Anticancer Drug-Phospholipid Conjugate for Enhancement of Intracellular Drug Delivery.

Tumor specific delivery of anti-cancer drugs is one of the major challenges faced by drug development processes. In this study, we prepared a doxorubicin (DOX)-conjugated liposome (DCL) by incorporating the newly synthesized DSPE-PEG2000-DOX (DPD) into liposomes as a lipid component and tested its anti-tumor activity in vivo. DPD was synthesized by coupling DOX to DSPE-PEG2000-COOH via amide linkage and the chemical structure of resulting DPD was confirmed by (1)H-NMR analysis. DCL having liposome size of 130 nm was prepared through thin film cast-hydration method. DCL was found to have significantly higher cellular uptake than conventional liposomes as confirmed by flow cytometry analysis. Anti-tumor activity of DCL against murine B16F10 melanoma tumor-bearing mice revealed that DCL inhibits tumor growth more efficiently than the conventional liposomes, presumably attributed to DOX mediated endocytosis process.