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

被引:45
作者
Muzzalupo, Rita [1 ]
Nicoletta, Fiore Pasquale [1 ]
Trombino, Sonia [1 ]
Cassano, Roberta [1 ]
Iemma, Francesca [1 ]
Picci, Nevio [1 ]
机构
[1] Univ Calabria, Dipartimento Sci Farmaceut, I-87030 Arcavacata Di Rende, Italy
关键词
niosomes; crown ether; drug delivery; 5-fluorouracil; in vitro delivery;
D O I
10.1016/j.colsurfb.2007.03.010
中图分类号
Q6 [生物物理学];
学科分类号
071011 ;
摘要
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 (4,710.13-pentaoxa-16-aza-cyclooctadecane)-hexadecanedioc acid diamide (Bola D-16) and alpha,omega-(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. (C) 2007 Elsevier B.V. All rights reserved.
引用
收藏
页码:197 / 202
页数:6
相关论文
共 40 条