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

Rajendra Awasthi, Giriraj Kulkarni, Malipeddi Venkata Ramana, Terezinha Pinto, Irene Satiko Kikuchi, Daniela Ghisleni, Marina de Souza Braga, Paul De Bank, Kamal Dua

Research output: Contribution to journalArticle

  • 3 Citations

Abstract

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 to 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.
LanguageEnglish
Pages721-732
JournalInternational Journal of Biological Macromolecules
Volume97
Early online date20 Jan 2017
DOIs
StatusPublished - Apr 2017

Fingerprint

repaglinide
Pharmaceutical Preparations
Tablets
Polymers
Excipients
Cross Reactions
Fourier Transform Infrared Spectroscopy
Hypoglycemia
Particle Size
Hypoglycemic Agents
Biological Availability
Half-Life
alginic acid
pectin
Amorphization
Medical problems

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Awasthi, R., Kulkarni, G., Ramana, M. V., Pinto, T., Kikuchi, I. S., Ghisleni, D., ... Dua, K. (2017). Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide. International Journal of Biological Macromolecules, 97, 721-732. DOI: 10.1016/j.ijbiomac.2017.01.050

Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide. / Awasthi, Rajendra; Kulkarni, Giriraj; Ramana, Malipeddi Venkata; Pinto, Terezinha; Kikuchi, Irene Satiko; Ghisleni, Daniela; de Souza Braga, Marina; De Bank, Paul; Dua, Kamal.

In: International Journal of Biological Macromolecules, Vol. 97, 04.2017, p. 721-732.

Research output: Contribution to journalArticle

Awasthi, R, Kulkarni, G, Ramana, MV, Pinto, T, Kikuchi, IS, Ghisleni, D, de Souza Braga, M, De Bank, P & Dua, K 2017, 'Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide' International Journal of Biological Macromolecules, vol 97, pp. 721-732. DOI: 10.1016/j.ijbiomac.2017.01.050
Awasthi R, Kulkarni G, Ramana MV, Pinto T, Kikuchi IS, Ghisleni D et al. Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide. International Journal of Biological Macromolecules. 2017 Apr;97:721-732. Available from, DOI: 10.1016/j.ijbiomac.2017.01.050
Awasthi, Rajendra ; Kulkarni, Giriraj ; Ramana, Malipeddi Venkata ; Pinto, Terezinha ; Kikuchi, Irene Satiko ; Ghisleni, Daniela ; de Souza Braga, Marina ; De Bank, Paul ; Dua, Kamal. / Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide. In: International Journal of Biological Macromolecules. 2017 ; Vol. 97. pp. 721-732
@article{88562ade5acb405d9537bcdfcd627253,
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 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{\circledR} 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 to 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.",
author = "Rajendra Awasthi and Giriraj Kulkarni and Ramana, {Malipeddi Venkata} and Terezinha Pinto and Kikuchi, {Irene Satiko} and Daniela Ghisleni and {de Souza Braga}, Marina and {De Bank}, Paul and Kamal Dua",
year = "2017",
month = "4",
doi = "10.1016/j.ijbiomac.2017.01.050",
language = "English",
volume = "97",
pages = "721--732",
journal = "International Journal of Biological Macromolecules",
issn = "0141-8130",
publisher = "Elsevier",

}

TY - JOUR

T1 - Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide

AU - Awasthi,Rajendra

AU - Kulkarni,Giriraj

AU - Ramana,Malipeddi Venkata

AU - Pinto,Terezinha

AU - Kikuchi,Irene Satiko

AU - Ghisleni,Daniela

AU - de Souza Braga,Marina

AU - De Bank,Paul

AU - Dua,Kamal

PY - 2017/4

Y1 - 2017/4

N2 - 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 to 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.

AB - 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 to 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.

UR - https://doi.org.10.1016/j.ijbiomac.2017.01.050

U2 - 10.1016/j.ijbiomac.2017.01.050

DO - 10.1016/j.ijbiomac.2017.01.050

M3 - Article

VL - 97

SP - 721

EP - 732

JO - International Journal of Biological Macromolecules

T2 - International Journal of Biological Macromolecules

JF - International Journal of Biological Macromolecules

SN - 0141-8130

ER -