Preparation of Fenofibrate loaded Eudragit L100 nanoparticles by nanoprecipitation method

Abstract

Abstract Successful adsorption of oral administered drugs is hindered by degradation during first pass metabolism. One method that has been recently employed to increase bioavailability of drugs is to encapsulate them in polymeric nanoparticles. In this study, Fenofibrate, used as a model substance for BCS type II drugs, has been encapsulated in Eudragit L100 nanoparticles, which shows pH dependent solubility at pH >6, thus release characteristics. This enables the loaded NPs to pass through the stomach without degradation until it reaches the intestine, where the drug is released and absorbed. For encapsulation, solvent displacement method was employed. Parameters that affect NPs quality such as polymer concentration, surfactant presence and concentration, and organic and aqueous ratio were optimized. In addition, an encapsulation efficiency test was carried out. The optimized concentration for Eudragit L100 was 1.35% since it was enough to get a critical nucleation concentration but not too high so that agglomeration is propitiated. Moreover, the surfactant with the best stabilization capacity was Tween® 80 due to its non-polymeric nature with a critical concentration obtained at 0.25%. Finally, a formulation with an end concentration of 250 µg/mL, presented the highest %EE determined with an HPLC assay.