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 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.
Muzzalupo
Rita
R
Dipartimento di Scienze Farmaceutiche, Università della Calabria, Via P. Bucci, Ed. Polifunzionale, Arcavacata di Rende, 87030 Rende, CS, Italy. rita.muzzalupo@unical.it
Nicoletta
Fiore Pasquale
FP
Trombino
Sonia
S
Cassano
Roberta
R
Iemma
Francesca
F
Picci
Nevio
N
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
D000964:Antimetabolites, Antineoplastic; D043844:Crown Ethers; D008081:Liposomes; D005472:Fluorouracil