Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Intracellular delivery and anti-tumor activity of polyethyleneglycol liposomes containing cationic lipid

양이온성 지질이 포함된 PEG 리포솜의 세포내 이입 및 항암효력 평가

  • Jung, Soon-Hwa (Center for drug discovery technologies, Korea Research Institute of Chemical Technology) ;
  • Kim, Sung-Kyu (Center for drug discovery technologies, Korea Research Institute of Chemical Technology) ;
  • Jung, Suk-Hyun (Center for drug discovery technologies, Korea Research Institute of Chemical Technology) ;
  • Seong, Ha-Soo (Center for drug discovery technologies, Korea Research Institute of Chemical Technology) ;
  • Cho, Sun-Hang (Center for drug discovery technologies, Korea Research Institute of Chemical Technology) ;
  • Shin, Byung-Cheol (Center for drug discovery technologies, Korea Research Institute of Chemical Technology)
  • 정순화 (한국화학연구원 신약기반기술연구센터) ;
  • 김성규 (한국화학연구원 신약기반기술연구센터) ;
  • 정석현 (한국화학연구원 신약기반기술연구센터) ;
  • 성하수 (한국화학연구원 신약기반기술연구센터) ;
  • 조선행 (한국화학연구원 신약기반기술연구센터) ;
  • 신병철 (한국화학연구원 신약기반기술연구센터)
  • Published : 2008.06.20
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Abstract

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 $97.0{\pm}1.3\;nm$ of mean particle diameter and $-21.7{\pm}1.2\;mV$ of zeta potential value. PCL had $96.4{\pm}1.8\;nm$ of mean particle diameter and $-8.7{\pm}1.1\;mV$ 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 $95.0{\pm}1.9%$. 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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References

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