title: Dual crosslinked pectin-alginate network as sustained release hydrophilic matrix for repaglinide.
abstract: Repaglinide, an oral antidiabetic agent, has a rapid onset of action and short half-life of approximately 1h. Developing a controlled and prolonged release delivery system is required to maintain its therapeutic plasma concentration and to eliminate its adverse effects particularly hypoglycemia. The present study aimed to develop controlled release repaglinide loaded beads using sodium alginate and pectin with dual cross-linking for effective control of drug release. The prepared beads were characterized for size, percentage drug entrapment efficiency, in vitro drug release and the morphological examination using scanning electron microscope. For the comparative study, the release profile of a marketed conventional tablet of repaglinide (Prandin®tablets 2mg, Novo Nordisk) was determined by the same procedure as followed for beads. The particle size of beads was in the range of 698±2.34-769±1.43μm. The drug entrapment efficiency varied between 55.24±4.61 to 82.29±3.42%. The FTIR results suggest that there was no interaction between repaglinide and excipients. The XRD and DSC results suggest partial molecular dispersion and amorphization of the drug throughout the system. These results suggest that repaglinide did not dissolve completely in the polymer composition and seems not to be involved in the cross-linking reaction. The percent drug release was decreased with higher polymer concentrations. In conclusion, the developed beads could enhance drug entrapment efficiency, prolong the drug release and enhance bioavailability for better control of diabetes.
authors.affiliation: NKBR College of Pharmacy & Research Centre, Meerut - Hapur Road, Meerut, 245 206, Uttar Pradesh, India. Electronic address: awasthi02@gmail.com.
authors.forename: Rajendra
authors.initials: R
authors.lastname: Awasthi
authors.affiliation: Amity Institute of Pharmacy, Amity University, Sec 125, Noida, 201303, Uttar Pradesh, India.
authors.forename: Giriraj T
authors.initials: GT
authors.lastname: Kulkarni
authors.affiliation: Amity Institute of Pharmacy, Amity University, Lucknow, 226028, Uttar Pradesh, India.
authors.forename: Malipeddi Venkata
authors.initials: MV
authors.lastname: Ramana
authors.affiliation: Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Rua Professor Lineu Prestes, 05508-000, Brazil.
authors.forename: Terezinha
authors.initials: T
authors.lastname: de Jesus Andreoli Pinto
authors.affiliation: Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Rua Professor Lineu Prestes, 05508-000, Brazil.
authors.forename: Irene Satiko
authors.initials: IS
authors.lastname: Kikuchi
authors.affiliation: Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Rua Professor Lineu Prestes, 05508-000, Brazil.
authors.forename: Daniela Dal
authors.initials: DD
authors.lastname: Molim Ghisleni
authors.affiliation: Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Rua Professor Lineu Prestes, 05508-000, Brazil.
authors.forename: Marina
authors.initials: M
authors.lastname: de Souza Braga
authors.affiliation: Department of Pharmacy and Pharmacology, The University of Bath, Claverton Down, Bath, BA2 7AY, United Kingdom.
authors.forename: Paul
authors.initials: P
authors.lastname: De Bank
authors.affiliation: School of Pharmaceutical Sciences, Shoolini University, Solan, Himachal Pradesh, 173229, India; School of Pharmacy and Biomedical Sciences, The University of Newcastle, Newcastle, Callaghan, NSW, 2308, Australia.
authors.forename: Kamal
authors.initials: K
authors.lastname: Dua
mesh_terms: D000268:Adhesiveness; D000464:Alginates / Q000737:chemistry*; D002219:Carbamates / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D004811:Epichlorohydrin / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D009092:Mucous Membrane / Q000737:chemistry; D010316:Particle Size; D010368:Pectins / Q000737:chemistry*; D010880:Piperidines / Q000737:chemistry*; D013696:Temperature
chemical_list: D000464:Alginates; D002219:Carbamates; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006603:Hexuronic Acids; D010880:Piperidines; D004811:Epichlorohydrin; C072379:repaglinide; D010368:Pectins; D020723:Glucuronic Acid
keywords: Crosslinked beads; Crosslinking method; Dual crosslinking; Repaglinide; Sustained release