African Journal of
Biotechnology

  • Abbreviation: Afr. J. Biotechnol.
  • Language: English
  • ISSN: 1684-5315
  • DOI: 10.5897/AJB
  • Start Year: 2002
  • Published Articles: 12506

Full Length Research Paper

Novel carrier system for enhancing oral delivery of metformin

Adedokun, M. O.*
  • Adedokun, M. O.*
  • Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, University of Uyo, Uyo, Akwa Ibom State, Nigeria.
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Momoh, M. A.
  • Momoh, M. A.
  • Drug Delivery Research Unit, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.
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Kenechukwu, F. C.
  • Kenechukwu, F. C.
  • Drug Delivery Research Unit, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.
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Umeh, O. N. C.
  • Umeh, O. N. C.
  • Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.
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Okpalanedu, C. M. J
  • Okpalanedu, C. M. J
  • Drug Delivery Research Unit, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.
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Ofokansi, K. C.
  • Ofokansi, K. C.
  • Drug Delivery Research Unit, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.
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  •  Received: 10 June 2014
  •  Accepted: 02 December 2014
  •  Published: 10 December 2014

Abstract

This study was designed to evaluate the potential of PEGylated lipospheres as carriers for improved oral delivery of metformin hydrochloride. Lipospheres were prepared by melt-emulsification method using Phospholipon® 90H in beeswax (30%w/w) as the lipid matrix containing increasing quantities of PEG 4000 and characterized. The in vitro and in vivo release of the formulations was evaluated. Results show that the particle size and encapsulation efficiency ranged from 33.18±1.75 - 83.23±6.05 μm and 85 to 93%, respectively. Drug release showed a biphasic pattern and was found to follow the Higuchi square root model. Metformin hydrochloride -loaded lipospheres lowered basal blood glucose levels by 60% and sustained antihyperglycemia for over 20 h. This study suggests that encapsulation of metformin hydrochloride into PEGylated lipospheres could reduce its dosing frequency and the associated side effects resulting from high doses of metformin hydrochloride as seen in conventional tablet formulations.

 

Key words: PEGylated, lipospheres, metformin hydrochloride, anti-diabetic.