Improved treatment efficacy of risedronate functionalized chitosan nanoparticles in osteoporosis: formulation development, in vivo, and molecular modelling studies

Abstract

Delivery of bisphosphonates-like risedronate has been a major challenge till date due to its poor bioavailability and gastrointestinal tract adverse effects. In this study, we explored the prospective use of risedronate functionalised chitosan nanoparticle (RISCN) for management and treatment of osteoporosis. The prepared nanoparticle was characterised by using scanning electron microscopy, atomic force microscopy, and dynamic light scattering technique. Osteoporosis was induced on quarantined female Wistar rats and treated with RISCN. Docking studies were performed to establish the molecular mechanism of RISCN in improving the bone microarchitecture. Results indicated that there was a significant improvement in bone mineral density and healing of trabecular microarchitecture with less cortical porosity on the bone surfaces of the treatment groups. Docking studies indicated a high affinity and binding of chitosan and RISCN towards the human farnesyl diphosphate synthase (FDPS). Thus, a novel risedronate-loaded chitosan nanoparticle revealed promising results in an effective bone bridging process and osteoporosis treatment.

Keywords:

• Chitosan
• osteoporosis
• risedronate sodium
• bone microarchitecture
• bone mineral density

Acknowledgements

Authors appreciatively acknowledge Fleming Laboratories, Hyderabad for providing gift sample of Risedronate sodium. Authors are thankful to Micro and Nano characterisation facility (MNCF), Indian Institute of Science, Bangalore for carrying out SEM and AFM studies. The authors candidly thank M.S.Ramaiah University of Applied Sciences and Gokula Education Foundation (GEF) for supporting with the facilities for the project. The authors wish to thank Dr Ann Mary and Ms Hajira Banu, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences for assisting in the language editing process and plagiarism check of the manuscript.

Disclosure statement

No potential conflict of interest was reported by the authors.