DEVELOPMENT OF MUCOADHESIVE MICROSPHERES OF LEVOFLOXACIN FOR THE TREATMENT OF H. PYLORI INFECTION
The rationale of the present investigation is to develop a new oral drug delivery system utilizing both the concepts of controlled release and mucoadhesiveness, which could remain in stomach and control the drug release for longer period of time and thus to improve the bioavailability of the drug and reducing its dose related side effects. Gelatin/Acrypol 934P mucoadhesive microspheres of Levofloxacin were prepared by Emulsification cross- linking method. Drug and excipients interactions are tested using Fourier Transform-Infrared Spectroscopy, indicated no interactions. The average particle size for optimized formulations of Gelatin/Acrypol 934P microspheres were found to be 41.5Âµm. Photomicrographs revealed that the microspheres were spherical in shape. The drug entrapment efficiency for Gelatin/ Acrypol 934P microspheres was found to be 85.43%. In vitro drug release from Gelatin/ Acrypol microspheres showed more than 75% of the drug was released within 8 Hr, while pure drug showed complete drug release within 3 hours. This suggested controlled delivery of Levofloxacin for a longer period. Regression analysis revealed that the drug release from the microspheres was followed zero order kinetics. SEM images suggested spherical shape with smooth surface of microspheres formulations. Optimized formulation of Gelatin/ Acrypol 934P microspheres showed excellent mucoadhesivity i.e., 86.5%. Thus, the proposed Gelatin/ Acrypol 934P mucoadhesive microspheres might make a contribution in complete eradication of Helicobacter pylori owing to prolonged stomach residence time and small particle size.
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