Characterization, Stability and In - Vivo Distribution of Asialofetuin Glycopeptide Incorporating DSPC/CHOL Liposomes Prepared by Mild Cholate Incubation

Kallinteri, Paraskevi and Liao, Wen-Yeh and Antimisiaris, Sophia G. and Hwang, Karl H. J. (2001) Characterization, Stability and In - Vivo Distribution of Asialofetuin Glycopeptide Incorporating DSPC/CHOL Liposomes Prepared by Mild Cholate Incubation. Journal of Drug Targeting, 9 (2). pp. 155-168. ISSN 1061-186X. (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided)

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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 incubation method 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.

Item Type: Article
Additional information: 459AY Times Cited:2 Cited References Count:38
Uncontrolled keywords: fetuin liposome drug targeting glycolipid asialoglycoprotein receptor sphingomyelin-cholesterol liposomes hepatic asialoglycoprotein receptor rabbit hepatocytes labeled liposomes lipid vesicles high-affinity binding degradation mouse gamma
Subjects: Q Science
R Medicine > RC Internal medicine > RC0254 Neoplasms. Tumors. Oncology (including Cancer)
Divisions: Faculties > Science Technology and Medical Studies > Medway School of Pharmacy
Depositing User: Paraskevi Kallinteri
Date Deposited: 27 May 2009 15:20
Last Modified: 08 Apr 2014 08:31
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