• Biomolecules & Therapeutics
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• v.10 no.2
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• pp.104-113
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• 2002

The effects of enzyme inhibitors and penetration enhancers on the permeation of leucine enkephalin (Leu-Enk) and its synthetic analog, [${D-ala}^2$]-leucine enkephalinamide (YAGFL) across the nasal, rectal and vaginal mucosae were evaluated. Enzyme inhibitors and penetration enhancers employed for Leu-Enk permeation study were amastatin(AM), thimerosal(TM) and ethylenediaminetetraacetic acid disodium salt(EDTA), and sodium taurodihydrofusidate (STDHF). Those for YAGFL permeation study were TM, benzalkonium chloride(BC) and EDTA, and STDHF, sodium deoxycholate(SDC), sodium glycholate(SGC), glycyrrhizic acid ammonium salt (GAA), L-$\alpha$-Iysophosphatidylcholine(LPC) and mixed micelle (MM, STDHF: linoleic acid = 15 mM : 5 mM). The addition of TM alone on the donor and receptor solutions for Leu-Enk permeation study across all the three kinds of mucosae failed to inhibit the degradation; it completely degraded in 6 hrs, and no permeation occurred. However, with addition of three kinds of inhibitors together, the fluxes across nasal, rectal and vaginal mucosae were $\20.7{pm}2.5$>/TEX>,$\0.3{pm}0.05$>/TEX> and $\1.4{pm}0.5$ $\mu$\mid$textrm{m}$/$\textrm{cm}^2$/hr, respectively. Moreover, the addition of STDHF in the presence of the above three inhibitors enhanced permeation across nasal, rectal and vaginal mucosae 1.3, 15 and 1.3 times, respectively. YhGFL also degraded in the donor and receptor solutions rapidly as time went. With mixed inhibitors of TM and EDTA, the percents of YAGFL remaining in the donor solutions facing nasal, rectal and vaginal mucosae were 69.7, 69.8 and 79.8%, respectively; the percent permeated increased to 10, 2.1 and 5.7%, respectively. The addition of STDHF in the presence of either BC/EDTA or TW/EDTA increased the permeation 2.2, 11.0 and 2.9 times, and 2.21, 14.0 and 2.7 times for nasal, rectal and vaginal mucosae, respectively. With SDC, SGC, GAA, LPC ud MM in the presence of TM/EDTA increased permeation; especially, they increased permeation across vaginal mucosae effectively, and the enhancement factors were 12.5, 7.6, 8.7, 5.7 and 5.5, respectively. The degradation extent of YAGFL was correlated with protein concentrations in the epidermal and serosal extracts. The flux of YAGFL across nasal mucosa increased dose-dependently.

• Journal of fish pathology
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• v.20 no.2
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• pp.119-127
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• 2007

Phosphoinositide-specific phospholipase Cδ (PLCδ) plays an important role in many cellular responses and is involved in the production of second messenger. The present study was conducted to characterize the catalytic and regulatory properties of the PLCδ of Misgurnus mizolepis (ML-PLCδ). The ML-PLCδ gene was cloned and expressed under according to the method of the previous report (Kim et al., 2004), and its recombinant protein was purified by successive chromatography using Ni2+-NTA affinity column. The recombinant ML-PLCδ showed a concentration-dependent PLC activity to phosphatidylinositol 4,5-bisphosphate (PIP2) or phosphatidylinositol (PI). Its activity was absolutely Ca2+-dependence, which was similar to mammalian PLCδ isozymes. The Ca2+ concentration yielding maximal activation of ML-PLCδ was 100 μM. However, the activity was decreased interestingly by a polyamine, such as spermine and spermidine. In vitro assay using cholate-micelle cell, ML-PLCδ activity was inhibited in dose-dependent manner by sphinogosine but increased by phosphocholine . In the lipid-binding assay, ML-PLCδ was strongly bound to LPA, PI(3)P, PI(4)P, PI(5)P, PI(3,5)P2, PI(4,5)P2, PI(3,4,5)P3 and PA, but it showed the low affinity to S1P, PI(3,4)P2 and PS. Taken together our results, it is suggested that the general catalytic and regulatory properties of ML-PLCδ are similar with those of mammalian PLCδ1 isozymes, but the N-terminal extended piscine phospholipase Cδ1 (ML-PLCδ) might reflect some distinctions in regulatory properties and inositol-lipid binding specificity between piscine ML-PLCδ and mammalian PLCδ isozymes.

• Journal of Pharmaceutical Investigation
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• v.27 no.4
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• pp.287-293
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• 1997

To make a stable o/w emulsion, the effects of egg lecithin as an emulsifier and polyvinylpyrrolidone (PVP) as an auxiliary emulsifier on the physical stability of emulsion were investigated. The oil-in-water emulsion system was manufactured by microfluidizer and evaluated the physical stability. Average particle size and size distribution of emulsion was measured by dynamic light scattering analyzer and interfacial tension was measured. From the interfacial tension tested, critical micelle concentration of the egg lecithin was 0.1 %w/v and optimal concentration for the preparation of emulsion was 1.0 %w/v. The mean particle size was about $0.2\;{\mu}m$ which was suitable for injections. The short-term accelerated stability studies were conducted by centrifugation, freeze-thaw method and shaking of the emulsion samples. The addition of PVP was caused the reduction in the particle size and improved the physical stability of emulsion. These results suggested that a mixed interfacial film comprising the egg lecithin and PVP was formed at the o/w interface and it was effective in preventing phase separation under thermic or mechanical stress. We used antineoplaston A10 (A10) as a model drug which is peptide and amino acid derivative having a action to the living organism against the development of neoplastic growth by a nonimmunological progress. It has a poor solubility in water and there may be a difficulty in formulation of A10. Emulsion formulation study about A10 was performed. Solubility of A10 in emulsion was about five times as high as that in water. From the results of solubility and partition coefficient, almost A10 molecules in o/w emulsion exist in the interface between oil and water.

• Journal of Pharmaceutical Investigation
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• v.39 no.2
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• pp.97-106
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• 2009

Although lovastatin (LS) is widely used in the treatment of hypercholesterolemia, its bioavailability is known to be around 5%. This study was aimed to increase the solubility and dissolution-permeation rates of LS using solid dispersions (SDs) with bile salts. The solubilities of LS in water, aqueous bile salt solutions and non-aqueous vehicles were determined, and effects of bile salts on the cellulose or duodenal permeation of LS from SDs were evaluated using a horizontal permeation system. SDs were prepared at various ratios of LS to carriers, such as sodium deoxycholate (SDC), sodium glycocholate (SGC) and/or 2-hydroxypropyl-$\beta$-cyclodextrin (HPCD). The addition of bile salts (25 mM) in water increased markedly the solubility of LS by the micellar solubilization. Some non-aqueous vehicles were effective in solubilizing LS. From differential scanning calorimetric studies, it was found that the crystallinity of LS in SDs disappeared, indicating a formation of amorphous state. The SDs showed markedly enhanced dissolution compared with those of their physical mixtures (PMs) and drug alone. In the dissolution-permeation studies using a cellulose membrane, the donor and receptor solutions were maintained as a sink condition using pH 7.0 phosphate buffer containing 0.05% sodium lauryl sulfate (SLS). The flux of LS alone was nearly same as that of LS-SDC-HPCD (1:3:6) PM. However, the flux of LS-SDC-HPCD (1:3:6) SD slightly increased compared with drug alone and PM, suggesting that entrapment of LS in micelles does not significantly hinder the permeation across cellulose membrane. In the dissolution-duodenal permeation studies using a LS-HPCD-SDC (1:3:6) SD, the addition of various bile salts in donor solutions (25 mM) enhanced the permeation of LS markedly, and the fluxes were found to be $0.69{\pm}0.41$, $0.87{\pm}0.51$, $0.84{\pm}0.46$, $0.47{\pm}0.17$ and $0.68{\pm}0.32{\mu}g/cm^2/hr$ for sodium cholate (SC), SDC, SGC, sodium taurodeoxycholate (STDC) and sodium taurocholate (STC), respectively. The stepwise increase of donor SGC concentration increased the flux dose-dependently. From the relationship of donor SGC concentration and flux, the concentration of SGC initiating the permeation across the duodenal mucosa was calculated to be 11.1 mM, which is nearly same as the critical micelle concentration (CMC, 11.6 mM) of SGC. However, with no addition of bile salts and below CMC, the permeation was very limited and irratic, indicating that LS itself is very poor permeable. Higher protions of bile salt in SD such as LS-SDC or LS-SGC (1 : 49 and 1 : 69) showed highly promoted fluxes. In conclusion, SD systems with bile salts, which may form their micelles in intestinal fluids, might be a promising means for providing enhanced dissolution and intestinal permeation of practically insoluble and non-absorbable LS.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.15 no.6
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• pp.4032-4038
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• 2014

Vegetable fatty acid solid soap requires a drying process for moisture evaporation and hardness after being manufactured through saponification. Although the soap is manufactured by mixing additives mainly from natural ingredients, existing studies have focused primarily on the usability of vegetable solid soap. Consequently, research into the physical properties of vegetable fatty acid solid soap mixed with natural ingredients has been unsatisfactory. Therefore, this study attempted to compare and observe the changes in the physical properties (pH, surface tension, critical micelle concentration, and cleansing power) of solid soap in accordance with the drying period and additives (tea tree E.O and $TiO_2$) using pH paper, the Du Nouy measurement method, sedimentation method, and ultrasound washer. Regardless of the mixture with additives, vegetable fatty acid solid soap showed the same pH, and there was no change in the pH while maintaining pH 8 beginning from the $2^{nd}$ weeks to $12^{th}$ weeks of drying. In addition, as a result of measuring the surface tension and CMC, regardless of the drying period, only the soap added with $TiO_2$ showed an even value of 62.5mg/L, whereas the other soap specimens showed a decline in CMC to 25mg/L on the fourth week of drying. As a result of measuring the detergency, the removal efficiency of vegetable fatty acid solid soap mixed with tea tree E.O and $TiO_2$ and dried for four weeks was 4.50~4.65%, which was higher than that of the vegetable fatty acid solid soap without additives (3.62~3.92%).

• Journal of the Korean Applied Science and Technology
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• v.37 no.2
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• pp.250-259
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• 2020

The solubilization constant (K_s) was determined by the UV-Vis method to investigate the interaction between organic matter (solubilized substance) and surfactant in solubilization. Solubilization constants and thermodynamic functions, according to the hydrophobic interaction between organic mater (4-alkylanilines with different alkyl substituent length) and cationic surfactants (DTAB, TTAB, and CTAB, having different hydrophobic lengths), were measured and calculated at various temperatures and compared with each other. As a result, the hydrophobic interactions between organic matters and cationic micelles increased with increasing the chain length of solute's substituent as well as surfactant's hydrophobe. However, the hydrophobic effect by the alkyl substituent of organic matter was greater than the hydrophobic effect by the surfactant. In addition, the results of the calculated thermodynamic functions showed that 4-alkylaniline was solubilized at the deep place in the micelle and its solubilization was greatly dependent on both the hydrophobic effects of organic matter and surfactant. At the calculated iso-structural temperature, the difference between the maximum and minimum values was less than 1K within the experimental conditions.

• Korean Chemical Engineering Research
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• v.50 no.6
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• pp.960-968
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• 2012

In this study, the measurement of physical properties of 3 different ethylene oxide adducted zwitterionic surfactants were measured such as critical micelle concentration, surface tension, interfacial tension, contact angle, viscosity and foam stability. Also, the dual function characteristics of the zwitterionic surfactants were investigated by determining an isoelectric point, which were obtained using zeta potential measurement and QCM (quartz crystal microbalance) experiments. The isoelectric point of the synthesized zwitterionic surfactant determined by zeta potential measurement was close to that obtained by QCM experiment and both results have shown almost the same trend as that determined by the frictional property measured using an automated mildness tester. In particular, it has been observed that all three surfactants used during this study provide better softening effect at a pH of neutral condition than at an acidic or an alkaline condition. This result indicates that the synthesized surfactants act as a cationic surfactant at a pH of neutral condition and thus provide good softening effect during a rinsing cycle in the detergency process.

• Korean Chemical Engineering Research
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• v.52 no.2
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• pp.219-225
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• 2014

In this study, effect of cosurfactant on the solubilization rate of n-octane, n-decane and n-dodecane oil was performed by micellar solutions of polymeric nonionic surfactant Pluronic L64($EO_{13}PO_{30}EO_{13}$) at room temperature. It has been found that the solubilization rate of a hydrocarbon oil was enhanced with an increase in both chain length and amount of alcohol added. In case of addition of a short chain alcohol such as 1-butanol, the solubilization rate of a hydrocarbon oil was slightly increased since most of alcohol molecules remained in an aqueous surfactant solution. On the other hand, the addition of a relatively long chain alcohol such as 1-hexanol and 1-octanol produced a big increase in solubilization rate of a hydrocarbon oil mainly due to incorporation of alcohol molecules into micelles and thus producing more flexible micellar packing density. Dynamic interfacial tension measurements showed the same trend found in solubilization rate measurement. Both interfacial tension value at equilibrium and time required to reach equilibrium decreased with an increase in chain length of an alcohol.

• Journal of the Korean Chemical Society
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• v.48 no.2
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• pp.195-202
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• 2004

Micellar catalysis is an essential part of theoretical and experimental curricular. The sodium dodecylsulfate (SDS) catalyzed reaction between glycine and potassium permanganate in acidic medium is an ideal kinetic experiment for the secondary and undergraduate physical chemistry laboratory, to show the effect of micellar catalysis on rate of the reaction. The reaction is conducted both with and without SDS to observe the rate enhancement in the presence of surfactant. To show surfactant catalysis a plot between k and [SDS] is plotted. As surfactant catalysis is observed even before the critical micelle concentration of SDS, this pre-micellar catalysis can be understood in the light of positive co-operativity. The value of positive cooperative index (n) has been found to be 2.37. Further, dependence of the reaction rate on substrate and oxidant concentrations is also discussed. The reaction follows pseudo-first-order kinetics. The overall reaction is second order, with first-order dependence on both glycine and permanganate concentrations. The theory of surfactant catalysis is also discussed. With the conditions specified in the experiment, total reaction times are in 3~4 hours lab session, thus allowing several data sets to be acquired in a single laboratory period. Preparation of solutions and procedure is also given in detail.

• Bulletin of the Korean Chemical Society
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• v.35 no.8
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• pp.2342-2348
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• 2014

Poly(lactic-co-glycolic acid) (PLGA) were grafted to both ends of Pluronic$^{(R)}$ F68 ($(EO)_{75}(PO)_{30}(EO)_{75}$) triblock copolymer to produce poly{(lactic acid)$_m$-co-(glycolic acid)$_n$}-b-poly(ethylene oxide)$_{75}$-b-poly(propylene oxide)$_{30}$-b-poly(ethylene oxide)$_{75}$-b-poly{(lactic acid)$_m$-co-(glycolic acid)$_n$} (PLGA-F68-PLGA) pentablock copolymers. Molecular weights of PLGA blocks were controlled and five kinds of pentablock copolymers with different PLGA block lengths were synthesized using in-situ ring-opening polymerization of D,L-lactide and glycolide with tin(II) 2-ethylhexanoate ($Sn(Oct)_2$) catalyst. PLGA-F68-PLGA pentablock copolymers were characterized by $^1H$- and $^{13}C$-NMR, GPC, and TGA. The numbers (2m, 2n) of repeating units for lactic acid and glycolic acid inside PLGA segments were obtained as (48, 17), (90, 23), (125, 40), (180, 59), and (246, 64), with $^1H$-NMR measurement. From NMR data, the resultant molecular weights were determined in the range of 12,700-29,700, which were similar to those obtained from GPC. Polydispersity index was increased in the range of 1.32-1.91 as the content of PLGA blocks increased. TG and DTG thermograms showed discrete degradation traces for PLGA and F68 blocks, which indicate the weight fractions of PLGA blocks in pentablock copolymers can be calculated by TG profile and it is possible to remove PLGA block selectively. Hydrodynamic radius and radius of gyration of pentablock copolymer micelle were obtained in the range of 46-68 nm and 31-49 nm, respectively, in very dilute (i.e. 0.005 wt %) aqueous solution of THF:$H_2O$ = 10:90 by volume at $25^{\circ}C$.