Peroral delivery of risedronate sodium for treatment of osteoporosis

Abstract

Oral route of administration is considered as most widely accepted route which is a potential site for drug delivery, direct access to systemic circulation and site of action. Bisphosphonates are the class of drugs which have been approved for clinical use in osteoporosis and other bone diseases. Bisphosphonates are very poorly absorbed from the GI tract and have limited bioavailability of less than 1% with adverse gastrointestinal effects in humans. The present work aimed to develop sublingual spray formulation using Risedronate sodium with combination of Pullulan gum and HPMC E5. Formulation of sublingual spray was developed by employing optimization technique. The optimized formulation was selected and evaluated for various pharmaco-technical parameters such as viscosity, spray angle, drug content per actuation, In-vitro drug diffusion study, Ex-vivo permeation study and In-vivo pharmacodynamics study by glucocorticoid induced model in rats. Pharmaco-technical parameter results of optimized formulation showed satisfactory results. Comparative In-vitro drug permeation and ex-vivo permeation studies showed maximum drug release of 85% for optimized formulation incorporated with permeation enhance transcutol. In-vivo pharmacodynamic study showed better efficacy in treatment animals with optimized formulation and thus newly developed risedronate sodium sublingual spray proved to be effective used in treatment of osteoporosis.