• Journal of Ginseng Research
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• v.42 no.4
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• pp.512-523
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• 2018

Background: 20(S)-Protopanaxadiol (20S-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability, thereby enhancing its skin deposition. Thus, we optimized microemulsion (ME)-based hydrogel (MEH) formulations for the topical delivery of 20S-PPD. Methods: MEs and MEHs were formulated and evaluated for their particle size distribution, morphology, drug loading capacity, and stability. Then, the deposition profiles of the selected 20S-PPD-loaded MEH formulation were studied using a hairless mouse skin model and Strat-M membrane as an artificial skin model. Results: A Carbopol-based MEH system of 20S-PPD was successfully prepared with a mean droplet size of 110 nm and narrow size distribution. The formulation was stable for 56 d, and its viscosity was high enough for its topical application. It significantly enhanced the in vitro and in vivo skin deposition of 20S-PPD with no influence on its systemic absorption in hairless mice. Notably, it was found that the Strat-M membrane provided skin deposition data well correlated to those obtained from the in vitro and in vivo mouse skin studies on 20S-PPD (correlation coefficient $r^2=0.929-0.947$). Conclusion: The MEH formulation developed in this study could serve as an effective topical delivery system for poorly soluble ginsenosides and their deglycosylated metabolites, including 20S-PPD.

• The Korean Journal of Physiology and Pharmacology
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• v.12 no.1
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• pp.7-12
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• 2008

OLETF (Otsuka Long-Evans Tokushima Fatty) rats are characterized by obesity-related insulin resistance, which is a phenotype of type 2 diabetes. Sulfonylurea drugs or benzoic acid derivatives as inhibitors of the ATP-sensitive potassium $(K_{ATP})$ channel are commercially available to treat diabetes. The present study compared sulfonylurea drugs (glimepiride and gliclazide) with one of benzoic acid derivatives (repaglinide) in regard to their long-term effect on ameliorating insulin sensitivity in OLETF rats. Each drug was dissolved and fed with drinking water from 29 weeks of age. On high glucose loading at 45 weeks of age, response of blood glucose recovery was the greatest in the group treated with glimepiride. On immunohistochemistry analysis for the Kir6.2 subunit of $K_{ATP}$ channels, insulin receptor ${\beta}$-subunits, and glucose transporters (GLUT) type 2 and 4 in liver, fat and skeletal muscle tissues, the sulfonylurea drugs (glimepiride and gliclazide) were more effective than repaglinide in recovery from their decreased expressions in OLETF rats. From these results, it seems to be plausible that $K_{ATP}$-channel inhibitors containing sulfonylurea moiety may be much more effective in reducing insulin resistance than those with benzoic acid moiety. In contrast to gliclazide, non-tissue selectivity of glimepiride on $K_{ATP}$ channel inhibition may further strengthen an amelioration of insulin sensitivity unless considering other side effects.

• Polymer(Korea)
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• v.26 no.5
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• pp.680-690
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• 2002

Implantable biodegradable wafers were prepared with pamidronate -loaded poly (L-lactide-co-glycolide) (PLGA, 75 : 25 mole ratio by lactide to glycolide, molecular weight : 20000 and 90000 g/mole) by direct compression method for the sustained release of pamidronate to investigate the possibility for the treatment of bone resorption. Pamidronate-loaded PLGA powders were prepared by means of physical mixing and spray drying with the control of formulation factors and characterized by scanning electron microscope and X-ray diffractometer. The pamidronate-loaded PLGA powders fabricated into wafers by direct compression under the constant pressure and time at room temperature. These wafers were also observed for their structural characteristic, release pattern, and degradation pattern. The release rate of pamidronate increased with increasing their initial loading ratio as well as increasing wafer thickness. The molecular weight of PLGA affects the release pattern : the higher molecular weight of PLGA, the faster release rate. It can be explained that the higher viscosity of high molecular PLGA solution at same concentration tends to aggregate PLGA and pamidronate resulting in unstable pharmaceutical dosage form. This system had advantages in terms of simplicity in design and obviousness of drug release rate and nay be useful as an implantable dosage form for the treatment of aural cholesteatoma.

• The Korean Journal of Physiology and Pharmacology
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• v.25 no.5
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• pp.479-488
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• 2021

This study aimed to develop docetaxel (DTX) loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (DTX-NPs) and to evaluate the different pharmacological sensitivity of NPs to MCF-7 and MDA-MB-231 breast cancer cells. NPs containing DTX or coumarin-6 were prepared by the nanoprecipitation method using PLGA as a polymer and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) as a surfactant. The physicochemical properties of NPs were characterized. In vitro anticancer effect and cellular uptake were evaluated in breast cancer cells. The particle size and zeta potential of the DTX-NPs were 160.5 ± 3.0 nm and -26.7 ± 0.46 mV, respectively. The encapsulation efficiency and drug loading were 81.3 ± 1.85% and 10.6 ± 0.24%, respectively. The in vitro release of DTX from the DTX-NPs was sustained at pH 7.4 containing 0.5% Tween 80. The viability of MDA-MB-231 and MCF-7 cells with DTX-NPs was 37.5 ± 0.5% and 30.3 ± 1.13%, respectively. The IC₅₀ values of DTX-NPs were 3.92- and 6.75-fold lower than that of DTX for MDA-MB-231 cells and MCF-7 cells, respectively. The cellular uptake of coumarin-6-loaded PLGA-NPs in MCF-7 cells was significantly higher than that in MDA-MB-231 cells. The pharmacological sensitivity in breast cancer cells was higher on MCF-7 cells than on MDA-MB-231 cells. In conclusion, we successfully developed DTX-NPs that showed a great potential for the controlled release of DTX. DTX-NPs are an effective formulation for improving anticancer effect in breast cancer cells.

• Journal of radiological science and technology
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• v.45 no.2
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• pp.127-134
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• 2022

In order to overcome the image quality limitations of the conventional C-arm, a flat panel detector (FPD) is used to enhance spatial resolution, detective quantum efficiency, frame rate, and dynamic range. Three-dimensional (3D) visualized information can be obtained from C-arm computed tomography (CT) equipped with an FPD, which can reduce patient discomfort and provide various medical information to health care providers by conducting procedures in the interventional procedure room without moving the patient to the CT scan room. Unlike a conventional C-arm device, a C-arm CT requires different basic safety and essential performance evaluation criteria; therefore, in this study, basic safety and essential performance evaluation criteria to protect patients, medical staff, and radiologists were derived based on International Electrotechnical Commission (IEC) standards, the Ministry of Food and Drug Safety (MFDS) standards in Korea, and the rules on the installation and operation of special medical equipment in Korea. As a result of the study, six basic safety evaluation criteria related to electrical and mechanical radiation safety (leakage current, collision protection, emergency stopping device, overheating, recovery management, and ingress of water or particulate matter into medical electrical (ME) equipment and ME systems: footswitches) and 14 essential performance evaluation criteria (accuracy of tube voltage, accuracy of tube current, accuracy of loading time, accuracy of current time product, reproducibility of radiation output, linearity and consistency in radiography, half layer value in X-ray equipment, focal size and collimator, relationship between X-ray field and image reception area, consistency of light irradiation versus X-ray irradiation, performance of the mechanical device, focal spot to skin distance accuracy, image quality evaluation, and technical characteristic of cone-beam computed tomography) were selected for a total of 20 criteria.

• The Korea Journal of Herbology
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• v.32 no.5
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• pp.39-46
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• 2017

Objective : This study was designed to evaluate the hypoglycemic effects of Helianthus tuberosi Rhizoma extracts and its optimum Heat processing conditions Methods : We investigated the Salivary ${\alpha}$-amylase, pancreas ${\alpha}$-amylase and ${\alpha}$-glucosidase inhibitory activities of extracts from Steam Heated Helianthus tuberosi Rhizoma Ext. The inhibitory activities of a 50% EtOH extract of Steam Heated Helianthus tuberosi Rhizoma Ext against ${\alpha}$-glucosidases were evaluated in this study. Inhibiting these enzymes involved in the absorption of disaccharides significantly decreases the postprandial increase in blood glucose level after a mixed carbohydrate diet. Furthermore, the postprandial blood glucose lowering effect of Steam Heated Helianthus tuberosi Rhizoma Ext. was compared to a known type 2 diabetes drug(Acarbose(R)) in a mice model. Steam Heated Helianthus tuberosus L. Ext significantly reduced the blood glucose increase after glucose loading. Results : The results were confirmed by real-time PCR that after treated with Streptozotocin in L6 cells, induced expression of GLUT4, after the steamed Helianthus tuberosus L. Ext. treated, observed its expression was increased. Steam Heated Helianthus tuberosus L Ext treated 4 hours in L6 cells, cytotoxicity was measured in MTT assay. Its toxicity were 5.7%, 9% and 11.3% at the treatment concentration $12.5{\mu}g/m{\ell}$, $25{\mu}g/m{\ell}$, the $50{\mu}g/m{\ell}$ respectively. Conclusions : Overall, the results of this study indicate that Hypoglycemic effect of Helianthus tuberosi Rhizoma caused by the Steam heat treatment, the optimum Heat processing condition is steamming at $121^{\circ}C$ for 30 min, and it will provide the basis for developing a useful dietary supplement for controlling postprandial hyperglycemia.

• Journal of Applied Biological Chemistry
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• v.57 no.1
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• pp.73-81
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• 2014

The present study was carried out to assess exposure and risk to thiophanate-methyl wettable powder for agricultural worker during mixing/loading and application with power sprayer in green pepper, cucumber and apple fields. Dermal exposure was measured with patches, gloves, socks and masks, while inhalation exposure was evaluated with personal air pump and solid sorbent. Those methods were full validated before experiment. During mixing/loading, dermal exposure amount in green pepper, cucumber and apple fields was $24.0{\pm}6.7$, $4.5{\pm}1.5$ and $18.5{\pm}0.6mg$, corresponding to mean 0.007, 0.001 and 0.005% of prepared active ingredient, respectively. The major exposed part for mixer/loader was hands (78-92%). Dermal exposure amount for applicator in green pepper, cucumber and apple fields was $84.9{\pm}14.0$, $34.0{\pm}20.8$ and $30.7{\pm}9.1mg$, corresponding to mean 0.024, 0.016 and 0.013% of applied active ingredient, respectively. The main body parts of exposure in apple field were hands, while thighs and shins in other fields. Inhalation exposure amount in green pepper, cucumber and apple fields was $1.5{\pm}2.2$, $52.7{\pm}48.9$ and $4.0{\pm}4.9{\mu}g$ during mixing/loading and $0.2{\pm}0.1$, $23.2{\pm}12.4$ and $0.4{\pm}0.6{\mu}g$ for applicator, respectively. These results were suggested that main factors affecting dermal exposure were contact frequency to the plants, foliage density, hygienic behavior, work type, and working environment, while inhalation exposure was affected mainly by working environment, especially wind. In risk assessment, margin of safety for thiophanate-methyl in all cases was over 1. However, during application in green pepper field, margin of safety was close to 1.

• Journal of the Korean Chemical Society
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• v.50 no.3
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• pp.216-223
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• 2006

To increase the stability of liposomes in blood circulation, surface modification of liposomes by incorporating a lipid-polymer derivative in the lipid bilayer or conjugating a hydrophilic polymer to the liposomal surface has been developed. In this study, the comblike copolymer, poly(HEMA-co-HPOEM), having multiple polyethyleneoxide side chains was prepared by free radical polymerization of hydroxyethylmethacrylate (HEMA) and hydroxypolyoxyethylenemethacrylate (HPOEM) as vinyl monomers. Poly(HEMA-co-HPOEM) was conjugated to the liposomal surface and the characteristics of the modified liposomes in serum were investigated. Conjugation of poly(HEMA-co-HPOEM) to liposomes increased the particle size of the liposomes by 30 nm and decreased the absolute value of zeta potential of the liposomes by shielding the negative charge of liposomal surface. Loading efficiency of model drug, doxorubicin, in liposomes was about 90% and the efficiency was not affected by conjugation of poly(HEMA-co-HPOEM) to liposomes. The particle size of poly(HEMA-co-HPOEM)-conjugated liposomes in serum did not changed and the protein adsorption was lower than that of control liposomes or liposomes containing polyethyleneoxide-lipid derivative (PEG-liposomes). These results suggest that poly(HEMA-co-HPOEM) is efficient for the stabilization of liposomes in blood circulation.

• Macromolecular Research
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• v.13 no.3
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• pp.167-175
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• 2005

This review explores recent works involving the use of the self-assembled nanoparticles of bile acid-modified glycol chitosans (BGCs) as a new drug carrier for cancer therapy. BGC nanoparticles were produced by chemically grafting different bile acids through the use of l-ethyl-3-(3-dimethylaminopropyl)-carbodiimide (EDC). The precise control of the size, structure, and hydrophobicity of the various BGC nanoparticles could be achieved by grafting different amounts of bile acids. The BGC nanoparticles so produced formed nanoparticles ranging in size from 210 to 850 nm in phosphate-buffered saline (PBS, pH=7.4), which exhibited substantially lower critical aggregation concentrations (0.038-0.260 mg/mL) than those of other low-molecular-weight surfactants, indicating that they possess high thermodynamic stability. The SOC nanoparticles could encapsulate small molecular peptides and hydrophobic anticancer drugs with a high loading efficiency and release them in a sustained manner. This review also highlights the biodistribution of the BGC nanoparticles, in order to demonstrate their accumulation in the tumor tissue, by utilizing the enhanced permeability and retention (EPR) effect. The different approaches used to optimize the delivery of drugs to treat cancer are also described in the last section.

• Polymer(Korea)
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• v.31 no.3
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• pp.189-193
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• 2007

We developed the doxorubicin-loaded PLGA double-layered microspheres using relatively simple oil-in-water (O/W) solvent evaporation method for sustained release of doxorubicin and investigated the release behavior according to PLGA molecular weight and initial drug loading. The double-layered microsphere was characterized on the surface, the cross-section morphology, the behavior of doxorubicin release for 5 weeks by SEM and fluorescence spectrophotometer. Double-layered microspheres showed smooth surfaces and clear difference between core and outer-shell. As the PLGA molecular weight increased, the release rate of doxorubicin-loaded, double-layered microspheres decreased. These results showed that the release behaviors can be controlled by the variation of molecular weight of PLGA.