• Biomolecules & Therapeutics
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• v.19 no.1
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• pp.109-117
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• 2011

In this work, we have investigated the effect of polyoxyethylene alkyl ester nonionic surfactants on percutaneous permeation enhancement of a model drug, ketoprofen. We also investigated the mechanism involved in the enhancement using impedance and solubility measurement. Three groups of nonionic surfactants with different ethylene oxide content were studied. The permeation results showed that all surfactants enhanced the percutaneous absorption, irrespective of the molecular weight. The permeation results from PEG-45 monostearate (PEGMS45) were rather unexpected. Impedance and solubility results indicate that the mechanism involved in the enhancement of permeation by PEG-10 monooleate (PEGMO10) and PEGMS45 is rather different. The results from PEGMS45 suggest that it could be a potential candidate as a skin penetration enhancer with high molecular weight, which may poses less skin irritation and systemic side effect than the smaller surfactant molecules. Overall, this work provided some useful information on percutaneous transport enhancement and the mechanistic insights involved in skin permeation for these nonionic surfactants.

• Journal of Korea Soil Environment Society
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• v.5 no.3
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• pp.55-64
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• 2001

Many organochlorine pesticides are persistent in the environment and have a tendency to bioaccumulate significantly through food chains. Aquatic environments are particularly more affected because the pesticides applied to agriculture systems are eventually carried into water bodies, through surface runoff, rivers, and groundwater flow. The objective of this paper is to study the effect of the coexistence of a heavy metal on the solubility enhancement of the two representative organochlorine pesticides, lindane and dieldrin, by humic acids. The solubility enhancement of pesticides by humic acid in a single system was compared with that in a binary system. The extent of solubility enhancement of lindane by humic acids was constant. while that of dieldrin by humic acids increased. Also, the solubility enhancement of dieldrin by humic acid with Pb decreased than that by humic acid without Pb.

• Journal of Microbiology and Biotechnology
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• v.16 no.5
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• pp.791-794
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• 2006

Cyclosophoraose (cyclic $\beta-(1,2)-glucan$, Cys) isolated from Rhizobium meliloti, a soil microorganism, was used as a solubility enhancer for flavonoids. The complexes of the cyclic oligosaccharide with flavonoids were confirmed through $^1H$ nuclear magnetic resonance (NMR) spectroscopic analysis. Flavonoids solubilized by Cys were quantitatively analyzed through high-performance liquid chromatography (HPLC). Among the flavonoids tested, the solubility of naringenin was greatly enhanced by Cys, compared with other compounds. The solubility of naringenin was enhanced about 7.1-fold by adding 10 mM Cys, compared with a control. $^1H$ NMR spectroscopic analysis indicated that the H-6 and H-8 protons, which are located on the A ring of naringenin, were greatly shifted upfield upon the complexation with Cys. This result suggested that Cys showed a regioselective interaction with the naringenin molecule upon the complexation, resulting in the solubility enhancement of naringenin.

• Journal of Korean Society of Environmental Engineers
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• v.22 no.4
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• pp.755-764
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• 2000

Fate and transport of hydrophobic organic contaminants can be influenced by naturally-existing humic substances and surfactants applied to wash polluted soils in the subsurface environment. The objective of this paper is to study the solubility enhancement of four PAHs (polycyclic aromatic hydrocarbon) and p,p'-DDT in humic acid and surfactant solutions. As the number of aromatic ring is increased, the extent of solubility enhancement of PAHs by humic acid increased. Although the hydrophobicity of p,p'-DDT was the largest among five organic compounds used, the extent of solubility enhancement of p,p'-DDT by humic acid was lower than that of pyrene. In case of anionic surfactants, the extent of the increased solubility of five organic compounds by SDS and SDDBS was increased linearly, but the extent of the increased solubility of p,p'-DDT by MADS-12 was lower than that of perylene.

• Archives of Pharmacal Research
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• v.18 no.1
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• pp.22-26
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• 1995

The solubility and dissolution rate of naproxen (NPX) complexed with 2-hydroxypropyl-.betha.-cyc-lodextrin (2-HP.betha.CD) using coprecipitation, evaporation, freeze-drying and kneading method were investigated. Solubility of NPX linearly increased (correlation cefficient, 0.995) as $2-HP\betaCD$ concentraction increased, resutling in $A_l$ type phase solubility curve. Inclusion complexes prepared by four different methods were compared by different methods were compared by dfferential scanning calorimetry(DSC). The NPX showed sharp endothemic peak around $156^{\circ}C$ but inclusion complexes by evaporation, freeze-drying and kneading method showed very broad peak without distinct phase transtion temperature. In contrast, inclusion complex prepared by coprecipitation method resulted in detectable peak around $156^{\circ}C$ which is similar to NPX, suggesting incoplete formation of indusion co plex. Dissolution rate of inclusion complexes prepared by evaporation, frezz-drying and kneding except coprecipitation method was largely enhanced in the simultaed gastric and intestinal fluid when compared to NPX powder and commercial $NA-XEN^\registered$tablet. However, about 65% of NPX in gstric fluid. in case of inclusion complex prepared by coprecipitation method, formation of inclusion complex appeared to be incoplete, resulting in no marked enhancement of dissolution rate. From these findings, inclusion complexes of poorly water-soluble NPX with $2-HP\betaCD$ were useful to increase soubility and dissolution rate, resting in enhancement of bioavailability and minimization of gastrointestinal toxicity of drug upon oral administration of inclusion complex.

• Journal of Pharmaceutical Investigation
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• v.25 no.1
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• pp.31-36
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• 1995

Solid dispersions and inclusion complex were prepared for the enhancement of solubility and dissolution rate of poorly water-soluble ibuprofen(IPF) as a model drug. Polyethylene glycol 4000(PEG4000) and polyvinylpyrrolidone(PVP) were used for the preparation of solid dispersion. $2-Hydroxypropyl-{\beta}-cyclodextrin(2-HP{\beta}CD)$ was also used for the preparation of inclusion complex. The solubility of IPF increased as the concentration of PEG4000, PVP and $2-HP{\beta}CD$ increased. Solubilization capacity of $2-HP{\beta}CD$ was increased about 10 times when compared to PEG 4000 and PVP. The dissolution rate of drug from solid dispersions and inclusion complex in the simulated gastric fluid was enhanced when compared to pure IPF and commercial $BR4^{\circledR}$ tablet as a result of improvement of solubility. In case of solid dispersions, dissolution rate of drug was proportional to polymer concentration in the formulation. The marked enhancement of dissolution rate of drug by inclusion complexation with $2-HP{\beta}CD$ was noted. However, dissolution rate of drug from solid dispersions and inclusion complex in the simulated intestinal fluid was not significant because IPF was readily soluble in that condition. From these findings, water-soluble polymers and cyclodextrin were useful to improve solubility and dissolution rate of poorly water-soluble drugs. However, easiness and reliability of preparation method, scale-up and cost of raw materials must be considered for the practical application of solid dispersion and inclusion complex in pharmaceutical industry.

• YAKHAK HOEJI
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• v.28 no.3
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• pp.161-167
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• 1984

To improve the solubility properties of indomethacin, a poorly water-soluble drug, some attempts were made with surfactants, such as sodium deoxycholate, sodium laurylsulfate and polysorbate-80. The enhancement effect in solubility was found to be due to the micellar solubilization and dependent on the concentration of surfactants, pH and temperature. The mechanism of interaction was suggested to be attributed to the formation of mixed micelles between the drug and solubilizers.

• Environmental Engineering Research
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• v.13 no.1
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• pp.8-13
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• 2008

The extent of solubility enhancement by biosurfactant was examined at various pHs prior to the biodegradation experiments. The molar solubilization ratio (MSR) was calculated from the batch solubilization experiments and the highest MSR was detected at pH 5. The effect of the biosurfactant, rhamnolipids, on the phenanthrene mineralization in soil-water system was investigated. The strain 3Y was selected for the mineralization assay and large amounts of phenanthrene were degraded at neutral pH in soil-water system without the biosurfactant. The addition of 150 mg/L rhamnolipids showed no effect on mineralization of phenanthrene in soil-water system, and total mineralization rates after 6 weeks incubation at each pH showed no differences in presence and absence of rhamnolipids. Our result indicated that the toxic effect of rhamnolipids can disappear when soil particles exist, and also the enhanced solubility of phenanthrene does not work for mineralization enhancement in this soil-water system.

• Bulletin of the Korean Chemical Society
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• v.29 no.3
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• pp.590-594
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• 2008

The inclusion complexes of cyclodextrins (CDs) with flavones in aqueous solution were investigated by phase solubility measurements. The effect of b -cyclodextrin (b -CD), heptakis (2,6-di-O-methyl) b -cyclodextrin (DM-b -CD) and 2-hydroxypropyl-b -cyclodextrin (HP-b -CD) on the aqueous solubility of three flavones, namely, chrysin, apigenin and luteolin was investigated, respectively. Solubility enhancements of all flavones obtained with three CDs followed the rank order: HP-b -CD > DM-b -CD > b -CD, and besides, CDs show higher stability constant on luteolin than that on others flavones. 1H-nuclear magnetic resonance (NMR) spectroscopy and molecular modeling was used to help establish the model of interaction of the CDs with luteolin. NMR spectroscopic analysis suggested that A-C ring, and part of the B ring of luteolin display favorable interaction with the CDs, which was also confirmed by docking studies based on the molecular simulation. The observed augmentation of solubility of luteolin by three CDs was explained by the difference of electrostatic interaction of each complex, especially hydrogen bonding.

• Proceedings of the Korean Society of Soil and Groundwater Environment Conference
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• 2000.11a
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• pp.286-289
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• 2000

Surfactants have been extensively considered for decontamination of the subsurface polluted with hydrophobic organic compounds. Enhanced solubilization of naphthalene and phenanthrene in surfactant solution of SDDBS, MADS12 and DADS12 was studied for single compounds and their binary mixture. The order of increasing solubility enhancement of naphthalene and phenanthrene is SDDBS < MADS12 < DADS12. The solubility enhancement of phenanthrene is more than that of naphthalene because of the higher hydrophobicity. A synergistic effect on the solubilization of two PAHs was observed in the presence of another PAH.