Enhanced efficacy of folate-incorporated cholesteryl doxorubicin liposome in folate receptor abundant cancer cell

Doxorubicin (Dox) is an anthracycline antitumor agent with the disadvantages of cumulative cardiotoxicity, short retention time, and rapid excretion. A liposomal formulation of cholesteryl Dox (LLD), developed to overcome the side effects of Dox, is characterized by a particle size and zeta potential (ZP) of 93.9 ± 1.4 nm and −12.7 ± 0.7 mV, respectively, as well as stability under extracellular pH conditions. In this study, a folate-incorporated liposomal formulation of cholesteryl Dox (FLLD) was prepared to target the folic acid receptor (FR). FLLD showed considerable enhancement of cytotoxicity in KB cells (FR positive) by increasing cell association. Intravenous FLLD suppressed KB tumors to a greater extent than Dox without adverse side effects on other organs, such as the heart and kidney. Moreover, the biodistribution experiment showed that folate incorporation improved the targeting effect compared with LLD. FLLD is a promising anticancer drug that could be used to target cancer cells expressing high FR.