Formulation and Evaluation of Quercetin Polycaprolactone Microspheres for the Treatment of Rheumatoid Arthritis

Quercetin had been shown to be effective in the management of arthritis. However, bioavailability of quercetin is a concern for such treatment. This work aims at the development of intra-articular drug delivery system by controlled release of quercetin (loaded in microspheres) for the management of rheumatoid arthritis. Polycaprolactone has been used for the preparation of microspheres (with quercetin) using the solvent evaporation method. The physio-chemical characterisation of polycaprolactone-loaded quercetin microspheres was carried out to obtain information about particle size distribution, drug loading efficiency, morphology, thermal properties, polymorphism and release trends in phosphate-buffered saline at pH 7.4 and 37 degrees C. Quercetin-loaded polycaprolactone microspheres were found to be biocompatible as evidenced from in vitro and in vivo studies using a rabbit synovial cells and Wistar rats, respectively. Quercetin release from microspheres of selected formulations showed biphasic nature due to initial burst effect followed by a controlled release. These results suggest that optimised quercetin-loaded polycaprolactone microspheres may be the viable strategy for controlled release of quercetin in the joint cavity for more than 30 days by intra-articular injection to treat rheumatoid arthritis. (C) 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:195-205, 2011