Folate-decorated Polysaccharide-doxorubicin Polymer: Synthesis, Characterization, and Activity in HeLa Cells

In order to develop the application of the natural polysaccharide lentinan (LNT) and decrease the side effects of doxorubicin, we successfully synthesized a novel folate-modified maleilated lentinan-doxorubicin (FA-M.LNT-DOX) polymer and used it for tumor-targeted drug delivery. The release efficiency and cytotoxicity of the prodrugs were evaluated in vitro. Although DOX release from FA-M.LNT-DOX was quite slow in a neutral buffer, it was particularly fast in an acidic solution with a pH of 5.0. Compared with DOX, FA-M.LNT-DOX showed higher cytotoxicity in HeLa cells and significantly lower cytotoxicity in normal cells. These results suggested that FA-M.LNT-DOX could be considered as a potential drug delivery candidate for folate receptor-positive cancer therapy.