• Proceedings of the SCSK Conference
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• 2003.09b
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• pp.60-72
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• 2003

To investigate the effect of cholesterol in liposome on the stability of incorporated retinol, the physico-chemical experiments for various amounts of cholesterol-containing liposomes were performed. Liposome with retinol containing cholesterol was prepared as multilamella vesicles(MLVs) by dehydration/rehydration method. The incorporation efficiency of retinol into liposome was maximized as 99.31 % at 50:50 (phosphatidylcholine/cholesterol) at pH 9. The stability of incorporated retinol at low storage temperature was enhanced with increasing cholesterol content than at high storage temperature. For example, incorporated retinol in liposome at glycine buffer(pH 9} was degraded slowly during storage at 4. The degradation of retinol in liposomes was slower at pH 9 than at pH 7. These results supported that cholesterol in liposome increased largely the stability of incorporated retinol.

• Journal of the Korean Chemical Society
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• v.48 no.6
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• pp.616-622
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• 2004

Liposome powders were prepared by a freeze-drying method for the application to the field of drug carrier. The effect of maltose as a liposome stabilizer was studied on the stability and the drug-loading efficiency of the freeze-dried liposome powders. The particle size of liposomes before and after freeze-drying was determined to evaluate the liposome stability. The drug-loading efficiency was measured by Fluorescence spectrophotometer using calcein as a model drug. When maltose was added after the preparation of the liposomes, the liposomes was stable, compared to the case of maltose addition at the hydration procedure. By the addition of maltose, the liposome was stable for 30 days at $4{\sim}37^{\circ}C$, while the particle size of the liposome without maltose increased with time. The liposome showed relatively high stability when the maltose/lipids molar ratio was 3 and 6.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.27 no.1
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• pp.29-42
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• 2001

We had prepared MLV liposome with Hibiscus Esculentus Ext.(HEE) which have fluorescent light in order to evaluate its percutaneous absorption about hairless rat skin. Then we investigated particle size of MLV using confocal laser scanning microscope(CLSM) and transmission electron microscope(TEM), respectively. Stability of MLV liposome and penetration of MLV liposome to hairless rat skin was measured by CLSM. As a result of experiments, MLV was globular shape and the rage of particle size was 0.3-0.5$\mu\textrm{m}$ mostly. Cream-type MLV had high stability comparatively. When we treated with MLV to rat skin, skin penetration was enhanced, especially, the optimum concentration of MLV on penetration to rat skin was 10%. Optimum penetration time was 6hr-12hr. And MLV-type HEE was more effective on percutaneous absorption than HEE-cream or liposome-type HEE.

• Applied Biological Chemistry
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• v.42 no.3
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• pp.205-209
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• 1999

Cholesterol plays an important role in various physiological responses and membrane stability. To investigate the effect of cholesterol in liposome on the stability of encapsulated ascorbic acid, the physico-chemical experiments using various amounts of cholesterol-containing liposomes were performed. The encapsulation efficiency of ascorbic acid was decreased with increasing cholesterol content in liposome, whereas size of liposome was increased. Furthermore, the stability of encapsulated ascorbic acid was increased with increasing the content of cholesterol. The stability was not affected by pH. Encapsulated ascorbic acid in liposome stored at $37^{\circ}C$ was rapidly oxidized compared to those stored at $4^{\circ}C$. These results suggest that cholesterol in liposome affects largely to the stability of encapsulated ascorbic acid.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.37 no.1
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• pp.55-60
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• 2011

In this study, DOPC liposomes were prepared with distilled water, phosphate buffer and phosphate buffered saline to evaluate the effects of salt on the stability of DOPC liposome. The changes in physical properties (likeparticle size and zeta potential) of liposome were measured after adding the salt. Liposomes were diluted 40 times and 80 times with hydration solvent to confirm the effect of dilution. Consequently, the stability of liposome was maintained up to 40 times dilution with hydration solvent. The liposome that prepared with distilled water was diluted with distilled water, phosphate buffer and phosphate buffered saline, and the liposome that prepared with phosphate buffer was diluted with phosphate buffer and phosphate buffered saline to evaluate the salt-induced changes in particle size and zeta potentia. As results, the particle size increased slightly and zeta potential became closer to 0 when the salt concentration was increased. In conclusion, particle size and zeta potential of liposome could be reasonable factors to evaluate the stability of liposome. In addition, we suggest that salt concentration of hydration solvent has a significant effect on the stability of liposome.

• 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.

• Journal of Pharmaceutical Investigation
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• v.40 no.3
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• pp.187-192
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• 2010

We aimed to evaluate the effect of temperature, pH, and light conditions on the stability of porcine placental extract (PPE)-loaded liposomes with different surface charges. The size distribution profiles and in vitro release patterns were investigated by dynamic light scattering method and spectrophotometry. The stability of PPE-loaded liposomes was affected by the surface charges of the liposomes. As compared to neutral and anionic liposomes, cationic liposome formulations showed significantly lower physical stability. At the test storage conditions of different temperatures and pHs, the mean sizes of cationic PPE-loaded liposomes substantially increased. In contrast, neutral and anionic liposomes did not reveal significant changes in mean sizes upon various storage conditions. The neutral and anionic liposomes showed no significant differences in the release profiles of PPE after storage at various temperatures and pHs. Our results indicate that anionic and neutral liposome compositions might be more suitable for the formulations of PPE providing the higher stability.

• 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.

• Preventive Nutrition and Food Science
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• v.8 no.3
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• pp.235-238
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• 2003

We investigated the effect of the phase transition temperature (T$_{c}$) of phospholipid in liposomes on the stability of incorporated retinol. Two kinds of phospholipid which have different T$_{c}$, L- $\alpha$ -dimyristoyl phosphatidyl choline (DMPC, T$_{c}$=22$^{\circ}$C) and D,L- $\alpha$ -dipalmitoyl phosphatidyl choline (DPPC, T$_{c}$=42$^{\circ}$), were used to prepare liposomes. Liposome with retinol was prepared as multilamella vesicles (MLVs) by the dehydration/rehydration method. The incorporation efficiency of retinol into liposomes prepared from DMPC and DPPC were 99.89$\pm$0.08% and 99.97$\pm$0.03, respectively. The average size of liposomes from DPPC were greater than that of DMPC. Two kinds of liposomes in phosphate buffer (10 mM, pH 7.0) were stored at 15, 30, and 5$0^{\circ}C$, and stability of incorporated retinol was analyzed. The stability of retinol in DMPC liposome was decreased, whereas the stability in DPPC liposome was increased as temperature increased, although the overall protection effect of liposome on the incorporated retinol was greater in DMPC liposomes than in DPPC liposomes.posomes.

• Journal of Pharmaceutical Investigation
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• v.40 no.2
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• pp.85-90
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• 2010

Docetaxel-loaded liposomes were prepared by emulsion-solvent evaporation method, then coated with chitosan at room temperature and lyophilized. This system was designed in order to improve solubility and stability of docetaxel in the GI tract for oral drug delivery. The solubilizing effect of some frequently used solubilizers and/or liposome was determined. Among the results docetaxel-loaded liposomes prepared with 0.5% TPGS as a solubilizer showed 100-fold higher solubility than docetaxel. In a stability test, mean particle size of different liposome formulations was measured by a particle size analyzer in simulated gastric fluid (SGF) and in simulated intestinal fluid (SIF). The particle size of uncoated liposomes was significantly increased compared with that of chitosan-coated liposomes in SGF, however, there was no significant difference between coated and uncoated liposome in SIF. It is evident that chitosan-coated liposomes were more stable in GI conditions. The release characteristics of docetaxel-loaded liposomes were also investigated in three buffer solutions (pH 1.2, 4.0, 6.8). Docetaxel release did not occur in pH 1.2 for 4 hrs. However, in pH 4.0 and 6.8 conditions, docetaxel was gradually released over 24 hrs as a sustained release. It seems that aggregation and precipitation of particles by electrostatic interaction might protect docetaxel from being released. In Conclusion, the results from this study show that the chitosan-coated liposomes may be useful in enhancing solubility and GI stability of docetaxel.