A new crown ether as vesicular carrier for 5-fluoruracil: synthesis, characterization and drug delivery evaluation |
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Authors: | Muzzalupo Rita Nicoletta Fiore Pasquale Trombino Sonia Cassano Roberta Iemma Francesca Picci Nevio |
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Institution: | aDipartimento di Scienze Farmaceutiche, Università della Calabria, Via P. Bucci, Ed. Polifunzionale, Arcavacata di Rende, 87030 Rende, CS, Italy |
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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 ,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. |
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Keywords: | Niosomes Crown ether Drug delivery 5-Fluorouracil In vitro delivery |
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