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Development, optimization, and anti-diabetic activity of gliclazide-loaded alginate-methyl cellulose mucoadhesive microcapsules.

Abstract

The purpose of this work was to develop and optimize gliclazide-loaded alginate-methyl cellulose mucoadhesive microcapsules by ionotropic gelation using central composite design. The effect of formulation parameters like polymer blend ratio and cross-linker (CaCl(2)) concentration on properties of gliclazide-loaded alginate-methyl cellulose microcapsules like drug encapsulation efficiency and drug release were optimized. The optimized microcapsules were subjected to swelling, mucoadhesive, and in vivo studies. The observed responses coincided well with the predicted values from the optimization technique. The optimized microcapsules showed high drug encapsulation efficiency (83.57 ± 2.59% to 85.52 ± 3.07%) with low T(50%) (time for 50% drug release, 5.68 ± 0.09 to 5.83 ± 0.11 h). The in vitro drug release pattern from optimized microcapsules was found to be controlled-release pattern (zero order) with case II transport release mechanism. Particle sizes of these optimized microcapsules were 0.767 ± 0.085 to 0.937 ± 0.086 mm. These microcapsules also exhibited good mucoadhesive properties. The in vivo studies on alloxan-induced diabetic rats indicated the significant hypoglycemic effect that was observed 12 h after oral administration of optimized mucoadhesive microcapsules. The developed and optimized alginate-methyl cellulose microcapsules are suitable for prolonged systemic absorption of gliclazide to maintain lower blood glucose level and improved patient compliance.

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    • Authors

    Pal D, Nayak AK

    Institution

    Faculty of Pharmacy, The University of Sydney, NSW, Australia. drdilip71@gmail.com

    Source

    AAPS PharmSciTech 12:4 2011 Dec pg 1431-41

    MeSH

    Adhesiveness
    Administration, Oral
    Alginates
    Animals
    Blood Glucose
    Calcium Chloride
    Capsules
    Chemistry, Pharmaceutical
    Cross-Linking Reagents
    Delayed-Action Preparations
    Diabetes Mellitus, Experimental
    Drug Carriers
    Drug Compounding
    Female
    Gliclazide
    Glucuronic Acid
    Goats
    Hexuronic Acids
    Hypoglycemic Agents
    Intestinal Mucosa
    Male
    Methylcellulose
    Models, Statistical
    Particle Size
    Rats
    Solubility
    Technology, Pharmaceutical
    Time Factors

    Pub Type(s)

    Journal Article

    Language

    eng

    PubMed ID

    22038475