FORMULATION, DEVELOPMENT AND EVALUATION OF MUCOADHESIVE MICROSPHERE OF STAVUDINE
Raj Karan Pal*1, Girijesh Kumar Pandey1, Amit Joshi1, B.K. Dubey1, Prabhat Jain2
ABSTRACT
treatment of HIV infection, AIDS and AIDS-related conditions either alone or in combination with other antiviral agents. The stavudine has a very short half-life (0.8 to 1.5hr) with rapid absorption. The side effects of stavudine are dose dependent and a reduction of the total administered dose reduces the severity of the toxicity. Stavudine is typically administered orally as a capsule and oral solution. Dosage forms that are retained in the stomach would increase the absorption, improve drug efficiency and decrease dose requirements. The aim of the present study was to develop stavudine loaded chitosan microspheres by the ionic gelation method using sodium tripolyphosphate (Na-TPP) as the crosslinking agent. The use of ionotropic gelation avoids the possibility of the occurrence of the toxic and undesirable effects associated with the use of glutaraldehyde, a chemical crosslinking agent. The prepared microspheres were evaluated for mean particle size and particle size distribution, drug loading, encapsulation efficiency and in-vitro drug release. FT-IR spectroscopic analysis was performed to ascertain drug polymer interaction. The release profiles showed zero-order release behavior up to 12 hours where the highest drug release was 98.78 % of the stavudine loaded in the chitosan microspheres, indicating a strong crosslinking between chitosan and TPP anions. The surface morphology of the prepared microspheres was studied by SEM. With an increase in the crosslinking density the rate of drug release decreased. From the results of the present investigation it may be concluded that drug loaded chitosan microspheres can be prepared by a simple technique which avoids the use of complex apparatus and special precautions.
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