Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Physical properties and intracellular uptake of polyethyleneglycol-incorporated cationic liposomes

폴리에틸렌글리콜이 도입된 양이온성 리포솜의 물리적 특성 및 세포이입효과

  • Jung, Soon-Hwa (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) ;
  • Kim, Sung-Kyu (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) ;
  • 정석현 (한국화학연구원 신약기반기술연구센터) ;
  • 김성규 (한국화학연구원 신약기반기술연구센터) ;
  • 성하수 (한국화학연구원 신약기반기술연구센터) ;
  • 조선행 (한국화학연구원 신약기반기술연구센터) ;
  • 신병철 (한국화학연구원 신약기반기술연구센터)
  • Published : 2008.02.21
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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 $98.6{\pm}1.0nm$ of mean particle diameter and $42.8{\pm}0.8mV$ of zeta potential value. The PEG-incorporated cationic liposomes had $110.1{\pm}1.2nm$ of mean particle diameter with an increase of about 10 nm compared to the cationic liposomes. Zeta potential value of them was $12.9{\pm}0.6mV$ 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 $58.4{\pm}1.1%$. Loading efficiency of model drug, doxorubicin, into cationic liposomes or PEG-incorporated cationic liposomes was about $96.0{\pm}0.7%$. 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.

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References

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