Formulation and Evaluation of Solid Lipid Nanoparticles of Posaconazole

Abstract

Posaconazole is a broad-spectrum triazole antifungal drug used for the treatment and prevention of invasive fungal infections. However, its poor aqueous solubility and limited bioavailability present significant challenges for effective oral drug delivery. The present study was aimed at the formulation and evaluation of Posaconazole-loaded Solid Lipid Nanoparticles (SLNs) using different polymers at varying ratios to enhance drug release and improve therapeutic performance.

A series of formulations (F1–F9) were prepared employing suitable lipids and polymers in different concentrations. The prepared formulations were evaluated for various physicochemical parameters. Pre-compression studies, including bulk density, tapped density, angle of repose, Carr's index, and Hausner ratio, demonstrated good flow properties of the formulations. Post-compression parameters such as hardness, friability, weight variation, drug content uniformity, and other quality control tests were found to be within the acceptable limits specified by the Indian Pharmacopoeia (IP), indicating satisfactory formulation characteristics.

The formulated SLNs were further characterized for particle size, entrapment efficiency, drug loading, and in vitro drug release studies. The results revealed that polymer concentration and drug-to-polymer ratio had a significant influence on the performance of the formulations. Among all the formulations, F4 was identified as the optimized formulation due to its superior drug release profile and satisfactory physicochemical properties. F4 exhibited a cumulative drug release of 99.47% over a period of 48 hours, which was significantly higher compared to the other formulations, indicating effective sustained-release behaviour and enhanced drug availability.

The study concludes that the developed Posaconazole-loaded Solid Lipid Nanoparticles successfully improved the drug release characteristics while maintaining acceptable pharmaceutical quality parameters. The optimized F4 formulation demonstrated excellent performance and has the potential to serve as an effective controlled-release drug delivery system for Posaconazole.