1983
DOI: 10.1016/0014-5793(83)80185-9
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Stability of liposomes in circulation is markedly enhanced by structural modification of their phospholipid component

Abstract: Replacement of the C-2 ester group in phosphatidylcholine by the carbamyloxy function rendered its liposomes completely stable and longer living in the circulation of rats. Drug delivery Modified liposomes Blood clearance

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Cited by 18 publications
(6 citation statements)
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“…The head-group modifications include introduction of ligands,5255 functional groups (such as malemide) for chemical conjugation of ligands (such as antibodies),56 and/or polymerizable moieties57 to produce stable liposomes. The carbonyl ester bonds of the glycerol backbone of PC (at both the sn-1 and sn-2 position) have been the choice for modifications with either ether58,59 or carbamyl esters,60–62 resulting in modulation of stability and in vivo circulation of these liposomes. The fatty acyl chain length and degree of unsaturation are important factors that govern bilayer packing properties of liposomes and contribute to the observed phase-transition (Tm) effect.…”
Section: Liposomes As Drug Carriersmentioning
confidence: 99%
“…The head-group modifications include introduction of ligands,5255 functional groups (such as malemide) for chemical conjugation of ligands (such as antibodies),56 and/or polymerizable moieties57 to produce stable liposomes. The carbonyl ester bonds of the glycerol backbone of PC (at both the sn-1 and sn-2 position) have been the choice for modifications with either ether58,59 or carbamyl esters,60–62 resulting in modulation of stability and in vivo circulation of these liposomes. The fatty acyl chain length and degree of unsaturation are important factors that govern bilayer packing properties of liposomes and contribute to the observed phase-transition (Tm) effect.…”
Section: Liposomes As Drug Carriersmentioning
confidence: 99%
“…The tetrapeptides I and II were synthesized by conventional methods and characterized by FAB/CAD mass spectrometry (unpublished). 6-CF (Eastman-Kodak) was used after purification as in [ 131. The radioactivity and 6-CF were measured as in [14].…”
Section: Methodsmentioning
confidence: 99%
“…Only the liposomes found in the top 3/4 of the supernatant were used. Free and liposomal 6-CF were separated by gel filtration [14]. The outer diameter of the liposomes, as measured by electron microscopy, was about 35-55 nm (mean size, -40 nm), which remained unaffected upon incorporating I (or II) in the liposomes bilayer.…”
Section: Liposomesmentioning
confidence: 99%
“…It was observed more than 10 years ago that blood plasma contained factors that were able to drastically enhance the rate at which encapsulated solutes were released from liposomes (ZBOROWSKI et al 1977) and that mainly high density lipoproteins were responsible for these liposome destabilizing effects . Also, the exploitation of phospholipid analogues, such as ether phospholipids, was shown to have a beneficial effect on plasma stability of liposomes (GUPTA et al 1981;BALI et al 1983;HERMETTER and PALTAUF 1983;AGARWAL et al 1986a,b). Incorporation of high proportions of cholesterol, for example, was shown to reduce the plasma-induced leakage of encapsulated solutes quite substantially (KIRBY et al 1980a,b;GREGORIADlS, 1980, 1981), as was the use of phospholipids with relatively high gel to liquid crystalline phase transition temperatures (SENIOR and GREGORIADIS 1982a;SCHERPHOF et al 1979).…”
Section: B Interactions With Body Fluidsmentioning
confidence: 99%