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Publication . Article . 1995

Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines

Marina Soncin; Laura Polo; Elena Reddi; Giulio Jori; M. E. Kenney; Gongzhen Cheng; Michael A. J. Rodgers;
Open Access
Published: 01 Apr 1995 Journal: British Journal of Cancer, volume 71, pages 727-732 (issn: 0007-0920, eissn: 1532-1827, Copyright policy )
Publisher: Springer Science and Business Media LLC
Abstract

Four Ge(IV)-octabutoxy-phthalocyanines (GePcs) bearing two alkyl-type axial ligands were assayed for their pharmacokinetic properties and phototherapeutic efficiency in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarcoma. The GePcs were i.v. injected at a dose of 0.35 mumol kg-1 body weight after incorporation into either Cremophor emulsions or small unilamellar liposomes of dipalmitoyl-phosphatidylcholine (DPPC). Both the nature of the delivery system and the chemical structure of the phthalocyanine were found to affect the behaviour of the GePcs in vivo. Thus, Cremophor-administered GePcs invariably yielded a more prolonged serum retention and a larger association with low-density lipoproteins (LDLs) as compared with the corresponding liposome-delivered phthalocyanines. This led to a greater efficiency and selectivity of tumour targeting. These effects were more pronounced for those GePcs having relatively long alkyl chains (hexyl to decyl) in the axial ligands. Maximal tumour accumulation (0.67 nmol per g of tissue) was found for Ge-Pc(hexyl)2 at 24 h after injection. Consistently, the Ge-Pc(hexyl)2, administered via Cremophor, showed the highest phototherapeutic activity towards MS-2 fibrosarcoma.

Subjects by Vocabulary

Microsoft Academic Graph classification: Dosage form Nuclear chemistry Phthalocyanine chemistry.chemical_compound chemistry In vivo Drug carrier Fibrosarcoma medicine.disease medicine Liposome Pharmacokinetics Photosensitizer Immunology

Subjects

Cancer Research, Oncology, Research Article

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