Development, optimization, and anti-diabetic activity of gliclazide-loaded alginate-methyl cellulose mucoadhesive microcapsules.
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.
Faculty of Pharmacy, The University of Sydney, NSW, Australia. drdilip71@gmail.com
Dilipkumar
D
Pal
Amit Kumar
AK
Nayak
D000268:Adhesiveness; D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects*; D002122:Calcium Chloride / Q000737:chemistry; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D003432:Cross-Linking Reagents / Q000737:chemistry; D003692:Delayed-Action Preparations; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy*; D004337:Drug Carriers; D004339:Drug Compounding; D005260:Female; D005907:Gliclazide / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D020723:Glucuronic Acid / Q000737:chemistry / Q000378:metabolism; D006041:Goats; D006603:Hexuronic Acids / Q000737:chemistry / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D007413:Intestinal Mucosa / Q000378:metabolism*; D008297:Male; D008747:Methylcellulose / Q000737:chemistry* / Q000378:metabolism; D015233:Models, Statistical; D010316:Particle Size; D051381:Rats; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors
D000464:Alginates; D001786:Blood Glucose; D002214:Capsules; D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006603:Hexuronic Acids; D007004:Hypoglycemic Agents; D020723:Glucuronic Acid; D008747:Methylcellulose; D005907:Gliclazide; D002122:Calcium Chloride