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Formulation And Evaluation Of Gastric- Mucoadhesive Drug Delivery Systems Of CaptoprilKeywords: Captopril , controlled release , orifice gelation , beads , mucoadhesion , oral drug delivery systems , sodium alginate. Abstract: Objective: A new oral drug delivery system was developed utilizing both the concepts ofcontrolled release and mucoadhesiveness, in order to obtain a unique drug delivery systemwhich could remain in stomach and control the drug release for longer period of time.Materials & Methods: Gastro-retentive beads of captopril were prepared by orifice ionicgelation method in 1:1 and 9:1 ratio of alginate along with mucoadhesive polymers viz;hydroxy propyl methyl cellulose, carbopol 934P, chitosan and cellulose acetate phthalate. Theprepared beads were subjected for various evaluation parameters.Results: The percentage drug content was found to be in the range of 59.4 - 91.9 percent forbeads. It was observed that as the alginate proportion was increased, the average size of beadsalso increased. Photomicrographs revealed that the beads were spherical in shape. Alginatechitosan(9:1) beads showed excellent microencapsulation efficiency (89.7 percent). Alginate-Carbopol 934P exhibited maximum efficiency of mucoadhesion in 0.1 N hydrochloric acid (44percent for 1:1 and 22 percent for 9:1) at the end of 8 hours, whereas least mucoadhesion wasobserved with alginate-Cellulose acetate phthalate beads. The in vitro release studies werecarried out in 0.1 N hydrochloric acid and the release were found to be more sustained withAlginate-chitosan beads (9:1) than Alginate-Carbopol 934P (1:1) beads. The alginate-celluloseacetate phthalate beads showed the better sustained release as compared to all other alginatepolymercombinations. Regression analysis showed that the release followed zero orderkinetics in 0.1 N hydrochloric acid (pH 1.2).Conclusion: The objectives of the present work was achieved ie, formulation, evaluation andusefulness of sodium alginate mucoadhesive beads of captopril with different mucoadhesivepolymers. Certainly these findings can be applied for sustained delivery of drugs withmucoadhesion. Further these findings help the industry to scale up the commercial production.
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