Tumour-localizing and tumour-photosensitizing properties of zinc(II)-octapentyl-phthalocyanine.
Zn(II)-octapentyl-phthalocyanine (ZnOPPc), incorporated into a Cremophor oil emulsion, was found to be a highly selective tumour-targeting agent (50-fold larger concentration in the tumour than in the peritumoral tissue) when injected at a dose of 1.46 mumol (kg body weight)-1 in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarcoma. The pharmacokinetic properties of this phthalocyanine were closely similar to those found for the analogous octadecyl derivative, whereas the unsubstituted Zn(II)-phthalocyanine showed a lower efficiency and selectivity of tumour targeting than the octaalkyl-substituted phthalocyanines. Irradiation of the ZnOPPc-loaded tumour with 620-700 nm light 24 h after injection caused a significant delay of tumour growth with a gradual shrinkage of the neoplastic mass; the damage involved important contributions from both random necrosis and apoptosis of malignant cells.
Fabris
C
C
Department of Biology, University of Padova, Italy.
Ometto
C
C
Milanesi
C
C
Jori
G
G
Cook
M J
MJ
Russell
D A
DA
D000818:Animals; D017209:Apoptosis; D004655:Emulsions; D005260:Female; D007211:Indoles / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D051379:Mice; D008807:Mice, Inbred BALB C; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000378:metabolism / Q000628:therapy*; D009942:Organometallic Compounds / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D010778:Photochemotherapy; D011092:Polyethylene Glycols; D011838:Radiation-Sensitizing Agents / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D004655:Emulsions; D007211:Indoles; D009942:Organometallic Compounds; D011838:Radiation-Sensitizing Agents; C061188:zinc 1,4,8,11,15,18,22,25-octa-n-butoxyphthalocyanine; C022131:cremophor; D011092:Polyethylene Glycols