Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide

Awasthi, R; Kulkarni, GT; Ramana, MV; de Jesus Andreoli Pinto, T; Kikuchi, IS; Molim Ghisleni, DD; de Souza Braga, M; De Bank, P; Dua, K

Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide

Awasthi, R Kulkarni, GT Ramana, MV de Jesus Andreoli Pinto, T Kikuchi, IS Molim Ghisleni, DD de Souza Braga, M De Bank, P Dua, K

Permalink

Publication Type:: Journal Article
Citation:: International Journal of Biological Macromolecules, 2017, 97 pp. 721 - 732
Issue Date:: 2017-04-01

Closed Access

	Filename	Description	Size
	1-s2.0-S0141813016324138-main.pdf	Published Version	4.6 MB	Adobe PDF	View/Open

Copyright Clearance Process

Recently Added
In Progress
Closed Access

This item is closed access and not available.

Full metadata record

Field	Value	Language
dc.contributor.author	Awasthi, R	en_US
dc.contributor.author	Kulkarni, GT	en_US
dc.contributor.author	Ramana, MV	en_US
dc.contributor.author	de Jesus Andreoli Pinto, T	en_US
dc.contributor.author	Kikuchi, IS	en_US
dc.contributor.author	Molim Ghisleni, DD	en_US
dc.contributor.author	de Souza Braga, M	en_US
dc.contributor.author	De Bank, P	en_US
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159	en_US
dc.date.available	2017-01-11	en_US
dc.date.issued	2017-04-01	en_US
dc.identifier.citation	International Journal of Biological Macromolecules, 2017, 97 pp. 721 - 732	en_US
dc.identifier.issn	0141-8130	en_US
dc.identifier.uri	http://hdl.handle.net/10453/124268
dc.description.abstract	© 2017 Elsevier B.V. Repaglinide, an oral antidiabetic agent, has a rapid onset of action and short half–life of approximately 1 h. 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 2 mg, 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 ± 1.43 μm. 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.	en_US
dc.relation.ispartof	International Journal of Biological Macromolecules	en_US
dc.relation.isbasedon	10.1016/j.ijbiomac.2017.01.050	en_US
dc.subject.classification	Polymers	en_US
dc.subject.mesh	Mucous Membrane	en_US
dc.subject.mesh	Carbamates	en_US
dc.subject.mesh	Glucuronic Acid	en_US
dc.subject.mesh	Hexuronic Acids	en_US
dc.subject.mesh	Epichlorohydrin	en_US
dc.subject.mesh	Piperidines	en_US
dc.subject.mesh	Pectins	en_US
dc.subject.mesh	Alginates	en_US
dc.subject.mesh	Delayed-Action Preparations	en_US
dc.subject.mesh	Drug Carriers	en_US
dc.subject.mesh	Temperature	en_US
dc.subject.mesh	Kinetics	en_US
dc.subject.mesh	Particle Size	en_US
dc.subject.mesh	Adhesiveness	en_US
dc.subject.mesh	Hydrophobic and Hydrophilic Interactions	en_US
dc.subject.mesh	Drug Liberation	en_US
dc.title	Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide	en_US
dc.type	Journal Article
utslib.citation.volume	97	en_US
utslib.for	0601 Biochemistry and Cell Biology	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Graduate School of Health
utslib.copyright.status	closed_access
pubs.publication-status	Published	en_US
pubs.volume	97	en_US

Abstract:

© 2017 Elsevier B.V. Repaglinide, an oral antidiabetic agent, has a rapid onset of action and short half–life of approximately 1 h. 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 2 mg, 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 ± 1.43 μm. 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.

Please use this identifier to cite or link to this item:

http://hdl.handle.net/10453/124268