期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 382, 期 1-2, 页码 254-261出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2009.08.002
关键词
Liposome; Cationic lipid; Polyethylene glycol; Intracellular uptake
资金
- Ministry of Knowledge and Economy of South Korea [10016573]
- Korea Institute of Industrial Technology(KITECH) [10016573] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Liposomes as one of the efficient drug carriers have some shortcomings such as their relatively short blood circulation time, fast clearance from human body by reticuloendothelial system (RES) and limited intracellular uptake to target cells. In this study, polyethylene glycol (PEG)-complexed cationic liposomes (PCL) were prepared by ionic complex of cationically charged liposomes with carboxylated polyethylene glycol (mPEG-COOH). The cationic liposomes had approximately 98.6 +/- 1.0 nm of mean particle diameter, and 45.5 +/- 1.1 mV of zeta potential value. While, the PCL had 110.1 +/- 1.2 nm of mean particle diameter and 18.4 +/- 0.8 mV of zeta potential value as a result of the ionic complex of mPEG-COOH with cationic liposomes. Loading efficiency of model drug, doxorubicin, into cationic liposomes or PCL was about 96.0 +/- 0.7%. Results of intracellular uptake evaluated by flow cytometry and fluorescence microscopy studies showed higher intracellular uptake of PCL than that of Doxil (R). In addition, in vitro cytotoxicity of PCL was comparable to cationic liposomes. in pharmacokinetic study in rats, PCL showed slightly lower plasma level of DOX than that of Doxil (R). In vivo antitumor activity of DOX-loaded PCL was comparable to that of Doxil (R) against human SKOV-3 ovarian adenocarcinoma xenograft rat model. Consequently, the PCL, of which surface was complexed with PEG by ionic complex may be applicable as drug delivery carriers for increasing therapeutic efficacy of anticancer drugs. (C) 2009 Elsevier B.V. All rights reserved.
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