PMID: 2110480Apr 30, 1990Paper

Mechanisms of delivery of liposome-encapsulated cytosine arabinoside to CV-1 cells in vitro. Fluorescence-microscopic and cytotoxicity studies

Biochimica Et Biophysica Acta
P M Brown, J R Silvius

Abstract

Fluorescence microscopy and assays of the cytotoxicity of liposome-encapsulated cytosine arabinoside (araC) have been used to examine the interactions of CV-1 cells with pH-sensitive liposomes, combining phosphatidylethanolamine (PE) with oleic acid or with double-chain protonatable amphiphiles, and with pH-insensitive liposomes combining phosphatidylcholine (PC) and phosphatidylglycerol (PG). Fluorescence-microscopic observations indicate that double-chain protonatable amphiphiles remain tightly associated with pH-sensitive liposomes during incubations with CV-1 cell monolayers, and that cellular uptake of liposomes is strongly promoted by transferrin coupled to the liposome surface. Liposome-encapsulated araC showed much greater cytotoxicity toward CV-1 cells than did the free drug at equivalent concentrations under the same conditions. The cytotoxicity of encapsulated araC was strongly enhanced by liposome-conjugated transferrin and was maximal using pH-sensitive liposomes combining PE with the double-chain protonatable amphiphile N-(N'-oleoyl-2-aminopalmitoyl)serine. However, the drug was also markedly more cytotoxic when encapsulated in other types of transferrin-conjugated liposomes, including pH-insensitive PC/PG/cholest...Continue Reading

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Citations

Apr 7, 2004·Advanced Drug Delivery Reviews·Marie-Andrée Yessine, Jean-Christophe Leroux
Aug 15, 2002·International Journal of Pharmaceutics·Emmanuelle RouxJean-Christophe Leroux
May 20, 1999·Molecular Membrane Biology·N MaurerP R Cullis
May 19, 2009·International Journal of Pharmaceutics·Pierre Simard, Jean-Christophe Leroux
Nov 1, 1995·Biochimica Et Biophysica Acta·S Shahinian, J R Silvius
Nov 18, 2000·Progress in Lipid Research·D C DrummondJ Leroux
Aug 14, 1992·Biochimica Et Biophysica Acta·D C Litzinger, L Huang
May 19, 2010·Molecular Pharmaceutics·Pierre Simard, Jean-Christophe Leroux

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