Abstract
STUDIES ON DEVELOPMENT OF GASTRORETENTIVE DOSAGE FORMS OF NELFINAVIR MESYLATE– AN ANTIRETROVIRAL DRUG, THROUGH THE STRATEGY OF MUCOADHESION

Jyothirmayee Devineni, Nagamalleswara Rao S. R. Buchi Naidu Nalluri and Vijaya Ratna Jayanti

ABSTRACT

Objectives: The aim and objective of present investigation was development and in vitro, in vivo evaluation of oral controlled release (CR) mucoadhesive tablets of Nelfinavir Mesylate (NLF), an anti-retroviral drug. Experimental: NLF Mucoadhesive tablets were prepared by direct compression method using chitosan, carbopol and hydroxyl propylmethyl cellulose (HPMC K4M) as mucoadhesive and release retardant polymers. The effect of different concentrations (10%, 15%, 20%w/w) of polymers and solubilizing agents like cyclodextrins were studied on the NLF release from mucoadhesive tablets. Also the NLF compatibility with the excipients was evaluated by Fourier Transmittance Infrared Spectrometry (FTIR) and Differential Scanning Calorimetry (DSC). Optimized formulation was further subjected to bioavailability studies using prototype formulation to the rabbit body weight. Results and Discussion: The FTIR and DSC results indicated that there was no in situ interaction between NLF and the selected excipients of the formulations. Formulation containing 10% w/w chitosan as mucoadhesive/release retardant polymer and 10% w/w hydroxypropyl-β-cyclodextrin(F10) gave a complete and controlled release of NLF (99.99 ± 0.14%) at the end of 10 h and the NLF release followed diffusion mechanism. Comparative bioavailability studies were carried out on optimized formulation and NLF suspension. Formulation F10 showed better relative bioavailability than that of NLF suspension. Conclusion: The results of this study provide guidance for developing mucoadhesive tablet of NLF that give greater bioavailability, than existing dosage forms, and provide protection against Permeability-glycoprotein (p-gp) efflux. The time plasma concentration profiles clearly indicated a controlled release of NLF over a period of 10 hrs.

Keywords: Nelfinavir mesylate, mucoadhesive polymers, cyclodextrins, Dissolution studies.


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