Abstract

Chukwuma O. Agubata*, Ozioma C. Onwumere, Jude N. Oraeluno, Josephat C. Obasi, Innocencia C. Chidebelu, Paul A. Akpa

ABSTRACT

Solid lipid microparticles are drug carriers that can be used to improve the efficacy, bioavailability and stability of drugs. The drug delivery system can also be used to control or modify the release of active pharmaceutical ingredients. The aim of this study is to prepare and characterize self-emulsifying solid lipid microparticles of glibenclamide, a hypoglycaemic anti-diabetic agent, using caprylocaproyl macrogol-8-glyceride (LABRASOL®). The microparticles were prepared by hot homogenization technique and batches were prepared with glibenclamide (0.05%w/v), stearic acid (1.5-2.5%w/v), MAISINE® oil (0.5-1.5%w/v), LABRASOL® (1-2%w/v), sodium benzoate (0.5%w/v) and distilled water. The dispersion of self-emulsifying solid lipid microparticles were evaluated for particle size, viscosity, pH, self-emulsification time, effect of aqueous dilution and centrifugation on stability, encapsulation efficiency and in vitro drug release and diffusion study. The results showed relatively stable formulations with self-emulsification time of 1.75-4 min, particle size range of 6.0 – 47.6?m, pH of around 6, viscosity of 8-78 mPas, encapsulation efficiency of mostly around 30%. Optimized formulations showed almost 100% drug diffusion through dialysis membrane in 30 min. In conclusion, the self-emulsifying solid lipid microparticles showed satisfactory physicochemical properties and diffusion capabilities, and are valuable carriers for glibenclamide in the management of diabetes mellitus.