| Title | Polyethylene glycol complexed cationic liposome for enhanced cellular uptake and anticancer activity. | | Author(s) | Jung SH, Jung SH, Seong H, Cho SH, Jeong KS, Shin BC | | Institution | Biomaterials Research Center, Korea Research Institute of Chemical Technology, Yuseong, Deajeon, Republic of Korea; Center for Bioactive Molecular Hybrids and Department of Chemistry, Yonsei University, Seoul, Republic of Korea. | | Source | Int J Pharm 2009 Aug 7. | | Abstract | 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+/-1.0nm of mean particle diameter and 45.5+/-1.1mV of zeta potential value. While, the PCL had 110.1+/-1.2nm of mean particle diameter and 18.4+/-0.8mV 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 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. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19666094 |
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