PREPARATION AND EVALUATION OF MARAVIROC MUCOADHESIVE MICROSPHERES FOR GASTRO RETENTIVE DRUG DELIVERY
Keywords:
Pectin, HPMC K4, HPMC K15M, HPMC K100, Maraviroc, Mucoadhesive microspheresAbstract
Objective: The objective of this research was to formulate and evaluate pectin and HPMC different grades mucoadhesive microspheres in combination with sodium alginate for controlled release of maraviroc.
Methods: The maraviroc mucoadhesive microspheres was successfully developed by Ionotropic gelation technique, using sodium alginate, pectin, HPMC K4, K15, and K100 as mucoadhesive polymer in various proportions in combination. Further, the prepared maraviroc mucoadhesive microspheres were characterized for particle size, morphology, micrometric studies, entrapment efficiency, mucoadhesion, in vitro drug release, release kinetics, compatibility studies (FTIR) and stability studies.
Results: The maraviroc Microspheres was discrete and free-flowing. The mean particle size ranged from 646.3±10.2 μm to 910.0±6.56 μm and the entrapment efficiency ranged from 50.80% to 91.43%. Entrapment efficiency of maraviroc microspheres was increased by increasing drug to mucoadhesive polymer ratio. Scanning electron microscopy revealed the rough surface morphology and no visible cracks of best formulation F16. The FTIR study confirmed the stable nature of maraviroc in the drug-loaded mucoadhesive microspheres. All the maraviroc microspheres showed good mucoadhesive property ranging from 04-73 % in the in-vitro wash off test after 8 hours. The Crystallinity of maraviroc was found to be reduced in prepared mucoadhesive microspheres, which were confirmed by XRD studies. The mechanism of maraviroc release from the mucoadhesive microsphere was found to be anomalous and super case-II transport type. Stability studies were carried out for the best formulation F16 indicates that there is no change in entrapment efficiency and percentage mucoadhesion of the formulation.
Conclusion: The results obtained in this research work clearly indicated a promising potential of control release maraviroc mucoadhesive microspheres containing HPMC K100 as a rate controlling polymer for the effective treatment of AIDS/HIV patients.
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