PMID: 3756214Oct 1, 1986Paper

Effect of phospholipid structure on stability and survival times of liposomes in circulation

Biochimica Et Biophysica Acta
K AgarwalC M Gupta

Abstract

The phosphatidylcholine (PC) component of liposomes was structurally modified by replacing its C-1, or both C-1 and C-2, ester linkage(s) with an ether and/or carbamyl bond(s) or by changing its steric configuration. Small unilamellar liposomes were formed from PC, traces of the corresponding 14C-labeled PC and cholesterol in the presence of 6-carboxyfluorescein (02.M) by sonication, and purified by centrifugation. These liposomes were administered intravenously to rats, and their stability in blood as well as the rate of their clearance from the circulation were determined. Stability and survival times of liposomes were markedly increased by modifying both the C-1 and the C-2 ester linkages in PC. A similar but quantitatively smaller effect was observed when only the C-1 ester linkage was modified. However, the stability remained unaffected by changing the steric configuration of PC, but this modification influenced the clearance rate of liposomes from the circulation. These results demonstrate that both stability in blood and the clearance rate from circulation can be modulated by structurally modifying the ester linkages in the phospholipid component of liposomes.

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Citations

Mar 24, 1993·Molecular and Cellular Biochemistry·T Hernández-CasellesJ C Gómez-Fernández
Dec 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·J T DerksenG L Scherphof
Oct 13, 2001·The Journal of Biological Chemistry·C M CrowderD F Covey
Feb 6, 2017·The AAPS Journal·Mamta KapoorKatherine M Tyner
Jul 10, 1989·Biochimica Et Biophysica Acta·V Bhakuni, C M Gupta
May 26, 2007·Pharmacology & Therapeutics·Gustav AkkSteven Mennerick

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