Chitosan-coated nanostructured lipid carriers of fenofibrate with enhanced oral bioavailability and efficacy

Abstract

Fenofibrate is frequently used to lower cholesterol levels in cardiovascular disease. Owing to its poor solubility and high gastrointestinal permeability, it is classified as a Biopharmaceutics Classification System class II compound. The aim of this study was to improve the solubility and bioavailability of fenofibrate by formulating it as fenofibrate-loaded nanostructured lipid carriers (FFB-NLCs) and coating it with a biodegradable polymer to allow controlled drug release. Chitosan-coated nanostructured lipid carriers (CF-NLCs) were prepared via an ultrasonication method using chitosan as the biodegradable polymer, stearic acid as the solid lipid, oleic acid as the liquid lipid, and Tween 80 as the surfactant. To study encapsulation efficiency and solubility conditions, stearic acid/oleic acid ratios were varied as 80/20, 70/30, 60/40, and 50/50 (mg/mg), by adjusting chitosan ratio. Chitosan is an adhesive polymer, coating the surface of the NLC to improve its bioavailability. All NLC formulations demonstrated a particle size of approximately 200 nm and a polydispersity index below 0.3. The encapsulation efficiencies of the NLC formulations were above 85%. For CF-NLCs, the solubility and encapsulation efficiency of fenofibrate were increased when compared with those of a commercial fenofibrate formulation. The pharmacokinetic and pharmacodynamic parameters of fenofibrate in the form of CF-NLCs were improved after oral administration. CF-NLCs can be used for allowing controlled release and improving the bioavailability and stability of fenofibrate.