title: Design and in vitro and in vivo characterization of mucoadhesive matrix pellets of metformin hydrochloride for oral controlled release: a technical note.
abstract: The aim of the current work was to design and develop matrix pellets of hydroxy propyl methyl cellulose K200M and microcrystalline cellulose in an admixture for a mucoadhesive gastroretentive drug delivery system. Pellets containing metformin hydrochloride (500 mg) were prepared by the pelletization technique using an extruder-spheronizer. Pellets were characterized by differential scanning calorimetry (DSC), x-ray diffraction (XRD), scanning electron microscopy (SEM), circularity, roundness, percent drug content, percent production yield, in vitro swelling, ex vivo mucoadhesion, in vitro drug release and in vivo x-ray imaging studies. Optimized pellets were sufficiently porous spheroids, free flowing, had smooth surfaces, had yields up to 75.45 ± 0.52% and had drug content up to 96.45 ± 0.19%. The average particle size of formulations MF2 and MF6 were 1.13 ± 0.41 mm and 1.22 ± 0.18 mm, respectively. Formulation MF6 exhibited strong adhesion, about 94.67%, to goat mucosal tissue, and the desired in vitro swelling, with a sustained drug release profile for 12 h and with retention in the upper small intestine of rabbits for 10 h. We conclude that hydroxy propyl methyl cellulose K200M and microcrystalline cellulose at a 2.80:1.00 w/w ratio could be an effective carrier for multiple unit controlled delivery of metformin hydrochloride.
authors.affiliation: Department of Pharmaceutics and Quality Assurance, R C Patel Institute of Pharmaceutical Education & Research, Shirpur, Dist Dhule, Maharashtra 425405, India. pradyumna_1978@rediffmail.com
authors.forename: Pradum Pundlikrao
authors.initials: PP
authors.lastname: Ige
authors.forename: Surendra Ganeshlal
authors.initials: SG
authors.lastname: Gattani
mesh_terms: D000268:Adhesiveness; D000284:Administration, Oral; D000818:Animals; D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004304:Dosage Forms; D004337:Drug Carriers; D004339:Drug Compounding; D005753:Gastric Mucosa / Q000378:metabolism*; D006041:Goats; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry; D065347:Hypromellose Derivatives; D007413:Intestinal Mucosa / Q000378:metabolism*; D007421:Intestine, Small / Q000000981:diagnostic imaging / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D008687:Metformin / Q000008:administration & dosage* / Q000737:chemistry; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D016062:Porosity; D011817:Rabbits; D011859:Radiography; D012995:Solubility; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D014961:X-Ray Diffraction
chemical_list: D003692:Delayed-Action Preparations; D004304:Dosage Forms; D004337:Drug Carriers; D007004:Hypoglycemic Agents; D065347:Hypromellose Derivatives; D002482:Cellulose; D008747:Methylcellulose; D008687:Metformin; C109691:microcrystalline cellulose