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KMID : 0369820080380010015
Jorunal of Korean Pharmaceutical Sciences
2008 Volume.38 No. 1 p.15 ~ p.21
Physical properties and intracellular uptake of polyethyleneglycol-incorporated cationic liposomes
Jung Soon-Hwa

Jung Suk-Hyun
Kim Sung-Kyu
Seong Ha-Soo
Cho Sun-Hang
Shin Byung-Cheol
Abstract
Liposomes as one of the efficient drug carriers have some shortcomings such as their short circulation time, fast clearance from human body by reticuloendothelial system (RES) and limited intracellular uptake to target cell. In this study, polyethylenglycol (PEG)-incorporated cationic liposomes were prepared by ionic complexation of positively charged liposomes with carboxylated polyethyleneglycol (mPEG-COOH). The cationic liposomes had approximately 98.6¡¾1.0nm of mean particle diameter and 42.8¡¾0.8nV of zeta potential value. The PEG-incorporated cationic liposomes had 110.1¡¾1.2nm of mean particle diameter with an increase of about 10 nm compared to the cationic liposomes. Zeta potential value of them was 12.9¡¾0.6nV indicating 30mV decrease of cationic charge compared to the cationic liposomes. The amount of PEG which was incorporated onto the cationic liposomes was assayed by using picrate assay method and the incorporation efficiency was 58.4¡¾1.1%. Loading efficiency of model drug, doxorubicin, into cationic liposomes or PEG-incorporated cationic liposomes was about 96.0¡¾0.7%. Results of intracellular uptake which were evaluated by flow cytometry analysis of doxorubicin loaded liposomes showed that intracellular uptake of PEG-incorporated cationic liposomes was higher than the cationic liposomes or DSPE-mPEG liposomes. In addition, cytotoxicity of PEG-incorporated cationic liposomes was comparable to cationic liposomes. Consequently, the PEG-incorporated cationic liposomes of which surface was incorporated with PEG by ionic complex may be applicable as anticancer drug carriers that can increase therapeutic efficacy.
KEYWORD
Liposome, Polyethyleneglycol, Intracellular uptake
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