• Title/Summary/Keyword: Cationic lipids

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Polyethylene glycol (PEG)-modified cationic liposome mediated gene delivery

  • Kim, Jin-Ki;Choi, Sung-Hee;Ahn, Woong-Shick;Kim, Chong-Kook
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.426.1-426.1
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    • 2002
  • In this study. we modified the cationic liposomes by polyethylene glycol (PEG)-grafted or PEG-added methods. The PEG-grafted transfection complexes were prepared by adding the plasmid DNA to the PEG-grafted cationic liposomes, composed of PEG and cationic lipids. PEG-added transfection complexes were prepared by adding the PEG to the mixture of cationic lipids and plasmid DNA. The particle sizes of PEG-modified transfection complexes did not change during storage compared to conventional transfection complexes. (omitted)

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The Effects of Supplements on the Plasmid Delivery and Expression in the Transfection Using Cationic Liposomes (양이온 리포좀을 이용한 유전자 전달 및 발현서 첨가제의 효과)

  • ;;;C. Schmid
    • KSBB Journal
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    • v.13 no.4
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    • pp.418-423
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    • 1998
  • Cellular transfections with cationic liposomes are widely empolyed for gene and oligonucleotide transfer in vitro because of their safety and ease of use. However, they still suffer from the low transfection efficiency comparing with viral vectors. Substantial effort shave been focused on increasing transfection efficiency by supplementing the liposome/DNA complexes(lipoplex) with various components. In this work, we tired three kinds of supplements, Poly-L-lysine(PLL), transferrin and a mixture of anionic lipids(PS/PE/PC), to study their effects on gene transfer yield and gene expression efficiency. PLL, a polycationic polymer, enhanced gene transfer yield by 3 times but the gene expression efficiency was increased only by 1.5 times. this result implies that PLL can enhance the transfection efficiency mainly by increasing the rate of outermembrane transport of lipoplex into the cells. On the other hand, transferrin which can facilitate the gene transfer via ligand-receptor interaction gave not only increased gene transfer yield but also enhanced gen expression efficiency by 2.8 times. Transferrin seems to contribute to the escape of plasmid from endosomes through ligand-receptor recycle mechanism. When the cells were treated with a mixture of anionic lipids for 3 hours before the transfection, gene transfer yield was slightly decreased but the gene expression efficiency was enhanced by 1.9 times. This is presumably due to the accelerated liposome-plasmid dissociation by the anionic lipids, and the increased delivery of plasmid to the nucleus. According to these results, it is clear that the supplementation to ameliorate transfection efficiency with cationic liposomes should be contrived in the direction of increasing delivery of plasmid.

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In vitro and in vivo transfection efficiency of a cationic lipid containing sodium cholate

  • Kim, Adele;Lee, Eun-Hye;Choi, Sung-Hee;Kim, Chong-Kook
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.425.3-426
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    • 2002
  • Cationic lipids have been used as one of the major components for making most promising non-viral gene delivery systems. whereas sodium cholate. an edge activator has been used as a surfactant in making ultradeformable and ultraflexible liposomes called Transfersomes. Using both a cationic lipid, DOTAP and sodium cholate. a newly formulated ultradeformable cationic liposome has been prepared. The average particle size of this formulation was approximately 80nm. (omitted)

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Intravenous and Intra-arterial Delivery of Plasmid DNA/Cationic Lipiodol Emulsion Complexes

  • Chae, Min-Jung;Chung , Hes-Son;Kwon, Ick-Chan;Chung, Jin-Wook;Park, Jae-Hyung;Sohn, Young-Taek;Jeong, Seo-Young
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.226.3-227
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    • 2003
  • A cationic lipid emulsion (o/w) containing lipiodol and 1, 2-dioleoyl-sn- glycero-3-trimethylammonium-propane (DOTAP) has been prepared as a gene delivery system. In order to increase the transfection efficiency of the lipiodol emulsion, 1 2-dioleoyl-sn-glycero-3-phospho-ethanolamine (DOPE) and polyoxyethylene sorbitan monooleate (Tween 80) were incorporated as additional lipids. By including DOPE and Tween 80, the cationic emulsion became a more potent gene carrier under in vitro condition in the presence of serum, and under in vivo condition. (omitted)

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Encapsulation of Plasmid DNA in Pegylated Liposome

  • Jang, Jung-Ok;Gwak, Hye-Sun;Lee, Hwa-Jeong
    • Journal of Pharmaceutical Investigation
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    • v.35 no.5
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    • pp.337-341
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    • 2005
  • The purpose of the study was to prepare the pegylated liposome carrying plasmid DNA with optimal encapsulation efficiency. Plasmid DNA (pCEP4 clone 790, 10.6 kb) was entrapped in the pegylated liposome composed of neutral lipid, POPC (l-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine), cationic lipid, DDAB (dimethyl dioctadecyl ammonium bromide) and anionic lipids, DSPE-PEG 2000 (distearoyl phosphatidyl ethanolamine polyethylene glycol 2000) and DSPE-PEG 2000-maleimide by freezing/thawing method. Free plasmid DNA was separated from the encapsulated one by Sepharose CL-4B column chromatography. The DNA amount encapsulated into the pegylated liposome was increased as cationic lipid concentration, initial amount of plasmid DNA and total lipid amount were increased.

Validation of Heterodimeric TAT-NLS Peptide as a Gene Delivery Enhancer

  • Doh, Kyung-Oh
    • Journal of Microbiology and Biotechnology
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    • v.25 no.6
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    • pp.788-794
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    • 2015
  • Cationic liposomes have been actively used as gene delivery vehicles despite their unsatisfactory efficiencies because of their relatively low toxicity. In this study, we designed novel heterodimeric peptides as nonviral gene delivery systems from TAT and NLS peptides using cysteine-to-cysteine disulfide bonds between the two. Mixing these heterodimeric peptides with DNA before mixing with lipofectamine resulted in higher transfection efficiencies in MCF-7 breast cancer cells than mixing unmodified TAT, NLS, and a simple mixture of TAT and NLS with DNA, but did not show an adverse effect on cell viability. In gel retardation assays, the DNA binding affinities of heterodimeric peptides were stronger than NLS but weaker than TAT. However, this enhancement was only observed when heterodimeric peptides were premixed with DNA before being mixed with lipofectamine. The described novel transfection-enhancing peptide system produced by the heterodimerization of TAT and NLS peptides followed by simple mixing with DNA, increased the gene transfer efficiency of cationic lipids without enhancing cytotoxicity.

Physical properties of cyclosporin A-loaded nanostructured lipid carriers (Cyclosporin A가 봉입된 nanostructured lipid carriers의 물리적 특성연구)

  • Song, Chung-Kil;Chung, Suk-Jae;Shim, Chang-Koo;Kim, Dae-Duk
    • Journal of Pharmaceutical Investigation
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    • v.38 no.1
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    • pp.39-43
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    • 2008
  • Cyclosporin A (CyA), a potent immunosuppressive drug used in allogeneic transplants and autoimmune disease, is a typical water-insoluble drug. Recently, nanoparticle carriers were investigated to improve the intestinal absorption of drugs. In this study, CyA-loaded nanostructured lipid carriers (NLCs) were prepared from a hot o/w emulsion using the high pressure homogenization method. The NLCs were consisted of cationic lipids, solid lipids, liquid lipids (oils), surfactant and stabilizer. Encapsulation efficiency of CyA in NLCs was approximately 71%. The average particle size and zeta potential of NLCs were below 250 nm and above +40 mV, respectively. The morphology of NLCs was confirmed by transmission electron microscopy (TEM) analysis. Compared to the CyA powder, higher in vitro release of CyA from NLCs was observed after burst release within 30 min. Thus, CyA-loaded NLCs could be applied not only for parenteral route but also for gastrointestinal administration, which needs further investigation.

Relative Bioavailability of Coenzyme Q10 in Emulsion and Liposome Formulations

  • Choi, Chee-Ho;Kim, Si-Hun;Shanmugam, Srinivasan;Baskaran, Rengarajan;Park, Jeong-Sook;Yong, Chul-Soon;Choi, Han-Gon;Yoo, Bong-Kyu;Han, Kun
    • Biomolecules & Therapeutics
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    • v.18 no.1
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    • pp.99-105
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    • 2010
  • The purpose of this study was to evaluate relative bioavailability of the coenzyme Q10 (CoQ10) in emulsion and three liposome formulations after a single oral administration (60 mg/kg) into rats. Emulsion formulation of CoQ10 was prepared by conventional method using Phospholipon 85G as an emulsifier, and three liposome formulations (neutral, anionic, and cationic) of CoQ10 were prepared by traditional lipid film hydration technique using Phospholipon 85G, cholesterol, and charge carrier lipids (1,2-dioleoyl-3-trimethylammonium-propane chloride salt for cationic liposome and 1,2-dimyristoyl-sn-glycero-3-phosphate monosodium salt for anionic liposome). Mean particle size of all CoQ10-loaded liposome was less than a micron, and size distribution of the liposome population was homogeneous. Bioavailability of CoQ10 in emulsion was 1.5 to 2.6-fold greater than liposome formulations in terms of $AUC_{0-24\;h}$. $T_{max}$ was 3 h when administered as emulsion while it was greater than 6 h in liposome formulations. Notably, it was approximately 8 h in cationic liposome. $C_{max}$ was highest in emulsion and was significantly decreased when administered as liposome. Charged liposome showed even lower $C_{max}$ than neutral liposome, especially in cationic liposome. In conclusion, therefore, it is suggested that clinicians and patients consider bioavailability issue a primary concern when choosing a CoQ10 product, especially when very high plasma level is required such as in the treatment of heart failure and Parkinson's disease.