Development and evaluation of a self-emulsifying drug delivery system of amphotericin B

Abstract

Amphotericin B is a polyene antifungal antibiotic belonging to Class IV of Biopharmaceutics Classification System which is not absorbed from the gastrointestinal tract after oral administration. The aim of this research work was to develop a self-emulsifying drug delivery system (SEDDS) of amphotericin B and to evaluate the dissolution and permeability of amphotericin B from the formulation. The solubility of amphotericin B in various oils, surfactants and cosurfactants was determined.Various SEDDS formulations were prepared with varying amounts of oil, surfactant and co-surfactant. Evaluation parameters for formulation optimization were drug content, self-emulsification, droplet size analysis, and precipitation studies. In vitro dissolution was studied in comparison to the pure drug. Permeability was studied using non-everted intestinal sac method. The optimized formulation consisted of glycerol mono-oleate (10%, w/w), tween 80 (36%, w/w), polyethylene glycol 400 (27%, w/w), and propylene glycol (27%, w/w) with a drug content of about 8 mg per ml. The self-emulsifying formulation showed 100% dissolution within 30 minutes whereas the pure drug exhibited a very poor rate of dissolution.In vitro intestinal permeability was studied by noneverted intestinal sac method using rat intestine. The self-emulsifying formulation showed 100% drug permeation within 30 minutes compared to negligible permeation from the drug suspension. The study demonstrates that SEDDS approach may be useful for enhancement of dissolution and intestinal permeation of amphotericin B belonging to class IV of Biopharmaceutic Classification System.