Development of Self-Nano-Emulsifying Drug Delivery System for Gemcitabine: In Vitro and Ex Vivo Evaluation

Abstract

Researchers often aim to develop novel drug delivery systems to overcome the barriers associated with conventional drug delivery systems. Therefore, GEM (Gemcitabine), an anti-cancerous drug, belonging to the Biopharmaceutics Classification System (BCS) Class III with reduced permeability, is an important challenge. Self-nano-emulsifying drug delivery system (SNEDDS) was opted to be designed in such a way that it improves the permeability of GEM. From compatibility and solubility studies, Kolliphor RH40, castor oil, and polyethylene glycol-400 were chosen in optimized ratios for preparation into GEM-SNEDDS. GEM-SNEDDS F3 showed -12.1±6.83 mV zeta-potential, 0.406 PDI, and 94.81±82.73 nm particle size when tested for in vitro and ex vivo studies, F3 showed improved GEM release in simulated gastric fluid and simulated intestinal fluid in vitro and enhanced permeability ex vivo. These factors are prerequisites for the improvement of poor bioavailability of GEM. From stability studies, it was evident that F3 retained its physical stability at several stability conditions and in drug encapsulation and loading. Hence, we developed GEM-SNEDDS as a novel drug delivery system for increasing the permeability and, in turn, the oral bioavailability of GEM.