Folate Receptor Mediated Targeting

The folate receptor is known to be over expressed in a large fraction of human tumors, but it is only minimally distributed in normal tissues. Therefore, the folate receptor has also been used as a tumortargeting ligand for several drug delivery systems. Recently, Hofland et al. synthesized folate-PEG-lipid derivatives to prepare folate-modified cationic liposomes.99 After an intravenous injection of folate-conjugated liposome complex, gene expression in the tumors was not changed, whereas gene expression in the lung was reduced as compared with the conventional complex. However, after intraperitoneal injection in a murine disseminated peritoneal tumor model, folate-conjugated liposome complex formulations produced approximately a 10-fold increase in tumor-associated gene expression compared with conventional complex.100

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