medium. Area under the curve of optimised ATC-SNEDDS in rats was 2.34-folds higher than ATC suspension. Pharmacodynamic studies revealed significant reduction in serum lipids of rats with fatty liver. Photomicrographs showed improvement in hepatocytes structure. In this study, we confirmed that ATC-SNEDDS would be a promising approach for improving oral bioavailability of ATC.
引用
收藏
页码：319 / 333
页数：15
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