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KMID : 0369820080380030163
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Jorunal of Korean Pharmaceutical Sciences
2008 Volume.38 No. 3 p.163 ~ p.169
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Intracellular delivery and anti-tumor activity of polyethyleneglycol liposomes containing cationic lipid
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Jung Soon-Hwa
Kim Sung-Kyu
Jung Suk-Hyun
Seong Ha-Soo
Cho Sun-Hang
Shin Byung-Cheol
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Abstract
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Liposomes are spherical vesicles composed of lipid bilayer membranes. However, the conventional liposomes have been found to be plagued by rapid opsonization and taken up by the reticuloendothelial system (RES), resulting in shortened circulation time and limited intracellular uptake to target cell. In this study, polyethyleneglycol-cationic liposomes (PCL) containing cationic lipid and DSPE-mPEG were prepared by thin film cast-hydration method. The PEG liposomes had approximately of mean particle diameter and of zeta potential value. PCL had of mean particle diameter and of zeta potential value with a decrease of about 10 mV compared to the PEG liposomes. Loading of model drug, doxorubicin (DOX), in liposomes were carried out by using remote loading method and the loading efficiency of DOX in liposomes was about . Intracellular uptake and cytotoxicity of PCL were higher than that of PEG liposomes to murine B16F10 melanoma cells. In addition, anti-tumor activity of PCL was similar to that of PEG liposomes on growth of A549 human lung carcinoma in BALB/c mice. Consequently, PCL modified with cationic lipid may be applicable as anticancer drug carriers that can increase intracellular uptake and therapeutic efficacy.
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KEYWORD
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Liposome, Polyethyleneglycol, Cationic, lipid, Intracellular, Anti-tumor
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