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

• Polymer(Korea)
• /
• v.33 no.3
• /
• pp.213-218
• /
• 2009

A cationic lipid emulsion containing 1,2-dioleoyl-3-trimethylammonium-propane(DOTAP), Tween80, squalene has been prepared as a gene delivery system. In order to increase the transfection efficiency of gene carrier, folate was used as the tumor-targeting ligand that was attached on PEG-DPPE. HeLa and 293 cells were used for the in vitro transfection experiment. HeLa cell is a folate-positive cell line. The mean particle sizes of polymeric lipid system and DNA/lipid complex system were 206.6 nm and 150.5 nm, respectively. The transfection efficiencies of our carriers(4:l(w:w) complex ratio)were 100 times higher than that of DOTAP only emulsion due to the targeting effect of folate.

• Molecules and Cells
• /
• v.22 no.2
• /
• pp.175-181
• /
• 2006

Delivery of DNA vaccines to airway mucosa would be an ideal method for mucosal immunization. However, there have been few reports of a suitable gene delivery system. In this study we used a cationic emulsion to immunize mice via the intranasal route with pCMV-S coding for Hepatitis B virus surface antigen (HBsAg). Complexing pCMV-S with a cationic emulsion dramatically enhanced HBsAg expression in both nasal tissue and lung, and was associated with increases in the levels of HBs-specific Abs in serum and mucosal fluids, of cytotoxic T lymphocytes (CTL) in the spleen and cervical and iliac lymph nodes, and of delayed-type hypersensitivity (DTH) against HBsAg. In contrast, very weak humoral and cellular immunities were observed following immunization with naked DNA. In support of these observations, a higher proliferative response of spleenocytes was detected in the group immunized with the emulsion/pCMV-S complex than in the group immunized with naked pCMV-S. These findings may facilitate development of an emulsion-mediated gene vaccination technique for use against intracellular pathogens that invade mucosal surfaces.

• Proceedings of the PSK Conference
• /
• 2003.10b
• /
• pp.226.3-227
• /
• 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)

• Biomolecules & Therapeutics
• /
• v.18 no.1
• /
• pp.99-105
• /
• 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.

• Journal of Pharmaceutical Investigation
• /
• v.40 no.6
• /
• pp.357-362
• /
• 2010

To enhance therapeutic effects of insulin-sensitizing adipokine, ADN gene and potent agonists, rosiglitazone for the $PPAR{\gamma}$, cationic liposomes as non-viral vectors were formulated. The particle size and zeta potential of drug loaded and unloaded cationic liposomes were investigated. The complex formation between cationic liposomes and negatively charged plasmid DNA was confirmed and the protection from DNase was observed. In vitro transfection was investigated in HepG2, HeLa, and HEK293 cells by mRNA expression of ADN. Encapsulation efficacy of rosiglitazone-loaded liposomes was determined by UV detection. Particle sizes of cationic liposomes were in the range of 110-170 nm and those of rosiglitazone-loaded cationic liposomes were in the range of 130-180 nm, respectively. Gel retardation of complexes indicated that the complex was formed at weight ratios of cationic lipid to plasmid DNA higher than 20:1. Both complexes protected plasmid DNA from DNase either drug free or drug loading. Encapsulation efficiency of rosiglitazone-loaded emulsion was increased by drug dose. The mRNA expression levels of ADN were dose-dependently increased in cells transfected with plasmid DNA. Therefore, cationic liposomes could be potential co-delivery system for drug and gene.

• Journal of Pharmaceutical Investigation
• /
• v.33 no.2
• /
• pp.121-127
• /
• 2003

The objective of this study was to solidify the simvastatin self-microemulsifying drug delivery system (SMEDDS) and to improve the encapsulation efficiency of solidified alginate beads using sodium alginate. Typical simvastatin SMEDDS was composed of various oils, surfactants and cosurfactants. Also solidified-alginate beads was prepared by crosslinking liquid emulsion mixtures containing sodium alginate and other excipients (cetylpyridinum chloride (CP-Cl), hydroxypropyl methylcellulose, starch and so on). in $CaCl_2$ solution, it has been investigated that the drug release pattern and encapsulation efficiency were varied with the ratio of cationic lipid (CP-Cl). Solidified sodium alginate beads containing simvastatin SMEDDS were redispersed into media without re-aggregation. Oil droplet size of redispersed solidified-beads in media produced smaller than the initial size. The density of beads and drug loading amount were increased with increasing cationic lipid content. These systems have advantages of storage stability and predictability of drug release rate.

• Journal of Pharmaceutical Investigation
• /
• v.38 no.1
• /
• pp.39-43
• /
• 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.