title: A new crown ether as vesicular carrier for 5-fluoruracil: synthesis, characterization and drug delivery evaluation.
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.
authors: Dipartimento di Scienze Farmaceutiche, Università della Calabria, Via P. Bucci, Ed. Polifunzionale, Arcavacata di Rende, 87030 Rende, CS, Italy. rita.muzzalupo@unical.it
authors: Rita
authors: R
authors: Muzzalupo
authors: Fiore Pasquale
authors: FP
authors: Nicoletta
authors: Sonia
authors: S
authors: Trombino
authors: Roberta
authors: R
authors: Cassano
authors: Francesca
authors: F
authors: Iemma
authors: Nevio
authors: N
authors: Picci
mesh_terms: D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage*; D043844:Crown Ethers / Q000138:chemical synthesis / Q000737:chemistry; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000008:administration & dosage*; D008081:Liposomes
chemical_list: D000964:Antimetabolites, Antineoplastic; D043844:Crown Ethers; D008081:Liposomes; D005472:Fluorouracil