Si(IV)-methoxyethylene-glycol-naphthalocyanine: synthesis and pharmacokinetic and photosensitizing properties in different tumour models.

Abstract

A Si(IV)-naphthalocyanine bearing two methoxyethylenglycol axial ligands to the centrally coordinated metal ion (SiNc) was prepared by chemical synthesis and assayed for the phototherapeutic activity after administration in a Cremophor formulation to C57BI/6 mice bearing a subcutaneously transplanted Lewis lung carcinoma or B16 pigmented melanoma. Pharmacokinetic studies indicate that the maximal accumulation in the tumour occurs at 24 h after intraperitoneal injection of 0.5 mg kg-1 of SiNc, although the naphthalocyanine concentration in the Lewis lung carcinoma (0.70 microgram g-1) is significantly larger than that in the B16 pigmented melanoma (0.15 microgram g-1). This results in a higher selectivity of tumour targeting in the case of the lung carcinoma. Photodynamic therapy (782 nm, 370 mW cm-2, 360 J cm-2) at 24 h after SiNc injection causes an efficient tumour response for Lewis lung carcinoma (50% lower tumour diameter on day 19 post-treatment as compared to untreated controls) while the pigmented melanoma shows only a minor response regarding the rate of tumour growth.

• Authors: V Mantareva, M Shopova, G Spassova, D Wöhrle, S Muller, G Jori, F Ricchelli
• Journal: Journal of photochemistry and photobiology. B, Biology (J Photochem Photobiol B) Vol. 40 Issue 3 Pg. 258-62 (Oct 1997) ISSN: 1011-1344 [Print] Switzerland
• PMID: 9372614 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Metalloporphyrins
• Porphyrins
• Radiation-Sensitizing Agents
• 2,3-naphthalocyanine

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, pharmacokinetics, therapeutic use)
• Disease Models, Animal
• Lung Neoplasms (therapy)
• Male
• Melanoma, Experimental (therapy)
• Metalloporphyrins (chemical synthesis, pharmacokinetics, therapeutic use)
• Mice
• Mice, Inbred C57BL
• Photochemotherapy
• Porphyrins (chemical synthesis, pharmacokinetics, therapeutic use)
• Radiation-Sensitizing Agents (chemical synthesis, pharmacokinetics, therapeutic use)