Development and Characterization of Rifampicin-Loaded Solid Lipid and PLGA Nanoparticles for Enhancement of Solubility and Bioavailability

Abstract

Tuberculosis remains a major global health concern, and rifampicin is a key first-line drug used in its treatment. However, rifampicin exhibits poor aqueous solubility and limited oral bioavailability, which may reduce therapeutic effectiveness. The present study aimed to develop and characterize rifampicin-loaded solid lipid nanoparticles (SLN) and poly (lactic-co-glycolic acid) (PLGA) nanoparticles to enhance drug solubility and bioavailability. PLGA nanoparticles were prepared using a modified multiple emulsion solvent evaporation technique, while SLN were formulated by hot high-shear homogenization. The formulations were optimized using response surface methodology and characterized for particle size, polydispersity index, zeta potential, encapsulation efficiency, and morphology. The optimized SLN showed particle sizes of 180–300 nm with 56.99% encapsulation efficiency, while PLGA nanoparticles exhibited sizes below 200 nm with 45.22% encapsulation efficiency. In vitro release studies demonstrated controlled drug release and improved dissolution compared with pure rifampicin. These results suggest that SLN and PLGA nanoparticles are promising carriers for enhancing rifampicin bioavailability in tuberculosis therapy.

Keywords: Rifampicin; Solid lipid nanoparticles; PLGA nanoparticles; Nanoparticle drug delivery; Bioavailability enhancement