C. Fabris et al., TUMOR-LOCALIZING AND TUMOR-PHOTOSENSITIZING PROPERTIES OF ZINC(II)-OCTAPENTYL-PHTHALOCYANINE, Journal of photochemistry and photobiology.B, Biology, 39(3), 1997, pp. 279-284
Zn(II)-octapentyl-phthalocyanine (ZnOPPc), incorporated into a Cremoph
or oil emulsion, was found to be a highly selective tumour-targeting a
gent (50-fold larger concentration in the tumour than in the peritumor
al tissue) when injected at a dose of 1.46 mu mol (kg body weight)(-1)
in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarc
oma. The pharmacokinetic properties of this phthalocyanine were closel
y similar to those found for the analogous octadecyl derivative, where
as the unsubstituted Zn(II)-phthalocyanine showed a lower efficiency a
nd selectivity of tumour targeting than the octaalkyl-substituted phth
alocyanines. Irradiation of the ZnOPPc-loaded tumour with 620-700 nm l
ight 24 h after injection caused a significant delay of tumour growth
with a gradual shrinkage of the neoplastic mass; the damage involved i
mportant contributions from both random necrosis and apoptosis of mali
gnant cells. (C) 1997 Elsevier Science S.A.