A new crown ether as vesicular carrier for 5-fluoruracil: Synthesis, characterization and drug delivery evaluation

Niosomes have shown promise as cheap and chemically stable drug delivery systems. In this paper a novel crown ether amphiphile, 1,16-hexadecanoyl-bis-(2-aminomethyl)-18-crown-6 (Bola A-16), has been synthesized with the aim of developing a long time stable controlled release system. Niosomes have be...

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Bibliographic Details
Published in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2007-08, Vol.58 (2), p.197-202
Main Authors: Muzzalupo, Rita, Nicoletta, Fiore Pasquale, Trombino, Sonia, Cassano, Roberta, Iemma, Francesca, Picci, Nevio
Format: Article
Language:English
Subjects:
5-Fluorouracil
Antimetabolites, Antineoplastic - administration & dosage
Crown ether
Crown Ethers - chemical synthesis
Crown Ethers - chemistry
Drug delivery
Drug Delivery Systems
Fluorouracil - administration & dosage
In vitro delivery
Liposomes
Niosomes
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Summary:Niosomes have shown promise as cheap and chemically stable drug delivery systems. In this paper a novel crown ether amphiphile, 1,16-hexadecanoyl-bis-(2-aminomethyl)-18-crown-6 (Bola A-16), has been synthesized with the aim of developing a long time stable controlled release system. Niosomes have been prepared with different molar ratios of amphiphile and cholesterol and their morphological properties have been determined by quasi-elastic light scattering and transmission electron microscopy. The composition of niosomes affects the entrapment efficiency and the release rate of 5-fluorouracil, a well-known antineoplastic molecule. In addition, other two known azacrown ether amphiphiles (4,7,10,13-pentaoxa-16-aza-cyclooctadecane)-hexadecanedioc acid diamide (Bola D-16) and α,ω-(4,7,10,13-pentaoxa-16-aza-cyclooctadecane)-hexadecane (Bola C-16), have been synthesized and the obtained vesicles have been characterized for comparison. Furthermore, the release profile of 5-fluorouracil in vitro, from these niosomes, has been studied over a period of 6 h in order to simulate a hematic adsorption.
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2007.03.010