A new crown ether as vesicular carrier for 5-fluoruracil: synthesis, characterization and drug delivery evaluation
Rita Muzzalupo1, Fiore Pasquale Nicoletta, Sonia Trombino
1Dipartimento di Scienze Farmaceutiche, Università della Calabria, Via P. Bucci, Ed. Polifunzionale, Arcavacata di Rende, 87030 Rende, CS, Italy. rita.muzzalupo@unical.it
Abstract:
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 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 6h in order to simulate a hematic adsorption.
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