Application of zotepine, an antipsychotic agent, was limited due to its low therapeutic index which in-turn due to its poor aqueous solubility and low oral bioavailability. Hence the aim of present study was to develop zotepine loaded nanoparticle (ZNP) to overcome the problems and also to improve its brain uptake. Zotepine loaded nanoparticles were prepared by solvent evaporation technique using biodegradable PLGA as carriers, PVA as surfactant and were evaluated. Zotepine loaded nanoparticles were optimized by evaluating particle size, zeta potential and % entrapment efficiency. TEM result confirmed the size distribution and morphology. Comparative brain uptake study was carried out through concentration achieved in brain and AUC for developed ZNPs and marketed formulation on male albino wistar rats by RP-HPLC method. Particle size, zeta potential and % E.E of optimized batch containing were found to be 259.13±3.42 nm, -23.3±3.02 mV and 70.41±2.71% respectively. Higher drug concentration at all-time points and also higher AUC for developed formulation suggesting effective CNS transport of drug. Findings of present investigation revealed that developed zotepine loaded nanoparticles through oral route could be a promising approach for brain targeting of zotepine.
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