Three Ply-Walled Microcapsules for Enhanced Pharmacokinetics of Poorly Absorbed Risedronate Sodium: Novel Stratagem Toward Osteoporosis

Abstract

Effective and optimized drug delivery has always been one of the major challenge for the researchers in the last few decades and is still a very active field of research. The present investigation focuses on the development of a novel strategy to enhance the bioavailability of risedronate sodium which shows very poor and erratic absorption. A multiple emulsion technique has been used to prepare the three ply-walled microcapsules needed for targeting the specific sites. Box-Behnken model has been selected to optimize the effect of various process variables on particle size and entrapment efficiency. Optimized microcapsules (PN-F) were found to have a particle size of 3.97 ± 0.29 μm (PDI = 0.19 ± 0.09), entrapment efficiency of 79.12 ± 2.19 %, and maximum release of 96.34 ± 3.426 and 97.32 ± 2.486 % in simulated gastric and intestinal fluid, respectively, over the period of 24 h. In vivo pharmacokinetic study exhibits a substantial increase in the absolute bioavailability of the microcapsules (F = 40.68 ± 2.636 %) as compared to marketed formulation, RISOFOS®, CIPLA (F = 0.98 ± 0.086 %) (p < 0.01) leading to a more effective drug transport. A stability analysis has also been carried out and is found to be quite promising for the present formulation. The obtained outcomes strongly support the fact that the present formulation not only plays a vital role in the optimized delivery of risedronate sodium in osteoporosis management but also depicts negligible pitfalls.