FORMULATION AND IN-VITRO/IN-VIVO ASSESSMENT OF ENHANCED BIOAVAILABILITY OF LACIDIPINE USING NANO PURE TECHNIQUE

The objective of this study was to formulate and evaluate a novel drug solubilization platform (so called Nano-suspension prepared by comminution method using High pressure homogenizer; GEA Niro soavi) and further use the nano-suspension as granulating fluid admixed with excipients for further tablet production. The solid state characterization of Lacidipine along with the excipients reveal compatibility , as confirmed X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and Differential scanning calorimetry (DSC). The performance of Nano suspension is highly dependent on the selection of polymer stabilizer; hence different polymers such as hydroxy propyl cellulose, propylene glycol and poly vinyl pyrollidone were used in the study and evaluated. The results revealed hydroxy propyl cellulose as a suitable stabilizer compared to others polymer. The dissolution studies of Lacidipine shows complete release of drug within 45 minutes using hydroxy propyl cellulose as stabilizer in comparison to  available marketed product. Hydroxy propyl cellulose was better adsorbed with the drug compared to other polymers resulting in better mechanical interaction during comminution which causes the drug particle size to reach in nano-meter scale. The particle size of the nano suspension as confirmed by Zeta sizer revealed a particle size of 293.7 nm. The appearance of the nano suspension shows a bluish opalescence and the morphology revealed by Transmission electron microscope shows a particle size of 200.0 nm. The In-Vivo pharmacokinetic study was performed on rabbits to assess the bioavailability, since the bioavailability is directly proportional to the particle size. The In-Vivo pharmacokinetic results revealed that the AUC and Cmax were increased to two and six folds respectively in comparison to conventional market tablet. This may be recognized to increase solubility and permeability of the drug due to this novel formulation approach.