Abstract

The main aim of the present work is to formulate, optimize and evaluate a Nanostructured Lipid Carrier (NLC) of a poorly water soluble antipsychotic drug: Ziprasidone hydrochloride monohydrate (ZHM) by high shear homogenization technique followed by ultrasonication method to enhance the oral bioavailability. ZHM a dopamine receptor antagonist, is an orally active atypical antipsychotic drug used in the treatment of schizophrenia and bipolar disorder. ZHM is a BCS Class II drug which is poorly water-soluble so its oral bioavailability is 60% when administered with food. The absorption of ZHM is increased up to two-fold in the presence of food. Preformulation studies including screening of excipients for solubility suggested the suitability of precirol ATO 5 as solid lipid, labrafil M1944 as liquid lipid and gelucire 50/13 as stabilizer for preparation of NLC. The optimized ZHM-NLC was characterised by measuring particle size, drug entrapment efficiency and in vitro drug release. The concentration of solid lipid and liquid lipid in the ratio of 70:30 was optimised as final formulation components concentration as it exhibited desired mean particle size (200-302 nm) and % Entrapment efficiency (54-84%). The in vitro drug release study indicated the ZHM-NLC sustained release formulation showed sustained release profile of 98.62 % release within 24 hours. Based on this results it was concluded that NLCs are promising drug delivery for improving the oral bioavailability of ZHM.