Polyethylene glycol-complexed cationic liposome for enhanced cellular uptake and anticancer activity

Suk Hyun Jung, Soon Hwa Jung, Hasoo Seong, Sun Hang Cho, Kyu Sung Jeong, Byung Cheol Shin

Research output: Contribution to journalArticlepeer-review

54 Citations (Scopus)

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 ± 1.0 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®. 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®. In vivo antitumor activity of DOX-loaded PCL was comparable to that of Doxil® 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.

Original languageEnglish
Pages (from-to)254-261
Number of pages8
JournalInternational Journal of Pharmaceutics
Volume382
Issue number1-2
DOIs
Publication statusPublished - 2009 Dec 1

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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