Development of calcium pectinate-tamarind seed polysaccharide mucoadhesive beads containing metformin HCl

• Published in: Carbohydrate polymers Vol. 101; pp. 220 - 230
• Main Authors: Nayak, Amit Kumar, Pal, Dilipkumar, Santra, Kousik
• Format: Journal Article
• Language: English
• Published: Kidlington Elsevier Ltd 30.01.2014; Elsevier
• Subjects: Adhesiveness; Animals; Applied sciences; Biological and medical sciences; Controlled drug release; Drug Carriers - chemistry; Drug Carriers - metabolism; Exact sciences and technology; Female; General and cellular metabolism. Vitamins; Intestinal Mucosa - metabolism; Ionotropic-gelation; Male; Medical sciences; Metformin - chemistry; Metformin - pharmacology; Metformin HCl; Microspheres; Mucoadhesion; Natural polymers; Pectin; Pectins - chemistry; Pharmacology. Drug treatments; Physicochemistry of polymers; Rats; Seeds - chemistry; Starch and polysaccharides; Tamarind seed polysaccharide; Tamarindus - chemistry; Metformin HCl; Tamarind seed polysaccharide; Pectin; Ionotropic-gelation; Controlled drug release; Mucoadhesion; Encapsulation; Rat; Mucosa; Drug carrier; Response surface methodology; Time variation; Optimization; Hypoglycemic agent; Calcium ion; Surface properties; Manufacturing; Release; Adhesivity; Swelling; Control release polymer; Gelation; Rodentia; Experimental study; Operating conditions; In vivo; Vertebrata; Tamarind gum; Mammalia; Animal; Morphology; Oside polymer; Kinetics; Hydrogel; Metformin; Spherical particle; Glycemia
• ISSN: 0144-8617; 1879-1344
• DOI: 10.1016/j.carbpol.2013.09.024

•Novel mucoadhesive beads of metformin HCl was developed and optimized.•Low methoxy (LM) pectin-tamarind seed polysaccharide polymer-blend was used.•The in vitro drug release followed zero-order with super case-II transport mechanism.•The optimized beads showed pH-sensitive swelling and good mucoadhesive property.•These beads proved prolonged and significant hypoglycemic effect in diabetic rats. Novel mucoadhesive beads containing metformin HCl made of low methoxy (LM) pectin-tamarind seed polysaccharide (TSP) polymer-blend was developed through ionotropic-gelation technique and optimized using 32 factorial design. Effects of LM pectin and TSP amounts on drug encapsulation efficiency (DEE), and cumulative drug release at 10h (R10h) were analyzed using response surface methodology. The optimized calcium pectinate-TSP beads containing metformin HCl showed DEE of 95.12±4.26%, R10h of 46.53±3.28%, and mean diameter of 1.93±0.26mm. The in vitro drug release from these beads was followed controlled-release (zero-order) pattern with super case-II transport mechanism. These beads were also characterized by SEM and FTIR. The optimized beads also exhibited pH-dependent swelling, good mucoadhesivity with goat intestinal mucosa and significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration.