International Journal of Pharmaceutical Investigation, 2016, 6, 2, 69-77.
DOI: 10.4103/2230-973X.177806
Published: March 2016
Type: Original Article
Authors:
Franklin C. Kenechukwu
Drug Delivery and Nanomedicines Research Unit, Department of Pharmaceutics, University of Nigeria, Nsukka, Enugu State, Nigeria.
Mumuni A. Momoh
Drug Delivery and Nanomedicines Research Unit, Department of Pharmaceutics, University of Nigeria, Nsukka, Enugu State, Nigeria.
ABSTRACT
Introduction: The aim of this study was to use Eudragit® RL 100 (pH-independent polymer) and magnesium stearate (a hydrophobic droplet stabilizer) in combination to improve the controlled release effect of insulin-loaded Eudragit® entrapped microspheres prepared by the emulsification-coacervation technique. Materials and Methods: Mucoadhesive insulin-loaded microspheres containing magnesium stearate and varying proportions of Eudragit® RL 100 were prepared by the emulsification-coacervation technique and evaluated for thermal properties, physicochemical performance, and in vitro dissolution in acidic and subsequently basic media. Results: Stable, spherical, brownish, discrete, freeflowing and mucoadhesive insulin-loaded microspheres with size range of 14.20 ± 0.30-19.80 ± 0.60 μm and loading efficiency of 74.55 ± 1.05-75.90 ± 1.94% were formed. After 3 h, microspheres prepared with insulin: Eudragit® RL 100 ratios of 1:4, 1:6, and 1:8 released 73.40 ± 1.38, 66.20 ± 1.59, and 71.30 ± 1.27 (%) of insulin, respectively. Conclusion: The physicochemical and physico-technical properties of the microspheres developed in this study demonstrated the effectiveness of the Eudragit® RL entrapped mucoadhesive microspheres (prepared by the emulsification-coacervation technique using varying polymer concentration) as a carrier system for oral insulin delivery.
Keywords: Eudragit® RL 100, Insulin release, Microspheres, Percentage mucoadhesion .