In Vivo and In Vitro Photodynamic Studies with Benzochlorin Iminium Salts Delivered by a Lipid Emulsion

In Vivo and In Vitro Photodynamic Studies with Benzochlorin Iminium Salts Delivered by a Lipid Emulsion

Benzochlorin iminium salts (Bis) are hydrophobic photosensitizers based on an octaethylbenzochlorin nucleus that absorb in the near‐IR region of the visible spectrum. In these studies the photodynamic activities of the zinc, copper and metal‐free BI derivatives were compared in vivo in C3H‐HeJ mice...

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Bibliographic Details
Published in:Photochemistry and photobiology Vol. 68; no. 4; pp. 561 - 568
Main Authors: Garbo, G. M., Fingar, V. H., Wieman, T. J., III, E. B. Noakes, Haydon, P. S., Cerrito, P. B., Kessel, D. H., Morgan, A. R.
Format: Journal Article
Language:English
Published: Oxford, UK Blackwell Publishing Ltd 01-10-1998
Subjects:
Adenocarcinoma - drug therapy
Animals
Cell Survival - drug effects
Cell Survival - radiation effects
Deuteroporphyrins - therapeutic use
Deuteroporphyrins - toxicity
Drug Carriers
Emulsions
Female
Fibrosarcoma
Imines - therapeutic use
Imines - toxicity
Leukemia L1210
Light
Mammary Neoplasms, Experimental - drug therapy
Mice
Mice, Inbred C3H
Neoplasms, Radiation-Induced
Photochemotherapy
Photosensitizing Agents - therapeutic use
Photosensitizing Agents - toxicity
Tumor Cells, Cultured
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Summary:Benzochlorin iminium salts (Bis) are hydrophobic photosensitizers based on an octaethylbenzochlorin nucleus that absorb in the near‐IR region of the visible spectrum. In these studies the photodynamic activities of the zinc, copper and metal‐free BI derivatives were compared in vivo in C3H‐HeJ mice bearing a mammary adenocarcinoma tumor line. In vitro studies were also performed with the radiation‐induced fibrosarcoma tumor line. An argon‐pumped Ti‐sapphire laser tuned to deliver light between 710 and 800 nm or an Oriel arc‐lamp filtered to deliver broadband light above 590 nm were used as light source. A lipid emulsion was used as the delivery system for sensitizers in all studies. A pronounced solvent dependence was observed for the Q band for each of all iminium salts examined. As an example, the metal‐free (BI) derivative had an absorption maximum at 798 nm in dichloromethane and at 727 nm in serum. The action spectra showed a greater PDT response at blue‐shifted wavelengths for each of the three iminium salts both in vivo and in vitro. Among the three derivatives, the zinc analog (ZnBI) produced the greatest tumor regression at the low drug/light dose of 0.7 (μ mole/kg and 200 J/cm2. These results indicate that iminium salts have characteristics that may make them promising third‐generation photosensitizers.
Bibliography:ArticleID:PHP561
istex:51937D6BFB1072BD8F7DA7A79C6795CFE6319AB7
ark:/67375/WNG-T9FNT630-X
ISSN:0031-8655
1751-1097
DOI:10.1111/j.1751-1097.1998.tb02514.x