Monomeric pheophorbide(a)-containing poly(ethyleneglycol-b-epsilon-caprolactone) micelles for photodynamic therapy.

Incorporation of unaggregated monomeric molecules of pheophorbide(a) into micelles of poly(ethyleneoxide-b-epsilon-caprolactone) has been characterized by fluorescence spectroscopy, dynamic light scattering, transmission electron microscopy and asymmetric flow field flow fractionation. It was shown that the method used leads to 20 nm micelles, corresponding to approximately 200 molecules of polymer and 4 molecules of monomeric pheophorbide(a) per nano-object which was able to generate (1)O(2) in the medium. They have been used thereafter as nanocarriers for photosensitizers in photodynamic therapy against cancer cells. The encapsulation of photosensitizer has been verified and in vitro tests on human cancerous cells have revealed a ca. 2-fold enhanced photocytotoxicity and cellular uptake compared to free pheophorbide(a).