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Novel PEG-coated niosomes based on bola-surfactant as drug carriers for 5-fluorouracil

Cosco, D. and Paolino, D. and Muzzalupo, R. and Celia, C. and Citraro, R. and Caponio, D. and Picci, N. and Fresta, M. (2009) Novel PEG-coated niosomes based on bola-surfactant as drug carriers for 5-fluorouracil. Biomedical Microdevices, 11 (5). pp. 1115-1125.

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Abstract

Innovative niosomes made up of α,ω-hexadecyl-bis-(1-aza-18-crown-6) (bola), Span 80® and cholesterol (2:5:2 molar ratio) are proposed as suitable delivery systems for the administration of 5-fluorouracil (5-FU), an antitumoral compound largely used in the treatment of breast cancer. The bola-niosomes, after sonication proce-dure, showed mean sizes of ~200 nm and a loading capacity of ~40% with respect to the amount of 5-FU added during the preparation. Similar findings wereachieved with PEG-coated bola-niosomes (bola, Span 80®, cholesterol, DSPE-mPEG2000, 2:5:2:0.1 molar ratio respectively). 5-FU-loaded PEG-coated and uncoated bola-niosomes were tested on MCF-7 and T47D cells. Both bola-niosome formulations provided an increase in the cytotoxic effect with respect to the free drug. Confocal laser scanning microscopy studies were carried out to evaluate both the extent and the time-dependent bola-niosome-cell interaction. In vivo experiments on MCF-7 xenograft tumor SCID mice models showed a more effective antitumoral activity of the PEGylated niosomal 5-FU at a concentration ten times lower (8 mg/kg) than that of the free solution of the drug (80 mg/kg) after a treatment of 30 days.

Item Type:Article
Subjects:Biomedical Science > Nanotechnology for human health
ID Code:8001
Deposited By:CSMNT
Deposited On:26 Aug 2010 09:41
Last Modified:26 Aug 2010 09:41

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