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Improvement of bone microarchitecture in methylprednisolone induced rat model of osteoporosis by using thiolated chitosan-based risedronate mucoadhesive film

Mukherjee, Dhrubojyoti and Srinivasan, Bharath and Anbu, J and Azamthulla, Mohammad and Banala, Venkatesh Teja and Ramachandra, SG (2018) Improvement of bone microarchitecture in methylprednisolone induced rat model of osteoporosis by using thiolated chitosan-based risedronate mucoadhesive film. In: DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 44 (11). pp. 1845-1856.

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Official URL: http://dx.doi.org/ 10.1080/03639045.2018.1503297

Abstract

Objective: In this study, we investigated the potential of thiolated chitosan-based mucoadhesive film, loaded with risedronate sodium in the treatment of osteoporosis. Significance: Risedronate sodium is a bisphosphonate derivative having very low bioavailability when administered through the oral route. Moreover, the adverse effects associated with the drug when administered through GIT necessitate an alternative and feasible route which can improve its bioavailability and therapeutic efficacy. Methods: Thiolation of chitosan was interpreted by different analytical techniques. The mucoadhesive films were prepared by the solvent evaporation method and evaluated for drug content analysis, swelling degree, mucoadhesive parameters, and permeation characterization. For the screening of preclinical efficacy and pharmacodynamic parameters, a methylprednisolone induced osteoporotic rat model was used. The trabecular microarchitecture and biochemical markers were evaluated for determination of bone resorption. Results: The different analytical characterization of synthesized thiolated chitosan revealed that chitosan was successfully incorporated with thiol groups. The formulation containing 2:1 ratio of thiolated chitosan and HPMC-4KM was found to have the maximum swelling degree, mucoadhesive strength with a good force of adhesion and better in vitro permeability compared to the marketed formulation. With respect to trabecular microarchitecture, the drug-loaded film formulation showed superior and promising results. Furthermore, the film formulation also improved the serum level of biomarkers better than the marketed formulation. Conclusions: The results significantly suggest that risedronate loaded novel mucoadhesive film formulation could be a logical approach in the therapeutic intervention of osteoporosis.

Item Type: Journal Article
Additional Information: Copy right for this article belong to TAYLOR & FRANCIS LTD
Keywords: Thiolation; mucoadhesive films; osteoporosis; risedronate sodium; methylprednisolone; trabecular microarchitecture
Department/Centre: Division of Biological Sciences > Central Animal Facility (Formerly Primate Research Laboratory)
Depositing User: Id for Latest eprints
Date Deposited: 11 Oct 2018 13:53
Last Modified: 11 Oct 2018 13:53
URI: http://eprints.iisc.ac.in/id/eprint/60865

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