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Titolo:
In vitro release of 5-fluorouracil with cyclic core dendritic polymer
Autore:
Zhuo, RX; Du, B; Lu, ZR;
Indirizzi:
Wuhananniv, Dept Chem, Lab Biomed Polymer Mat State Educ Commiss China, Wuh Wuhan Univ Wuhan Peoples R China 430072 at State Educ Commiss China, Wuh
Titolo Testata:
JOURNAL OF CONTROLLED RELEASE
fascicolo: 3, volume: 57, anno: 1999,
pagine: 249 - 257
SICI:
0168-3659(19990222)57:3<249:IVRO5W>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
STARBURST DENDRIMERS; POLYAMIDOAMINE DENDRIMERS; ANTITUMOR-ACTIVITY; MACROMOLECULES;
Keywords:
dendrimer; 1,4,7,10-tetraazacyclododecane; Michael addition; 5-fluorouracil; release;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
16
Recensione:
Indirizzi per estratti:
Indirizzo: Zhuo, RX Wuhananniv, Dept Chem, Lab Biomed Polymer Mat State Educ Commiss China, Wuh Wuhan Univ Wuhan Peoples R China 430072 Educ Commiss China, Wuh
Citazione:
R.X. Zhuo et al., "In vitro release of 5-fluorouracil with cyclic core dendritic polymer", J CONTR REL, 57(3), 1999, pp. 249-257

Abstract

This paper describes the first synthesis of a series of dendritic polymerswith a care of 1,4,7,10-tetraazacyclododecane. This core was allowed to react with methyl acrylate through a Michael addition and was then amidated with ethylenediamine. Repeating the two steps led to controlled molecular weight increasing and branching on the molecular level and produced four direction poly(amide-amine) dendrimers. We successfully synthesized dendrimers from generation 0.5 to generation 5.5. Each generation was analyzed by Fourier- transform infrared (FT-IR) spectroscopy, H-1 NMR and elemental analysis. Titrimetry was also used to determine the number of -NH2 of each full generation (2.0, 3.0, 4.0, 5.0). SEC (size exclusion chromatography) was performed to test the purity of G-3.0, G-4.0 and G-5.0. Parts of the outer layer -NH2 groups of the dendrimers generation 4 and generation 5 were acylatedby acetic anhydride. The solubility in water of the dendrimer was thus greatly enhanced. The acetylated dendrimers were then reacted with 1-bromoacetyl-5-fluorouracil to form dendrimer-5FU conjugates. Hydrolysis of the conjugates in a phosphate buffer solution (pH 7.4) at 37 degrees C win release free 5FU. Different generation of dendrimer-5FU conjugates exert marking influence on the amount of 5FU released. The dendritic polymer seems to be a promising carrier for the controlled release of antitumor drugs. (C) 1999 Published by Elsevier Science B.V.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/07/20 alle ore 05:34:07