Antiangiogenic
photodynamic therapy (
PDT) is a promising modality for
cancer treatment, since it causes efficient cutoff of
oxygen and nutrients to the
tumor cells and thus indirectly eradicates the
tumor cells. For the improvement of therapeutic efficacy of antiangiogenic
PDT by using a
photosensitizer benzoporphyrin derivative monoacid ring A (
BPD-MA) in a liposomal formulation, we endowed the
liposomes with an active-targeting probe,
Ala-Pro-Arg-Pro-Gly (APRPG), a
peptide specific for angiogenic endothelial cells. APRPG-PEG-modified liposomal
BPD-MA (APRPG-PEG-LipBPD-MA) accumulated in
tumor tissues to a similar extent as PEG-LipBPD-MA at 3-h postinjection. In contrast, APRPG-PEG-LipBPD-MA strongly suppressed
tumor growth by
PDT treatment, but PEG-LipBPD-MA did not. This finding suggests that antiangiogenic
PDT with targeted
liposomes is an efficient modality for
tumor treatment, whereas PEG-modified nontargeted
liposomes are not suitable as a carrier of
photosensitizers. The reason for the observed ineffectiveness of PEG-LipBPD-MA is as follows: In the case of
PDT, the amount of
photosensitizer bound to or taken up into the target cells during the time interval between injection of the agent and
laser irradiation is critical, rather than the total amount of
photosensitizer in
tumor tissue. Therefore, active-targeting technology is quite useful for antiangiogenic
PDT.