Development and evaluation of liposomal nanoparticles incorporating dimethoxycurcumin. In vitro toxicity and permeability studies

Abstract

Liposomes belong to the class of drug delivery nanosystems and are widely used for the incorporation and delivery of lipophilic drug molecules. The present work deals with the physicochemical characterization of different liposomal nanocarriers, loaded with dimethoxycurcumin (DMC), an analog of curcumin with antioxidant and anticancer activity. The in vitro toxicity and intestinal permeability of drug-free liposomes were evaluated using a Caco-2/TC7 and HT29-MTX co-culture. The results revealed that all liposomal nanosystems were of size lower than 180 nm upon preparation, while their ζ-potential depended on the type of utilized biomaterials. The incorporation efficiency of DMC inside the nanocarriers was dependent on their composition and affected their properties. In addition, the systems did not induce cytotoxic effects on epithelial cells, as MTT assay indicated. Permeability studies of rhodamine-loaded nanoparticles demonstrated 2–2.5-fold intestinal permeability enhancement of the chromophore when using liposomes compared to the free molecule. Among these systems, the liposomes containing cationic lipids exhibited the highest percentage of transport across the epithelial monolayer. Conclusively, the composition and resultant properties of the liposomes are determinant for DMC incorporation and their in vitro toxicity and permeability. The herein developed nanosystems are promising for further application, due to their biocompatibility and permeability. © 2022