title: 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.affiliation: Institute of Organic Chemistry, Bulgarian Academy of Sciences, Sofia, Bulgaria.
authors.forename: V
authors.initials: V
authors.lastname: Mantareva
authors.forename: M
authors.initials: M
authors.lastname: Shopova
authors.forename: G
authors.initials: G
authors.lastname: Spassova
authors.forename: D
authors.initials: D
authors.lastname: Wöhrle
authors.forename: S
authors.initials: S
authors.lastname: Muller
authors.forename: G
authors.initials: G
authors.lastname: Jori
authors.forename: F
authors.initials: F
authors.lastname: Ricchelli
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use*; D004195:Disease Models, Animal; D008175:Lung Neoplasms / Q000628:therapy*; D008297:Male; D008546:Melanoma, Experimental / Q000628:therapy*; D008665:Metalloporphyrins / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use*; D051379:Mice; D008810:Mice, Inbred C57BL; D010778:Photochemotherapy; D011166:Porphyrins / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D008665:Metalloporphyrins; D011166:Porphyrins; D011838:Radiation-Sensitizing Agents; C076388:2,3-naphthalocyanine