• 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.

• International Journal of Industrial Entomology and Biomaterials
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• v.4 no.1
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• pp.57-62
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• 2002

Cationic liposomes complexed with DNA have been extensively utilized for the delivery of reporter or therapeutic genes both in culture and in vivo. We investigated and determined the optimum conditions of a cationic liposome, composed of dimethyldioctadecy-lammonium bromide (DDAB) and dioleoyl phosphati-dylethanolamine UOPE), mediated a reporter plasmid expressing luciferase into insect cell lines (Sf-21 and Bm-N) and silkworm larvae. Together the data demonstrated that Bombyx mori nuclear polyhedrosis virus (BmNPV) genomic DNA (128 kb) was successfully transfected into Bm-5 cells using this liposome. These results suggest that DDAB/DOPE liposome will be useful as delivery agents for gene transfer to insect cells both in vitro and in vivo.

• 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.

• Bulletin of the Korean Chemical Society
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• v.34 no.3
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• pp.735-742
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• 2013

Peptide nucleic acids (PNAs) that bind to complementary nucleic acid sequences with extraordinarily high affinity and sequence specificity can be used as antisense oligonucleotides against microRNAs, namely antagomir PNAs. However, methods for efficient cellular delivery must be developed for effective use of PNAs as therapeutic agents. Here, we demonstrate that antagomir PNAs can be delivered to hepatic cells by complementary DNA oligonucleotide and cationic liposomes containing galactosylated ceramide and a novel cationic lipid, DMKE (O,O'-dimyristyl-N-lysyl glutamate), through glycoprotein-mediated endocytosis. An antagomir PNA was designed to target miR-122, which is required for translation of the hepatitis C virus (HCV) genome in hepatocytes, and was hybridized to a DNA oligonucleotide for complexation with cationic liposome. The PNA-DNA hybrid molecules were efficiently internalized into hepatic cells by complexing with the galactosylated cationic liposome in vitro. Galactosylation of liposome significantly enhanced both lipoplex cell binding and PNA delivery to the hepatic cells. After 4-h incubation with galactosylated lipoplexes, PNAs were efficiently delivered into hepatic cells and HCV genome translation was suppressed more than 70% through sequestration of miR-122 in cytoplasm. PNAs were readily released from the PNA-DNA hybrid in the low pH environment of the endosome. The present study indicates that transfection of PNA-DNA hybrid molecules using galactosylated cationic liposomes can be used as an efficient non-viral carrier for antagomir PNAs targeted to hepatocytes.

• Journal of the Korean Applied Science and Technology
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• v.33 no.3
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• pp.428-434
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• 2016

In this study, benzyltrialkylammonium chlorides with different alkyl chain length were synthesized and applied to liposome. Prepared cationic surfactant embedded liposomes were measured particle size, zetapotential, release property and antibacterial activity. The average particle size of liposomes was 120~140 nm. As alkyl chain length was increased, the liposome size was increased. Zetapotential for the solution of liposomes added cationic surfactants were in the range of +80~90 mV. In release test, collagen release rate could be controlled by alkyl chain length. liposome embedded long alkyl chain surfactant had enhanced sustained release property. Entrapment efficiency of hydrophilic collagen were 25.9~27.5%.

• Journal of Pharmaceutical Investigation
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• v.28 no.2
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• pp.93-98
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• 1998

We have developed liposomes which can be easily prepared with inexpensive lipid, have enhanced stability, and can efficiently deliver DNA into the COS-l cells, Liposome formulations were prepared using cationic materials such as dimethyldioctadecyl ammonium bromide (DDAB), cetyltrimethyl ammonium bromide(CTAB), We investigated the effect of cationic liposome formulations on in vitro DNA transfection, DDAB-containing liposomes showed increased transfection efficiency which was 3.2-fold as much as that by $Lipofectin^{\circledR}$, but CTAB-containing liposomes were inactive in gene transfection. The effect of colipid of DDAB-containing liposome was also investegated. As a colipid, dioleylphosphatidylethanolamine(DOPE) and cholesterol did altered the transfection efficiency of DDAB-containing liposomes. And increased DDAB concentration lowered the transfection efficiency. The optimum amount of liposomal formulation was $10\;{\mu}M$ for $1\;{\mu}g$ of DNA. In the experiment of stability, DOPE-containing liposomes formulation showed a broad size distribution and separation of two major peaks on a 5th day of preparation, but liposomes containing cholesterol was stable for 10 days. DDAB-containing liposomal DNA delivery system was prepared easily and was stable.

• 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.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.

• 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)

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.427.1-427.1
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• 2002

To improve stability and transfection efficiency, a novel combination of cationic emulsion and galactosylated chitosan was developed for targeted gene delivery. Six formulations of cationic liposome and our novel emulsion were prepared for comparison of stability and transfection efficiency. Cationic liposomes composed of 3［N-(N.N dimethylaminoethylene) carbamoyl］ cholesterol (DC-Chol) and dioleyl phophatidyl ethanolamine (DOPE) were prepared by extrusion method and cationic emulsions composed of DC-Chol. DOPE. castor oil, and Tween 80 were prepared by sonication method. (omitted)