Innovative niosomes made up of alpha,omega-hexadecylbis-(1-aza-18-crown-6) (bola), Span 80 (R) 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 procedure, showed mean sizes of similar to 200 nm and a loading capacity of similar to 40% with respect to the amount of 5-FU added during the preparation. Similar findings were achieved with PEG-coated bola-niosomes (bola, Span 80 (R), 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.
Novel PEG-coated Niosomes Based on Bola-surfactant as Drug Carriers for 5-Fluorouracil
COSCO D;Paolino D;CITRARO R;FRESTA M
2009-01-01
Abstract
Innovative niosomes made up of alpha,omega-hexadecylbis-(1-aza-18-crown-6) (bola), Span 80 (R) 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 procedure, showed mean sizes of similar to 200 nm and a loading capacity of similar to 40% with respect to the amount of 5-FU added during the preparation. Similar findings were achieved with PEG-coated bola-niosomes (bola, Span 80 (R), 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
