• Biotechnology and Bioprocess Engineering:BBE
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• v.6 no.4
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• pp.279-283
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• 2001

Cationic lipid emulsion system consisting of 1, 2-dioleoyl-sn-slycero-3-trimethyl-ammonium-propane(DOTAP) and plasmin DNA with various counterions in the lipid headgroups were prepared. The transfection activity of the cationic lipid emulsion systems was then investigated in vitro and in vivo. The complex formation of plasmid DNA lipid emulsion was affected by the counterions through charged headgroup repulsion and also by the salt concen-tration in the media. As such , the transfection activity of the DOTAP emulsion system can be controlled by changing the counterions.

• Bulletin of the Korean Chemical Society
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• v.34 no.3
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• pp.931-935
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• 2013

Lipid events in liposome-mediated transfection (lipofection) are largely unknown. Here we studied whether phospholipase D (PLD), an important enzyme responsible for phospholipid breakdown, was affected during lipofection of HepG2 cells with a luciferase plasmid. Synthetic cholesterol (Chol) derivatives, including $3{\beta}$[L-ornithinamide-carbamoyl]Chol, [polyamidoamine-carbamoyl]Chol and $3{\beta}$[N-(N',N'-dimethylaminoethane)-carbamoyl]Chol, and a cationic lipid, N-[1-(2,3-dioleyloxy)propyl]-N,N,N-trimethylammonium chloride were mixed with a helper lipid dioleoylphosphatidylethanolamine to form respective cationic liposomes. All cationic liposomes were found to stimulate PLD. Although orders of magnitude effects of the cationic liposomes on PLD stimulation did not consistently match those on cytotoxicity and luciferase expression, a causal relationship between PLD activation and cytotoxic effect was remarkable. PLD stimulation by the cationic liposomes was likely due to their amphiphilic characters, leading to membrane perturbation, as supported by similar results obtained with other membrane-perturbing chemicals such as oleate, melittin, and digitonin. Our results suggest that lipofection induces cellular lipid changes such as a PLD-driven phospholipid turnover.

• Journal of Pharmaceutical Investigation
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• v.39 no.5
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• pp.339-343
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• 2009

Recently, co-delivery of drug and gene has been attempted for higher therapeutic effects of anticancer agents. In this study, cationic liposomes were prepared using 1,2-dioleoyl-3-trimethylammoniopropane (DOTAP) as a cationic lipid to investigate the effect of drug loading on the physicochemical characteristics of cationic liposomes/DNA complexes. The complex formation between cationic liposomes and negatively charged plasmid DNA was confirmed and the protection from DNase was observed. Particle size of complexes was reduced not by drug loading, but by the increased ratio of cationic lipid to plasmid DNA. Meanwhile, zeta potential of complex was increased by the addition of cationic liposomes to complexes and the effect of drug loading on the zeta potential was not much higher than on particle size. Gel retardation of complexes was indicated when the complexation weight ratios of cationic lipid to plasmid DNA were higher than 24:1 for drug free complexes and 20:1 for drug loaded ones, respectively. Agarose gel retardation showed the similar complexation between plasmid DNA and drug free liposomes or drug loaded liposomes. Both complexes protected plasmid DNA from DNase independent of complexation temperature. From the results, drug loading may affect not the complex formation of cationic liposomes and plasmid DNA, but the particle size of complex.

• Bulletin of the Korean Chemical Society
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• v.33 no.7
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• pp.2187-2192
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• 2012

This study presents a facile way synthesizing disc-like lipid bilyaer nanostructures with a cationic amphiphilic polyelectrolyte. The cationic amphiphilic polyelectrolyte was in a form of partially quarternized copolymer and was synthesized with 2-(dimethylamino)ethyl methacrylate and stearyl methacrylate. At some concentration ranges of the polymer, the addition of the polymer to lipid components during the preparation of bilayer nanostructures resulted in discs with a fairly high yield (~99%). The mechanism for the formation of the nanostructures was discussed based on the physical properties of these nanostructures and by comparing the nanostructures obtained with an anionic amphiphilic polyelectrolyte.

• BMB Reports
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• v.33 no.6
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• pp.476-482
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• 2000

In this paper, we report a new cationic lipid composed of L-lysinamide and cholesterol as a potent gene delivery vector. $3{\beta}$[L-Lysinamide-carbamoyl] cholesterol could self-assemble with plasmid DNA forming discrete lipoplexes. From atomic force microscopic images of the complexes, the size distribution was observed to range from 100 to 150 nm in diameter. The transfection efficiency of this amphiphile on different cell lines was evaluated as a micellar solution in the absence of the fusogenic helper lipid, dioleoyl phosphatidyletbanolamine (DOPE). Transfection experiments were performed as a function of charge ratio (lipid/DNA) and transfection time. Cytotoxicity and in vitro transfection efficiency of the amphiphile was demonstrated and compared with those of commercially available Lipofectin and polyethylenimine (PEI).

• Microbiology and Biotechnology Letters
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• v.34 no.4
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• pp.329-334
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• 2006

Cationic liposome has been studied as one of the most promising non-viral gene delivery systems. In this report, we describe a new synthesized cholesterolic cationic lipid (2-aminoethylcarbamate-cholesterol) and dioleylphosphatidylethanolamine (DOPE) improve the cellular uptake properties of antisense ODNs, as well as plasmid DNA with low toxicity. This formulation of cholesterolic cationic lipid termed Chol-E, efficiently transfects ODNs and plasmids into many cell types in the presense or absence of 10% serum in the medium.

• Journal of Pharmaceutical Investigation
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• v.38 no.3
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• pp.163-169
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• 2008

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.

• 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)

• Journal of Microbiology and Biotechnology
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• v.22 no.6
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• pp.866-871
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• 2012

A novel cholesterol-based cationic lipid containing a tri-2-hydroxyethylamine head group and ether linker (Chol-THEA) was synthesized and examined as a potent gene delivery vehicle. In the preparation of cationic liposome, the addition of DOPE as helper lipid significantly increased the transfection efficiency. To find the optimum transfection efficiency, we screened various weight ratios of DOPE and liposome/DNA (N/P). The best transfection efficiency was found at the Chol-THEA:DOPE weight ratio of 1:1 and N/P weight ratio of 10~15. Most of the plasmid DNA was retarded by this liposome at the optimum N/P weight ratio of 10. The transfection efficiency of Chol-THEA liposome was compared with DOTAP, Lipofectamine, and DMRIE-C using the luciferase assay and GFP expression. Chol-THEA liposome with low toxicity had better or similar potency of gene delivery compared with commercial liposomes in COS-7, Huh-7, and MCF-7 cells. Therefore, Chol-THEA could be a useful non-viral vector for gene delivery.

• KSBB Journal
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• v.14 no.3
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• pp.377-379
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• 1999

In order to improve the transfection efficiency of CHO/dhfr- cells using cationic lipid, optimal concentrations of the cationic lipid($LipofectAmine^{TM}$) and DNA(pEGFP-C1) need to be determined. The use of green fluorescent protein(GFP) gene as a reporter gene facilitated the quantification of transfection efficiency. The green fluorescence intensity of each cell transfected at various lipid-DNA concentrations was measured using fluorescence-activated cell sorter(FACS) analysis. A combination of $2.0{\mu}L$ cationic lipid and 0.4{$\mu}g$ DNA in a well resulted in the highest trasfection efficiency. Taken together, the method using FACS analysis of GFP is simple and fast, facilitating the optimization of transfection.