Polymeric nanoencapsulation of zaleplon into PLGA nanoparticles for enhanced pharmacokinetics and pharmacological activity

Zaleplon (ZP) is a sedative and hypnotic drug used for the treatment of insomnia. Despite its potent anticonvulsant activity, ZP not commonly convulsion since characterized by low oral bioavailability as result poor solubility extensive liver metabolism. The following study aimed to formulate specifically controlled release nano-vehicles parenteral delivery enhance biological activity. A modified single emulsification–solvent evaporation method sonication force was adopted optimize inclusion into biodegradable nanoparticles (NPs) using poly (dl-lactic-co-glycolic acid) (PLGA). impacts various formulation variables on physicochemical characteristics ZP-PLGA-NPs profiles were investigated. Pharmacokinetics pharmacological activity studied experimental animals compared with generic tablets. Assessment gamma-aminobutyric acid (GABA) level in plasma after administration conducted enzyme-linked immunosorbent assay. maximal electroshock-induced seizures model evaluated ZP-loaded NPs. prepared ZP-PLGA NPs negatively charged spherical particles an average size 120–300 nm. Optimized showed higher GABA levels, longer sedative, effects, 3.42-fold augmentation comparison ZP-marketed products. Moreover, ZP-NPs free drug. Oral achieved significant improvement bioavailability, pronounced