Formulation, in vitro and in vivo evaluation of oral sustained release insulin-loaded microspheres based on Eudragit® RS100

FORMULATION, IN VITRO AND IN VIVO EVALUATION OF ORAL SUSTAINED RELEASE INSULIN-LOADED MICROSPHERES BASED ON EUDRAGIT® RS100

Mumuni A. Momoh1*, Franklin C. Kenechukwu1, Akpabio E. Ibanga2, Salome A. Chime3, Samson C. Ugwuagbo1, Kenneth C. Ofokansi1

  1. Drug Delivery Unit, Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Nigeria
  2. Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka 410001, Nigeria

Afr. J Pharm Res Dev; Volume 7(2): 109-123; Nov/Dec 2015

ABSTRACT

The objective of the study is to formulate oral sustained release insulin-loaded microspheres and to evaluate the in vitro and in vivo properties. Microspheres were formulated by double emulsion solvent evaporation method using Eudragit® RS 100 as the polymer. The microspheres were characterized based on differential scanning calorimetry, fourier transform infrared spectroscopy, the yield, particle size, micromeritic properties, encapsulation efficiency (EE%), bio-adhesion, in vitro drug release and in vivo hypoglycemic properties. Insulin-loaded microspheres showed endothermic peaks of 60.9 to 63 °C, maximum EE of 98.89 % and highest percentage bio-adhesion of 95 % and good flowability. Microspheres had good sustained release of insulin with 73.46 at 8 h. Insulin-loaded microspheres had significant blood glucose reduction comparable to the parenteral insulin between 6 to 8 h (P< 0.05). In conclusion, insulin-loaded microspheres had good in vivo and sustained release properties and could be used orally for the management of diabetes mellitus.

*Author for correspondence: audu.momoh@unn.edu.ng