Liposomal encapsulation enhances the antitumour efficacy of the vascular disrupting agent ZD6126 in murine B16.F10 melanoma

Autor: Marcel H.A.M. Fens, F R Westwood, Raymond M. Schiffelers, K J Hill, Anderson J. Ryan, David C. Blakey, J Issa, Gert Storm, Susan Ashton
Jazyk: angličtina
Rok vydání: 2008
Předmět:
Zdroj: British Journal of Cancer, 99, 1256. Nature Publishing Group
British Journal of Cancer
ISSN: 1532-1827
0007-0920
Popis: Vascular disrupting agents (VDAs) are able to affect selectively tumour endothelial cell morphology resulting in vessel occlusion and widespread tumour cell necrosis. However, single-agent antitumour activity of VDAs is typically limited, as tumour regrowth occurs rapidly following drug treatment. To improve the therapeutic effectiveness of VDAs, we investigated liposomal targeting using ZD6126 as a model VDA. ZD6126 is a phosphate-prodrug of the tubulin-binding vascular disrupting agent ZD6126 phenol. ZD6126 was encapsulated into long circulating PEG-liposomes for passive targeting and PEG-liposomes conjugated with peptide ligands containing the RGD-motif for active targeting to alpha(v)-integrins on tumour endothelial cells. ZD6126 could be stably encapsulated, and liposomes displayed minimal leakage in vitro (
Databáze: OpenAIRE