Mucoadhesive chitosan-coated PLGA nanoparticles for oral delivery of ferulic acid

Abstract

This paper describes the development and in vitro evaluation of poly(lactic-co-glycolic acid) (PLGA) nanoparticles coated with chitosan (CS) for oral delivery of ferulic acid (FA). Nanoparticles were obtained by an emulsion evaporation technique and characterized. Furthermore, we evaluated the scavenging activity over hypochlorous acid (HOCl), the cytotoxicity over tumour cells and the in vitro intestinal permeability. Nanoparticles were spherical with a mean diameter of 242 nm, positive zeta potential and 50% of encapsulation efficiency. The in vitro release in phosphate buffered saline (PBS) (pH 7.4) demonstrated a prolonged and biphasic profile diffusion-controlled. In simulated gastrointestinal fluids, about 15% of FA was released in gastric fluid and a negligible release was observed in the intestinal fluid. In the HOCl scavenging activity and cytotoxicity over B16-F10 and HeLa cells, FA-loaded nanoparticles presented the same efficacy of the free drug. Besides, in the antioxidant and cytotoxic assay, CS contributed to FA effects. In the intestinal permeability study, FA-loaded nanoparticles exhibited a permeation of 6% through the Caco-2 monolayer and 20% through the Caco-2/HT29-MTX/Raji B co-culture. CS-coated PLGA nanoparticles are promising carriers for oral delivery of FA.