Tumour-localizing and tumour-photosensitizing properties of zinc(II)-octapentyl-phthalocyanine.

Abstract

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.

• Authors: C Fabris, C Ometto, C Milanesi, G Jori, M J Cook, D A Russell
• Journal: Journal of photochemistry and photobiology. B, Biology (J Photochem Photobiol B) Vol. 39 Issue 3 Pg. 279-84 (Jul 1997) ISSN: 1011-1344 [Print] Switzerland
• PMID: 9253202 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Emulsions
• Indoles
• Organometallic Compounds
• Radiation-Sensitizing Agents
• zinc 1,4,8,11,15,18,22,25-octa-n-butoxyphthalocyanine
• cremophor
• Polyethylene Glycols

Topics

• Animals
• Apoptosis
• Emulsions
• Female
• Indoles (chemistry, pharmacokinetics, therapeutic use)
• Mice
• Mice, Inbred BALB C
• Molecular Structure
• Neoplasms, Experimental (metabolism, therapy)
• Organometallic Compounds (chemistry, pharmacokinetics, therapeutic use)
• Photochemotherapy
• Polyethylene Glycols
• Radiation-Sensitizing Agents (chemistry, pharmacokinetics, therapeutic use)
• Structure-Activity Relationship