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Research Article

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

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Pages 319-333 | Received 13 Dec 2016, Accepted 05 May 2017, Published online: 23 May 2017
 

Abstract

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 −19.52 mV, t90 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.

Disclosure statement

The authors report no conflicts of interest.

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