Self-Nanoemulsifying Drug Delivery System for Atorvastatin Calcium: Design, Optimization and Evaluation

Abstract

Atorvastatin calcium (ATC) is the choice of drug in the treatment of moderate to severe hypercholesterolemia. In the current study, ATC self-nanoemulsifying drug delivery systems (SNEDDS) were prepared in an attempt to improve the bioavailability by enhancing its solubility. The solubility of ATC in various oils, surfactants, and co-surfactants were determined. Based on their solubility, Capmul MCM (oil), Tween 20 (surfactant), propylene glycol (Co-surfactant) was selected for preparation of SNEDDS. Self-nanoemulsification region were determined by pseudo-ternary phase diagrams. The compatibility of drug with excipients were determined by FTIR spectroscopy and Optimized SNEDDS were evaluated for thermodynamic stability, dispersibility, robustness to dilution, particle size measurements, refractive index, percent transmittance, drug content, In vitro drug release etc. The SNEDDS were successfully formulated with the selected excipients. FTIR studies confirm there is no significant interaction between drug and excipients. The metastable formulations were ruled out by thermodynamic tests and robust to dilution test. The optimized ATC SNEDDS yielded nano-emulsion of mean globule size 42.21 nm. In vitro release studies shows that all the SNEDDS released more than 90% of drug at the end of 30 min, whereas the pure drug shows only the release of 29.54% at 30 min. The optimized formulation was subjected to various conditions of storage as per ICH guidelines for 3 months. ATC SNEDDS successfully withstood the stability testing. Thus this study indicates that the SNEDDS can be used as a potential drug carrier for solubility enhancement thereby drug release of ATC and other lipophilic drugs.

Keywords: Self-nanoemulsifying drug delivery systems, Pseudo-ternary phase diagrams, Thermodynamic stability

Cite this Article

Panner Selvam R, Parthasarathi K Kulkarni, Mudit Dixit, Self-Nanoemulsifying Drug Delivery System for Atorvastatin Calcium: Design, Optimization and Evaluation, Research & Reviews: A Journal of Drug Design & Discovery, 2015; 2(2): 27–36p.