Colon targeted releases and uptakes of paclitaxel loaded in modified porous starch

Abstract

Hyaluronic acid can modify porous starch through cross-linking and hydrogen bonding, effectively achieving a paclitaxel entrapment efficiency of ∼92 % and drug loading of ∼23 %. In this study, the pores and intergranular gaps of porous starch were filled with paclitaxel under solvent volatilization, and the enrichment process and its characteristics were recorded using a microscope. The paclitaxel-loaded particles were coated with chitosan-phytic acid to target the colon. In vivo imaging in mice showed that the capsule released paclitaxel in the colon rather than in the upper digestive tract, and the paclitaxel distribution in the main organs at 24 h was significantly lower than that of raw paclitaxel. Hyaluronic acid-modified porous starch can target cancer cells. Cell internalization of paclitaxel mediated by hyaluronic acid was approximately 1.97 times that of raw paclitaxel, higher than that of receptor-shielded cells and cells incubated with unmodified carriers, as evidenced by the accumulation of fluorescent paclitaxel in the nucleus and marked cell apoptosis. The hyaluronic acid-modified porous starch system is an effective method for the high-load and targeted release of hydrophobic anticancer drugs.

Keywords: Apoptosis; Colon targeted; Effective adsorption; Hyaluronic acid; Targeted uptake.