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Titolo:
Characterization, stability and in-vivo distribution of asialofetuin glycopeptide incorporating DSPC/CHOL liposomes prepared by mild cholate incubation
Autore:
Kallinteri, P; Liao, WY; Antimisiaris, SG; Hwang, KHJ;
Indirizzi:
Univ Patras, Dept Pharm, Patras 26500, Greece Univ Patras Patras Greece 26500 Patras, Dept Pharm, Patras 26500, Greece Univ So Calif, Sch Pharm, Los Angeles, CA 90033 USA Univ So Calif Los Angeles CA USA 90033 h Pharm, Los Angeles, CA 90033 USA
Titolo Testata:
JOURNAL OF DRUG TARGETING
fascicolo: 2, volume: 9, anno: 2001,
pagine: 155 - 168
SICI:
1061-186X(2001)9:2<155:CSAIDO>2.0.ZU;2-1
Fonte:
ISI
Lingua:
ENG
Soggetto:
SPHINGOMYELIN-CHOLESTEROL LIPOSOMES; HEPATIC ASIALOGLYCOPROTEIN RECEPTOR; RABBIT HEPATOCYTES; LABELED LIPOSOMES; LIPID VESICLES; HIGH-AFFINITY; BINDING; DEGRADATION; MOUSE; GAMMA;
Keywords:
fetuin; liposome; drug targeting; glycolipid; asialoglycoprotein receptor;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
38
Recensione:
Indirizzi per estratti:
Indirizzo: Antimisiaris, SG Univ Patras, Dept Pharm, Patras 26500, Greece Univ Patras Patras Greece 26500 m, Patras 26500, Greece
Citazione:
P. Kallinteri et al., "Characterization, stability and in-vivo distribution of asialofetuin glycopeptide incorporating DSPC/CHOL liposomes prepared by mild cholate incubation", J DRUG TAR, 9(2), 2001, pp. 155-168

Abstract

In this study, a small triantennary asialoglycopeptide of fetuin (A-F-2) was used as a ligand to direct liposomes to hepatocytes. A-F2 was cleaved from asialofetuin, purified, conjugated with fatty acids and incorporated into pre-formed sonicated DSPC/Chol (2:1) liposomes. A mild cholate incubationmethod for incorporating the A-F2 ligand on pre-formed vesicles was used. In preliminary in vivo experiments In-111(3+) encapsulated in A-F-2/palmityl liposomes was seen to accumulate in the liver of mice significantly faster than when encapsulated in non-ligand bearing liposomes of the same lipid composition (studied before), justifying further investigation of this system. The presence of the A-F-2/fatty acid conjugate in a functional form on the vesicle surface was confirmed by their reversible agglutination in the presence of Ricinus communis agglutinin (RCA(120)). Effects of ligand incorporation on the vesicle size distribution, z-potential, membrane integrity and stability were monitored. The results demonstrate that highest ligand incorporation was achieved when liposomes and ligand were co-incubated in the presence of 1mM sodium cholate. Incorporation increased with the length of the fatty acid used for A-F2 conjugation. Ligand-bearing liposomes were demonstrated to be smaller in diameter (about 30%) with a more positive z-potential in comparison to control vesicles while ligand incorporation did not influence the liposome membrane integrity. The size of the ligand-incorporating vesicles was maintained after 24 hours of incubation in isotonic buffer, proving that the vesicles do not aggregate. Although the preliminary biodistribution results may suggest that ligand bearing liposomes are accumulating in the liver, further cell culture in vivo distribution and especially liver fractionation studies are required in order to clarify the intrahepatic localization of these liposomes and the ability to target liver hepatocytes in vivo.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 12:17:05