• KSBB Journal
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• v.10 no.4
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• pp.428-434
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• 1995

Target-sensitive(TG-S) liposomes, which have the antibodies coupled on the surface of liposome and can release their entrapped contents by the binding of antibodies with the specigic target cells, were prepared and employed to study the release of calcein and the selective delivery of an anticancer agent, doxorubicin(DOX). The monoclonal antibody, Y3, used for the preparation of the TG-S liposome was one against major histocompatibility complex class 1 of mouse(MHCI, H-2Kｂtype) and the target cells were EL-4 and RMA, which have the MHC1, H-2Kbtype on their membrane surfacem. The release of calcein from TG-S liposome occurred when the target cells were contacted with liposomes and it was proportionally increased with the rise of binding capacity of antibody coupled on the surface of liposome to the target cells. The experimental results of drug delivery were similar to the cases of calcein release. The viability of specific target cell, EL-4 with liposomal DOX was not so different from that with the free DOX, while for the non-specific target cell, Yacl(H-2Kf), the cell viability with Iiposomal DOX was much higher than that with free DOX. This shows the fact that the liposomal DOX can be efficiently delivered to the specific target cells, while it was not the case for the non-specific target cells. And the drug delivery was lnhibited when the free antibody of Y3 was added in the contact process between EL-4 and TG-S liposomes, which means the drug delivery occurred mainly by the destabilization of TG-S liposomes. From these results, we could conclude that the selective drug delivery to specific target cell using the TG-S liposome would be feasible.

• Journal of the Korean Society of Food Science and Nutrition
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• v.30 no.3
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• pp.421-425
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• 2001

Antioxidative effects of crude chlorophylls and carotenoids extracts from mustard leaf kimchi on the lipid peroxidation in rat liver homogenate, egg phosphatidyl choline (EPC) liposome and superoxide anion radical were examined. The extracts were found to inhibit the increase of the thiobarbituric acid (TBA) value and show the effect of antioxidative activity on the liposomal phospholipid membrane. The oxidation index of EPC liposome was markedly decreased in the prescence of the extracts. The antioxidative activity of the extracts from mustard leaf kimchi was not related with fermentation period of the kimchi. The extracts from mustard leaf showed the similar antioxidative activity of $\alpha$-tocopherol within in the given level of addition. However, the oxidation index. When the effect of the extracts from mustard leaf kimchi on free radical scavenging was observed by the determination of the superoxide anion radical scavenging activity, it had similar value to that of $\alpha$-tocopherol.

• Journal of Life Science
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• v.12 no.2
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• pp.121-128
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• 2002

The object of this study was to investigate the effect of membrane fluidity of bellflower(Platycodon grandiflorum A. DC, ; PG) fractions in phosphatidylcholine(PC) liposomes, measured with high-sensitivity differential scanning calorimetry(DSC). We used dipalmitoylphosphatidylcholine(DPPC) bilayers which slake most stable liposomes among the other phosphatidylcholine. The sample PG was extracted and fractionated to five different types : butanol(PGMB), ethylacetate(PGMEA), ethylether(PGMEE), hexane (PGMH) and methanol(PGMM). Among five different solvent fractions, the PGMEE, PGMEA, PGMH and PGMM fractions markedly affected the thermotropic properties of DPPC liposomes, broadened and shifted the thermograms, and reduced the cooperative unit. It might be said that the incorporation of PGMEE, PGMEA and PGMH in DPPC liposomes were located in the hydrophobic core of DPPC bilayers and, PGMM and PGMB in the hydrophilic core of DPPC bilayers. These results suggest that certain substances in the PGMEE, PGMEA and PGMH fractions might have biologically significant effect on the membrane fluidity.

• Journal of the Korean Society of Food Science and Nutrition
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• v.31 no.3
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• pp.506-510
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• 2002

The effect of antioxidant activity of Platycodon grandiflorum (PG) on the liposomal phospholipid membrane was investigated by spectrophotometry. Membrane oxidation causes damage to the membrane fluidity and permeability. It brings further destruction to the sustenance of biological homeostasis. In addition, it is related to several diseases, aging and carcinogenesis. The sample PG was extracted and fractionated to five different types; butanol (PGMB), ethylacetate (PGMEA), ethylether (PGMEE), hexane (PGMH) and methanol (PGMM). The oxidation indices of PGMEA and PGMEE fractions in oxidized dilinoleoylphosphatidylcholine (DLPC) liposomes had stronger antioxidant activities than that of ${\alpha}$-tocopherol and were similar to antioxidant activities compared with butylated hydroxy toluene (BHT), a well-known potent antioxidant, in oxidized DLPC liposomes. The oxidation indices of PGMM extract, PGMB and PGMH fractions exhibited weak antioxidant activity compared with ${\alpha}$-tocopherol in oxidized DLPC liposomes. The oxidation indiex of PGMEE fractions added with vitamin C showed even strong antioxidant activity in the oxidized DLPC liposomes. The oxidation activity of BHT with vitamin C also proved to be stronger than BHT without vitamin C. Therefore vitamin C evidently helps to improve the effect of antioxidant in DLPC liposomes. These results indicate that potentially bioactive substances in PGMEE fraction has a function as potent antioxidant against phospholipid membrane oxidation.

• Archives of Pharmacal Research
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• v.28 no.5
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• pp.626-635
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• 2005

Liposome as a carrier of topotecan (TPT), a promising anticancer drug, has been reported in attempt to improve the stability and antitumor activity of TPT. However, the biodistr ibution pattern of TPT liposome in vivo and PEG-modified liposome containing TPT have not been studied systemically. In this paper, the in vitro stability and in vivo biodistribution behavior of several liposomes containing TPT with different lipid compositions and PEG-modification were studied. Compared with the 'fluid' liposome (S-Lip) composed of soybean phosphatidylcholine (SPC), the 'solid' liposome (H-Lip) composed of hydrogenated soybean phosphatidylcholine HSPC decreased the leaking efficiency of TPT from liposome and enhanced the stability of liposome in fetal bovine serum (FBS) or human blood plasma (HBP). The results of biodistribution studies in S$_{180}$ tumor-bearing mice showed that liposomal encapsulation increased the concentrations of total TPT and the ratio of lactone form in plasma. Compared with free TPT, S-Lip and H-Lip resulted in 5- and 19- fold increase in the area under the curve (AUC$_{0\rightarrow\propto}$), respectively. PEG- modified H-Lip (H-PEG) showed 3.7-fold increase in AUC$_{0\rightarrow\propto}$ compared with H-Lip, but there was no significant increase in t$_{1/2}$ and AUC$_{0\rightarrow\propto}$ for PEG-modified S-Lip (S-PEG) compared with S-Lip. Moreover, the liposomal encapsulation changed the biodistribution behavior, and H-Lip and H-PEG dramatically increased the accumulation of TPT in tumor, and the relative tumor uptake ratios were 3.4 and 4.3 compared with free drug, respectively. There was also a marked increase in the distribution of TPT in lung when the drug was encapsulated into H-Lip and H-PEG. Moreover, H-PEG decreased the accumulation of TPT in bore marrow compared with unmodified H-Lip. All these results indicated that the membrane fluidity of liposome has an important effect on in vitro stability and in vivo biodistribution pattern of liposomes containing TPT, and PEG-modified 'solid' liposome may be an efficient carrier of TPT.

• KSBB Journal
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• v.29 no.1
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• pp.36-41
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• 2014

Skin disease is one of the most common diseases and its incidence is increasing dramatically in modern society. Specially, many attempts have been made to treat chronic skin inflammation diseases, such as psoriasis and atopic dermatitis, but effective therapies for the immune cell-mediated skin diseases, including psoriasis and atopic dermatitis have not been developed. Until recently, several drug candidates which were claimed to be effective for skin diseases have been reported, but most of them are not used to treat chronic skin disease. Especially, Psoriasis is characterized by excessive growth and aberrant differentiation of keratinocytes, but is fully reversible with appropriate therapy. The trigger of the keratinocyte response is thought to be activation of the cellular immune system, with T cells and various immune-related cytokines. Formation of new blood vessels starts with early psoriatic changes and disappears with disease clearance. Several angiogenic mediators are up-regulated in psoriasis development. Contact- and mediator-dependent factors derived from keratinocytes, mast cells and immune cells may contribute to the strong blood vessel formation of psoriasis. New technologies and experimental models provide new insights into the role of angiogenesis in psoriasis pathogenesis. TMP and its derivatives themselves effectively inhibited in vitro cell migration, tube formation, and the expression of angiogenic factors. However, TMP and its derivatives induced side effects including hemolysis and local side effects. Therefore, in an attempt to reduce the toxicity and the undesirable side effects of TMP and derivatives, a liposomal formulation was prepared and tested for its effectiveness. TMP and derivatives liposomes retained the effectiveness of TMP in vitro while side effects were reduced. These results support the conclusion that TMP effectively inhibits in vitro angiogenesis, with the possibility that use as a psoriasis relief agent.

• Journal of the Korean Society of Food Science and Nutrition
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• v.30 no.4
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• pp.646-650
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• 2001

In this study, we investigated the thermotropic behavior of Daucus carota L. (DCS) extracts in phosphatidylcholine(PC) liposomes using high-sensitivity differential scanning calorimetry (nano-DSC). We used dipalmitoylphosphatidylcholine (DPPC) bilayers which made most stable liposomes among the other phosphatidylcholine. The sample DCS was extracted and fractionated to four different types, hexane(DCSMH), ethylacetate (DCSMEA), butanol (DCSMB) and aqueous(DCSMA) fractions. Compared to the other fractions of Daucus carota L., the DCSMH and DCSMEA fractions markedly affected the thermotropic properties of DPPC liposomes, broadened and shifted the thermograms of transition to lower temperatures. The incorporation of DCSMH and DCSMEA in DPPC liposomes were preferentially located in the hydrophobic core of DPPC bilayers, where it reduced the lipid packing orderness (cooperative unit) in the gel state compared to it in the liquid-crystalline state. These results suggest that the activities of the Daucus carota L. extracts to enhance the fluidity of the liposomal membrane have implication in their biological activities.