To develop nanoparticles for oral controlled release of antifungal drug Clotrimazole and to improve its bioavailability. Nanoparticles of antifungal drug Clotrimazole were prepared by emulsion–solvent evaporation technique using PLGA as polymer. Different formulations were prepared using drug and polymer in 1:1, 1:2, 1:3 ratios respectively. To determine the effect of polymer and PVA the formulations were characterized for their entrapment efficiency, particle size, surface morphology and release behavior. In vivo study was carried out on Laca mice. Plasma drug concentration was determined by validated HPLC technique. The maximum percentage entrapment efficiency was found to be 66.50 ± 1.89. Mean particle size was found to be in the range of 308.0 to 438.5 nm. In vitro drug release studies showed that formulation F1 to F6 followed a diffusion controlled release. The biodistribution data suggested that there was a controlled drug release for 85 (h) with the selected formulations as compared to unencapsulated drug, which was cleared within 4-5 h after intravenous and oral administration. There was a striking improvement in the relative and absolute bioavailability of drug. The oral administration of unencapsulated drug was detected in various body organs such as liver, lungs and spleen up to 6 hrs. In case of drug loaded nanoparticles drug was found in liver, lungs, spleen, small intestine and kidney for one day. It can be concluded that oral administration of Clotrimazole nanoparticles form a sound basis for controlling drug release and improving its bioavailability
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