• Journal of Pharmaceutical Investigation
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• v.26 no.4
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• pp.291-297
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• 1996

Liposomes of $pSV-{\beta}-Galactosidase$ vector plasmid DNA with various lipid composition were prepared by the thin-film method. Size distribution, shape and the efficiency of plasmid DNA encapsulation were investigated. Effect of sonication time on the plasmid DNA entrapment in liposomes and stability at $4^{\circ}C$ were also examined. Sizes of neutral liposomes were about 100-200 nm and above $1\;{mu}m$, and those of cationic liposomes were about 400-600 nm and above $1\;{mu}m$. Shapes of liposomes entrapped plasmid DNA were spherical. Proper sonication time for better entrapment was below 15 minutes and stability at $4^{\circ}C$ was decreased rapidly after 1 day. Plasmid DNA entrapments of complex liposomes of various lipids were higher than those of liposomes made from one sort of lipid. Plasmid DNA entrapments of cationic liposomes were higher than those of neutral liposomes.

• Journal of Pharmaceutical Investigation
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• v.34 no.4
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• pp.305-310
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• 2004

This study was to prepare the anionic liposomes which were to release anticancer drug (doxorubicin) at the hyperthermia temperature $({\sim}42^{\circ}C)$ and to stabilize in bovine serum solution at $37^{\circ}C$. The vesicle size and zeta potential of liposomes in Tris-HCl buffered solution (pH 7.4) were measured by an electrophoretic light scattering spectrophotometer. To estimate the stability of liposomes, liposome size was measured in bovine serum solution at $37^{\circ}C$ for 72 h. The release of doxorubicin from liposome was determined by measuring the fluorescence intensity using fluorescence spectrophotometry with temperature and time. The size of liposomes was from 120 to 160 nm and zeta potential was from $-33.3{\pm}2.4$ to $-75.6{\pm}6.9\;mV$. Anionic liposome was stabilized in bovine serum solution at $37^{\circ}C$ within 72 h. Additionally, the release transition temperature of doxorubicin from liposomes was increased by increasing mole % of anionic phospholipid.

• Journal of Pharmaceutical Investigation
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• v.22 no.2
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• pp.155-161
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• 1992

Although glycosylated liposomes have attracted much attention as targeting delivery systems (DDS) of drugs to specific organs which have glycoside receptors, physical instability of liposomes greatly limits their practical application. In this case, proliposomes might be a potential answer to solve this problem. Utilizing the proliposomes as tageting DDS has been a goal of our series of works; we have tried to develop DDS which form liposomes uppon adding water and can deliver drugs to specific target organs/cells such as hepatocytes. In this paper, preparation of glycosylated liposomes and binding of the liposomes with lectin (agglutinin RCA 120) was studied. Asialoletuin (AF) was selected as a model compound which has galactose terminal and is favorable for binding with galactose receptor on the surface of hepatocytes. AF was obtained by splitting the terminal N-acetylneuraminic acid (NANA) of fetuin. Small unilamellar AF-liposomes were prepared by mixing aqueous solution of AF-palmitate with thin film of phosphatidyl choline and cholesterol (30:10 w/w) formed on the innersurface of the round bottomed flask. They were successively extruded through polycarbonate membranes (0.45 mm). Palmitoyl-AF not incorporated into the liposomal bilayer was separated from liposomes by a Sepharose 4B column equilibrated with 10 mM Tris-HCI buffered saline. Lectin (agglutinin RCA 120) was added to the suspension of AF-liposomes and incubated at $37^{\circ}C$ for 2 hr. After centrifugation, the unbound lectin in the supernatant was assayed for protein. The binding of the lectin to AF-liposomes (AF content 2.8 nmole) at $37^{\circ}C$ was linear at least upto 35 mg of lectin indicating high affinity association of the lectin to AF molecules of the liposomes.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.2
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• pp.207-210
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• 2004

Glycyrrhiza uralensis (licorice root) is very useful medicinal herb because of strong anti-inflammatory and anti-wrinkle effect. Therefore, it is widely used in functional cosmetics. However, it is insoluble and easily decomposed by light, heat, oxygen, etc. In this study, we first prepared NanoSolve-Licorice (30-50nm) using Glycyrrhiza uralensis and propylene glycol! hydrogenated lecithin/caprylic/capric triglyceride/glycerin/water system with microfluidizer. And then, NanoSolve-Licorice and porous PMMA are dispersed in ethanol. Finally, we could get a stabilized system with high-pressure homogenizer (1,000 Bar, 3 passes). According to HPLC measurement for glabridin content, our system is more stable compared with general liposome ones. Capsulated licorice has an enhanced anti-inflammatory effect on account of excellent skin penetration. We also evaluated our final product through image analyzer, particle size analyzer, FF-TEM and chromameter.

• Korean Journal of Clinical Laboratory Science
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• v.52 no.3
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• pp.253-260
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• 2020

Alzheimer's disease (AD) is a chronic and progressive neurodegenerative disease that can be described by the occurrence of dementia due to a decline in cognitive function. The disease is characterized by the formation of extracellular and intracellular amyloid plaques. Amyloid beta (Aβ) is a hallmark of AD, and microglia can be activated in the presence of Aβ. Activated microglia secrete pro-inflammatory cytokines. Furthermore, S100A9 is an important innate immunity pro-inflammatory contributor in inflammation and a potential contributor to AD. This study examined the effects of metformin and α-LA on the inflammatory response and NLRP3 inflammasome activation in Aβ- and S100A9-induced BV-2 microglial cells. Metformin and α-LA attenuated inflammatory cytokines, such as tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). In addition, metformin and α-LA inhibited the phosphorylation of JNK, ERK, and p38. They activated the nuclear factor kappa B (NF-κB) pathway and the NOD-like receptor pyrin domain containing 3 (NLRP3) inflammasome. Moreover, metformin and α-LA reduced the marker levels of the M1 phenotype, ICAM1, whereas the M2 phenotype, ARG1, was increased. These findings suggest that metformin and α-LA are therapeutic agents against the Aβ- and S100A9-induced neuroinflammatory responses.

• Journal of Pharmaceutical Investigation
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• v.23 no.2
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• pp.111-118
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• 1993

The hemolytic characteristics of amphotericin B-containing liposomes have been investigated in vitro. From the hemolysis of human erythrocytes against free and liposomal amphotericin B, the marked reduction in the toxicity of amphotericin B was observed by incorporating the drug in egg PC liposomes. For 45 min, free amphotericin B at $9.6\;{\mu}g/ml$ could completely lyse 2 wt% human erythrocytes. However, liposomal amphotericin B had essentially no lytic effect even in the range over $9.6\;{\mu}g/ml$. In the 66 hr-hemolysis experiment, liposomal amphotericin B showed the slowly hemolysing chracteristics during the experimental period regardless of the concentration of amphotericin B but rapid hemolysis only for 12 hr was observed in the case of free amphotericin B and the degree of hemolysis for 12 hr was maintained after that time. Also the hemolysing ability of liposomal amphotericin B at $4\;{\mu}g/ml$ was lower than that of free amphotericin B at the same concentration for 66 hr. On the other hand, the dependence of hemolysis on amphotericin B contents in egg PC liposomes was significant between 1.64 mole% amphotericin B-containing liposomes and 15.79 or 27.27 mole% amphotericin B-containing liposomes. But no marked difference in hemolysis was observed between 15.79 and 27.27 mole% amphotericin B-containing liposomes. Especially, cholesterol as an excipient in amphotericin B-containing liposomes significantly reduced the hemolysis of human erythrocyte. The degree of hemolysis in 5 mole% amphotericin B-containing liposomes was reduced to approximately 50% of value in the cholesterol-free liposomes by adding 50% cholesterol.

• 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.

• Journal of Pharmaceutical Investigation
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• v.39 no.6
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• pp.423-429
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• 2009

Liposomes have been used as one of the efficient carriers for drug delivery. In this study, anionic liposomes of which surface was modified by using both electrostaic interaction between anionic liposomes and cationically charged BSA molecules at lower pH than isoelectric point (pI) of BSA and denaturation of the BSA-coated liposomes by thermal treatment. The thermally denatured BSA-coated liposomes (DBAL) had mean particle diameter of 125.2${\pm}$1.7 nm and zeta potential value of -22.4${\pm}$4.5 mV. Loading efficiency of model drug, doxorubicin (DOX), into liposomes was 83.0${\pm}$2.6%. Results of in vitro stability study of DBAL in blood plasma showed that the mean particle diameter of DBAL 400 did not increase in blood plasma and adsorption of plasma protein was much less than plain or anionic liposomes. Intracellular uptake of DBAL 400 evaluated by confocal microscopy observation was higher than that of PEG liposomes.

• Journal of the Korea Institute of Information and Communication Engineering
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• v.20 no.12
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• pp.2395-2400
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• 2016

Conventional drug carriers such as liposomes, nanoparticles, polymer micelles, polymeric conjugate and lipid microemulsion for cancer chemotherapy shield normal tissues from toxic drugs to treat cancer cells in tumors. However, inaccurate tumor targeting uncontrolled drug release from the carriers and unwanted accumulation in healthy sites can limit treatment efficacy with current conventional drug carriers with insufficient concentrations of drugs in the tumors and unexpected side effects as a result. Sickle red blood cells show natural tumor preferential accumulation without any manipulation due to the adhesive interaction between molecular receptors on the membrane surface and counter-receptor on endothelial cells. In addition, structural changes of microvascular in tumor sites enhances polymerization of sickle red blood cells. In this research, we examined the use of sickle red blood cells as a new drug carrier with novel tumor targeting and controlled release properties to quantify its therapeutic effects.

• Journal of Life Science
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• v.18 no.3
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• pp.298-303
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• 2008

Using a phage peptide library approach, we have isolated a peptide ligand that binds to transferrin receptor on the surface of human melanoma cell, B16F10. The library was first screened twice by recovering internalized phages and was further screened three times by competitively eluting transferrin receptor-specific phages with human transferrin among the phages bound to the cell surface. The peptides displayed by the selected phages were fused to translocation and catalytic domain of Pseudomonas exotoxin to prepare recombinant toxins. After estimating cytotoxicity of each recombinant toxin toward B16F10 cell, seven clones were selected. Sequence analysis revealed that one of the clones displayed a peptide which had a significant sequence homology with human transferrin. The peptide was chemically synthesized and was shown to be functional in delivering cytotoxic agents into B16F10 cell via interaction with transferrin receptor.