PUB029 Eudragit Coated Chitosan Nanoparticles for Colon Cancer

Abstract

Cancer is the second leading cause of death worldwide, the deaths projected to continue rising, with an estimated 12 million deaths in 2030. Aim of the present investigation is to prepare and compare the uncoated (U-CH NP) and eudragit S 100 coated (E-U-CH NP) chitosan nanoparticles encapsulating a caspase 3 activator (UCN 01), by ionic gelation method. The prepared formulations were studied for various parameters like particles size, zeta potential, transmission electron microscopy, atomic force microscopy, in vitro release study, ex vivo study using Caco 2 colon cancer cell line and in vivo studies. Developed formulation showed particle size of 168 ± 3.7 nm and 265 ± 4.1 nm for U-CH NP and E-U-CH NP, respectively. The cytotoxicity of prepared formulations was performed on Caco2 cell line by MTT assay. U-CH NP showed enhanced cytotoxicity as compared to blank (without drug) formulation. There was an increase in caspase 3 activity of U-CH NP as compared to UCN 01 alone. The E-U-CH NP showed better in vitro release than uncoated formulation in SCF (pH 6.8) than in SGF (pH 1.2) due to eudragit S 100 coating. E-U-CH NP showed better tumor regression ability than U-CH NP. The results obtained demonstrated that E-U-CH NP has continuous release profile of UCN 01 and comprehensive residence time. Thus, it is better acceptable than free UCN 01 and may be a potential delivery system for the targeting and treatment of colon cancer.