FORMULATION AND EVALUATION OF NEVIRAPINE MUCOADHESIVE MICROSPHERES
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 6
Abstract
Objective: The objective of the present research was to formulate and evaluate HPMC K4M, HPMC K100, and Carbopol 940 Mucoadhesive microspheres in combination with sodium alginate for controlling release of Nevirapine. Methods: Nevirapine microspheres were prepared by an Ionotropic gelation method using aluminium sulfate as a cross linking agent. The developed Nevirapine microspheres were characterized for Micromeritic properties, morphology, drug entrapment efficiency, in vitro wash off test, in vitro drug release, and interaction studies (Fourier transfer infrared spectroscopy (FTIR) & Differential scanning calorimetry (DSC). Results: The Nevirapine mucoadhesive microspheres were free-flowing and discrete. The mean particle size ranged from 705.21±2.00 to 935.45±2.07 μm and the entrapment efficiencies ranged from 63.50 to 96.42 %. All the nevirapine microsphere batches showed good in vitro mucoadhesive property ranging from 03-68 % in the in-vitro mucoadhesive test after 8 h. FT-IR studies indicated the lack of nevirapine-polymer interactions in the nevirapine microspheres formulation. There were no compatibility issues and the crystallinity of nevirapine was found to be reduced in prepared mucoadhesive microspheres, which were confirmed by DSC and X-ray diffraction studies (XRD). Among different formulations, the nevirapine microspheres of batch F8 had shown the optimum percent drug entrapment and the controlled release of the nevirapine for about 12 h (98.65%). The Release pattern of nevirapine from microspheres of batch F8 followed the Korsmeyer- peppas and zero-order release kinetic model. The value of ‘n’ was found to be 1.402, which indicates that the drug release was followed super case II transport type. Stability studies were carried out for F8 formulation at 4 °C/Ambient, 25±2 °C/60±5 %, 40±2 °C/75±5 % RH revealed that the drug entrapment and mucoadhesive behavior were within permissible limits. Conclusion: The results obtained in this present work demonstrate the potential use of HPMC K100 polymer for preparation of controlled delivery nevirapine mucoadhesive microspheres and prolonged residence at the absorption site.Â
Authors and Affiliations
Dasari Ararath, Sellappan Velmurugan
Keywords
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