Preparation and Evaluation of Pirfenidone Loaded Microspheres

Abstract

The present study was aimed at the preparation and evaluation of Pirfenidone-loaded microspheres for sustained drug delivery. Pirfenidone is an antifibrotic agent used in the treatment of idiopathic pulmonary fibrosis, and the development of a controlled-release formulation can improve therapeutic efficacy and patient compliance. Microspheres were prepared using an appropriate microencapsulation technique and evaluated for their physicochemical characteristics and drug release behaviour.

A series of formulations (F1–F9) were developed by varying the polymer concentrations. The prepared microspheres were subjected to pre-compression and post-compression evaluation tests, including bulk density, tapped density, angle of repose, Carr's index, Hausner's ratio, particle size analysis, drug content, entrapment efficiency, and in vitro drug release studies. The results revealed that all pre-compression and post-compression parameters were within the acceptable limits prescribed by the Indian Pharmacopoeia (IP), indicating good flow properties, uniformity, and overall quality of the formulations.

Among all the formulations, F5 was identified as the optimized formulation based on its superior performance in drug release studies. The optimized formulation exhibited a cumulative drug release of 99.72% over a period of 12 hours, which was higher than that of the other formulations and demonstrated an effective sustained-release profile.