Poor aqueous solubility and limited oral bioavailability remain major challenges in the effective delivery of many therapeutically potent drugs. Nanostructured drug delivery systems offer a promising approach to overcome these limitations by enhancing solubility, permeability, and controlled drug release. The present study aimed to formulate and evaluate nanostructured controlled drug delivery systems for improving the bioavailability of Curcumin, a BCS Class IV drug with low solubility and permeability. Six nanostructured formulations (F1–F6) were developed using polymeric nanoparticle technology employing poly(lactic-co-glycolic acid) (PLGA) with varying polymer–drug ratios. The formulations were evaluated for particle size, polydispersity index (PDI), zeta potential, drug entrapment efficiency, in vitro drug release, release kinetics, morphology, stability, and bioavailability enhancement potential. Among all formulations, F4 demonstrated optimized characteristics with nanoscale particle size, high entrapment efficiency, sustained drug release, and superior release kinetics. Statistical analysis confirmed significant improvement (p < 0.05) in performance parameters of the optimized formulation. The study concludes that nanostructured controlled drug delivery systems are an effective strategy for enhancing the bioavailability of poorly soluble drugs.

Nanostructured drug delivery, Controlled release, Bioavailability enhancement, PLGA nanoparticles, Curcumin