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Journal article

Enzymatic degradation of polymer covered SOPC-liposomes in relation to drug delivery

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Department of Chemistry, Technical University of Denmark1

Polyethylenoxide (PEG) covered liposomes are used as lipid-based drug-delivery systems. In comparison to conventional liposomes the polymer-covered liposomes display a long circulation half-life in the blood stream. We investigate the influence of polyethyleneoxide-distearoylphosphatidylethanolamine (DSPE-PEG$-750$/) lipopolymer concentration on phospholipase A$-2$/ (PLA$-2$/) catalyzed hydrolysis of liposomes composed of stearoyloleoylphosphatidylcholine (SOPC).

The characteristic PLA$-2$/ lag-time was determined by fluorescence and the degree of lipid hydrolysis was followed by HPLC analysis. Particle size and zeta-potential were measured as a function of DSPE-PEG$-750$/ lipopolymer concentration. A significant decrease in the lag-time, and hence an increase in enzyme activity, was observed with increasing concentrations of the anionic DSPE-PEG$-750$/ lipopolymer lipids.

The observed decrease in lag-time might be related to changes in the surface potential and the PLA$-2$/ lipid membrane affinity.

Language: English
Year: 2001
Pages: 303-311
ISSN: 18733727 and 00018686
Types: Journal article
DOI: 10.1016/s0001-8686(00)00058-0
ORCIDs: 0000-0002-6621-3784 and 0000-0002-4258-8960

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