• 제목/요약/키워드: cell permeability

검색결과 604건 처리시간 0.025초

Development of Transdermal Delivery Systems Containing Clenbuterol (클렌부테롤 경피흡수제제의 개발)

  • Choi, Han-Gon;Quan, Qi-Zhe;Jung, Si-Young;Rhee, Jong-Dal;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • 제30권4호
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    • pp.247-252
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    • 2000
  • The advantages of transdermal administration are avoiding hepatic first pass effect, minimizing inter- and intra-patient variation, maintaining steady-state plasma level to provide long-term therapy from a single dose, and allowing a rapid termination of drug input. Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease. For the development of transdermal systems containing clenbuterol, two limiting factors - long lag time and low flux - must be overcome. In this study, we attempted to select optimal formulation for preparation of clenbuterol patch using hairless mouse skin and flow-through diffusion cell. The flux of clenbuterol increased as the percent of clenbuterol dose dependently in the concentration range of 5-15%. Based on this result, we fixed the concentration of clenbuterol as 15%. The effect of various penetration enhancers on percutaneous absorption of clenbuterol through hairless mouse skin was investigated. Labrafil was the most effective enhancer, which increased the permeability of clenbuterol approximately 4-fold compared with the control without penetration enhancer. Optimal enhancer concentration was 3%. The effect of various adhesives on penetration of clenbuterol was also investigated. Among the adhesives studied, MA-31 was the most effective adhesive. Furthermore, the clenbuterol patch composed of 15% clenbuterol, 3% Labrafil and 82% MA-31, which gave most excellent penetration of drug in in vitro penetration study, maintained therapeutic plasma levels in in vivo study using S.D. rats. These studies demonstrated a good feasibility of clenbuterol administration through the intact skin using a transdermal patch, and show a possibility of the development of clenbuterol patches.

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Skin Permeation and Anti-inflammatory Effects of Hydrolyzed Products of Gardeniae Fructus Extracts (치자 엑스의 가수분해에 의한 피부투과 및 항염효과)

  • Yang, Jae-Heon;Lee, Nam-Hee
    • Journal of Pharmaceutical Investigation
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    • 제34권2호
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    • pp.115-123
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    • 2004
  • Geniposide and its related iridoid compounds have been used in traditional herbal medicine for thε treatment of Jaundice hepatic diseases and various inflammatorys. For the purpose to increase trandsdermal absorption, the hydrolyzed products of Gardeniae Furctus were identified and assayed of active ingredients and investigated trandsdermal absorption and anti-inflammatory effects. Geniposide was hydrolyzed to genipin by ${\beta}-glucosidase$ and it was suggested that genipin was more suitable form than geniposide for transdermal absorption by its lipophilic property. Using Franz type diffusion cell and the skin of hairless mouse, the permeation rate of hydrolyzed products and their emulsion preparation were determined. Genipin have more increased absorption ratio through the skin of hairless mouse than geniposide. Also, the emulsion of hydrolyzed products of extracts showed higher permeability than that of nonhydrolyzed preparations. After 9 hours $280.85\;{\mu}g/cm^2$ of genipin was absorbed and $193.52\;{\mu}g/cm^2$ in case of geniposide. The Js of geniposide and genipin were $26.27{\pm}4.11\;{\mu}g/cm^2/hr$ and $40.35{\pm}5.04\;{\mu}g/cm^2/hr$ respectively. After carrageenan injection, the swelling was increased repidly to 24 hr and maintained as plateau. but emulsion group weer reached about 2.5 mL and the swelling decreased successively form 24 hr to 72 hr. The anti-inflammation effects of extracts and hydrolyzed products emulsion were increased with significant difference with control group after 24 hr, 48 hr and 72 hr. In carrageenan induced edema, inhibition of swelling was increased in case of hydrolyzed product emulsion compare with nonhydrolyzed group at 24 hr, 48 hr and 72 hr after swelling. In histological study, the anti-inflammatory effects of hydrolyzed products were remarkable at 48 hr and 72 hr compare with nonhydrolyzed. Hydrolyzed products of Gardeniae Fructus extracts containing genipin would be a suitable preparation to increase the transdermal absorption and anti-inflammatory effects.

Danchunhwan Protects the Cytotoxicity of Beta-amyloid in SH-SY5Y Neuroblastoma Cells (베타아밀로이드 유도성 SH-SY5Y 세포독성에서 단천환(丹川丸)의 보호효과)

  • Yu, Bong-Sun;Kim, Jin-Kyung;;Park, Chan-Ny;So, Hong-Seob
    • Journal of Physiology & Pathology in Korean Medicine
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    • 제20권6호
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    • pp.1516-1523
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    • 2006
  • The water extract of Danchunhwan(DCH) has been traditionally used for treatment of dementia damage in oriental medicine. However, little is known about the mechanism by which the water extract of DCH rescues cells from neurodegenerative disease such as Alzheimer's disease. This study was designed to investigate the protective mechanisms of DCH on ${\beta}$-amyloid or $H_2O_2$-induced cytotoxicity in SH-SY5Y neuronblastoma cells. ${\beta}$-amyloid and $H_2O_2$ markedly decreased the viability of SH-SY5Y cells, which was characterized with apparent apoptotic features such as membrane blebbing as well as fragmentation of genomic DNA and nuclei. However, the water extract of DCH significantly reduced both ${\beta}$-amyloid or $H_2O_2$-induced cell death and apoptotic characteristics through reduction of intracellular peroxide generation. Also, the water extract of DCH prevented prevented the mitochondrial dysfunction including the disruption of mitochondria membrane permeability transition (MPT) and the perturbation in Bcl-2 family protein expressions in $H_2O_2$-treated SH-SY5Y cells.

Study on Anti-allergic Effects of Electroacupuncture in Allergic Mouse Model

  • Yoon Ji-Won;Jeong Kyoung-Ah;Cho Zang-Hee;Sung Kang-Keyng
    • Journal of Physiology & Pathology in Korean Medicine
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    • 제20권1호
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    • pp.196-201
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    • 2006
  • Electroacupuncture(EA) is commonly used in various diseases. In the present study, the effect of EA in the allergic mouse model was examined. Allergy is generated via immunological mechanism and non-immunological mechanism. Mast cells activated dy those mechanisms get to release various substances such as histamine, leukotrienes, prostaglandin, TNF-$\alpha$, IL-4, IL-6, etc. which induce allergic reactions and the following inflammatory responses. To evaluate the anti-allergic effects of EA, mortality, ear swelling response, vascular permeability and cytokine secretion were investigated in EA group and non-EA group of which mice were compound 48/80-induced allergy model or PCA model. Compound 48/80 induces allergic reaction via non-immunological mechanism and PCA model is generated through the same mechanism with immediate-type(Type1) allergic reaction, one of immunological allergic reactions. EA inhibited compound 48/80-induced ear swelling response but did not inhibit the systemic anaphylaxis. EA also inhibited passive cutaneous anaphylaxis(PCA) activated dy anti-dinitrophenol IgE. In addition, EA inhibited IL-6 and TNF-$\alpha$ secretion from 48 h PCA in mice. These results indicate that EA may be used for the treatment of mast cell-mediated allergic diseases, especially immediate-type(Type 1) allergy and non-immunologically mediated allergy.

Effect of Diet and Water Intake on Aquaporin 2 Function

  • Kim, Jun-Mo;Kim, Tae-Hee;Wang, Tong
    • Childhood Kidney Diseases
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    • 제20권1호
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    • pp.11-17
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    • 2016
  • Appropriate control of diet and water intake is important for maintaining normal blood pressure, fluid and electrolyte homeostasis in the body. It is relatively understood that the amount of sodium and potassium intake directly affects blood pressure and regulates ion transporters; Na and K channel functions in the kidney. However, little is known about whether diet and water intake regulates Aquaporin (AQP) function. AQPs, a family of aquaporin proteins with different types being expressed in different tissues, are important for water absorption by the cell. Water reabsorption is a passive process driven by osmotic gradient and water permeability is critical for this process. In most of the nephron, however, water reabsorption is unregulated and coupled to solute reabsorption, such as AQP1 mediated water absorption in the proximal tubule. AQP2 is the only water channel founded so far that can be regulated by hormones in the kidney. AQP2 expressed in the apical membrane of the principal cells in the collecting tubule can be regulated by vasopressin (antidiuretic hormone) controlling the final volume of urine excretion. When vasopressin binds to its receptor on the collecting duct cells, it stimulates the translocation of AQP2 to the membrane, leading to increased water absorption via this AQP2 water channel. However, some studies also indicated that the AQP2 is also been regulated by vasopressin independent mechanism. This review is focused on the regulation of AQP2 by diet and the amount of water intake on salt and water homeostasis.

Development of Triaxial Cells Operable with In Situ X-ray CT for Hydro-Mechanical Laboratory Testing of Rocks (원위치 X-ray CT 촬영이 가능한 암석의 수리-역학 실험용 삼축셀 개발)

  • Zhuang, Li;Yeom, Sun;Shin, Hyu-Soung
    • Journal of the Korean Geotechnical Society
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    • 제36권9호
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    • pp.45-55
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    • 2020
  • X-ray computed tomography (CT) is very useful for the quantitative evaluation of internal structures, particularly defects in rock samples, such as pores and fractures. In situ CT allows 3D imaging of a sample subjected to various external treatments such as loading and therefore enables observation of changes that occur during the loading process. We reviewed state-of-the-art of in situ CT applications for geomaterials. Two triaxial cells made using relatively low density but high strength materials were developed aimed at in situ CT scanning during hydro-mechanical laboratory testing of rocks. Preliminary results for in situ CT imaging of granite and sandstone samples with diameters ranging from 25 mm to 50 mm show a resolution range of 34~105 ㎛ per pixel pitch, indicating the feasibility of in situ CT observations for internal structural changes in rocks at the micrometer scale. Potassium iodide solution was found to improve the image contrast, and can be used as an injection fluid for hydro-mechanical testing combined with in situ CT scanning.

Influence of column yielding on degree of consolidation of soft foundations improved by deep mixed columns

  • Jiang, Yan;Han, Jie;Zheng, Gang
    • Geomechanics and Engineering
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    • 제6권2호
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    • pp.173-194
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    • 2014
  • Laboratory and field data showed that deep mixed (DM) columns accelerated the rate of consolidation of the soft foundations. Most analyses of consolidation of DM column-improved foundations so far have been based on the elastic theory. In reality, the DM columns may yield due to the stress concentration from the soft soil and its limited strength. The influence of column yielding on the degree of consolidation of the soft foundation improved by DM columns has not been well investigated. A three-dimensional mechanically and hydraulically-coupled numerical method was adopted in this study to investigate the degree of consolidation of the DM column foundation considering column yielding. A unit cell model was used, in which the soil was modeled as a linearly elastic material. For a comparison purpose, the DM column was modeled as an elastic or elastic-plastic material. This study examined the aspects of stress transfer, settlement, and degree of consolidation of the foundations without or with the consideration of the yielding of the DM column. A parametric study was conducted to investigate the influence of the column yielding on the stress concentration ratio, settlement, and average degree of consolidation of the DM column foundation. The stress concentration ratio increased and then decreased to reach a constant value with the increase of the column modulus and time. A simplified method was proposed to calculate the maximum stress concentration ratios under undrained and drained conditions considering the column yielding. The simplified method based on a composite foundation concept could conservatively estimate the consolidation settlement. An increase of the column modulus, area replacement ratio, and/or column permeability increased the rate of consolidation.

Bacterial Exopolysaccharides: Insight into Their Role in Plant Abiotic Stress Tolerance

  • Bhagat, Neeta;Raghav, Meenu;Dubey, Sonali;Bedi, Namita
    • Journal of Microbiology and Biotechnology
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    • 제31권8호
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    • pp.1045-1059
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    • 2021
  • Various abiotic stressors like drought, salinity, temperature, and heavy metals are major environmental stresses that affect agricultural productivity and crop yields all over the world. Continuous changes in climatic conditions put selective pressure on the microbial ecosystem to produce exopolysaccharides. Apart from soil aggregation, exopolysaccharide (EPS) production also helps in increasing water permeability, nutrient uptake by roots, soil stability, soil fertility, plant biomass, chlorophyll content, root and shoot length, and surface area of leaves while also helping maintain metabolic and physiological activities during drought stress. EPS-producing microbes can impart salt tolerance to plants by binding to sodium ions in the soil and preventing these ions from reaching the stem, thereby decreasing sodium absorption from the soil and increasing nutrient uptake by the roots. Biofilm formation in high-salinity soils increases cell viability, enhances soil fertility, and promotes plant growth and development. The third environmental stressor is presence of heavy metals in the soil due to improper industrial waste disposal practices that are toxic for plants. EPS production by soil bacteria can result in the biomineralization of metal ions, thereby imparting metal stress tolerance to plants. Finally, high temperatures can also affect agricultural productivity by decreasing plant metabolism, seedling growth, and seed germination. The present review discusses the role of exopolysaccharide-producing plant growth-promoting bacteria in modulating plant growth and development in plants and alleviating extreme abiotic stress condition. The review suggests exploring the potential of EPS-producing bacteria for multiple abiotic stress management strategies.

Development of Improving Water Quality in Eutrophic Lake Using Microalgal Cultivation (미세조류 배양을 이용한 부영양호 내 수질 개선 기술 개발)

  • Kim, Ki-Hyun;Kang, Sung-Mo;Cho, Yonghee;Jeon, Sanghyun;Kim, Jun-Ho;Park, Hanwool;Lee, Yunwoo;Jeong, Jeongho;Lim, Sang-Min;Lee, Choul-Gyun
    • Journal of Marine Bioscience and Biotechnology
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    • 제10권2호
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    • pp.91-96
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    • 2018
  • There are many eutrophic lakes by point and non-point pollution sources such as in dustrial waste water, domestic raw sewage, and mucks. The eutrophic lakes not only cause algal blooms but also destroy the ecosystem in the lakes due to high nutrient concentrations. The purpose of this study was to improve water quality in eutrophic lakes by cultivating microalgae using photobioreactors (PBRs) with selectively permeable mesh (SPM), supplying nutrients in the lake and inhibiting cell leakage by diffusion and water permeability. Chlorella vulgaris, was cultivated using PBRs with SPM installed in Inkyung Lake located in Inha university, Incheon, Korea. When cultivating C. vulgaris, $8.3g/m^2/day$ of average biomass productivity was obtained at 3 days. Furthermore, concentrations of total nitrogen and phosphorus were reduced by 35.7% and 84.2%, respectively, compared to initial condition and water quality in eutrophic lake was improved to oligotrophic environment. These results suggest that microalgal cultivation using PBRs with SPM in the lake could produce microalgal biomass as well as improve water quality by decreasing nutrient concentrations.

Inactivation of Mycobacteria by Radicals from Non-Thermal Plasma Jet

  • Lee, Chaebok;Subhadra, Bindu;Choi, Hei-Gwon;Suh, Hyun-Woo;Uhm, Han. S;Kim, Hwa-Jung
    • Journal of Microbiology and Biotechnology
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    • 제29권9호
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    • pp.1401-1411
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    • 2019
  • Mycobacterial cell walls comprise thick and diverse lipids and glycolipids that act as a permeability barrier to antibiotics or other chemical agents. The use of OH radicals from a non-thermal plasma jet (NTPJ) for the inactivation of mycobacteria in aqueous solution was adopted as a novel approach. Addition of water vapor in a nitrogen plasma jet generated OH radicals, which converted to hydrogen peroxide ($H_2O_2$) that inactivated non-pathogenic Mycobacterium smegmatis and pathogenic Mycobacterium tuberculosis H37Rv. A stable plasma plume was obtained from a nitrogen plasma jet with 1.91 W of power, killing Escherichia coli and mycobacteria effectively, whereas addition of catalase decreased the effects of the former. Mycobacteria were more resistant than E. coli to NTPJ treatment. Plasma treatment enhanced intracellular ROS production and upregulation of genes related to ROS stress responses (thiolrelated oxidoreductases, such as SseA and DoxX, and ferric uptake regulator furA). Morphological changes of M. smegmatis and M. tuberculosis H37Rv were observed after 5 min treatment with $N_2+H_2O$ plasma, but not of pre-incubated sample with catalase. This finding indicates that the bactericidal efficacy of NTPJ is related to the toxicity of OH and $H_2O_2$ radicals in cells. Therefore, our study suggests that NTPJ treatment may effectively control pulmonary infections caused by M. tuberculosis and nontuberculous mycobacteria (NTM) such as M. avium or M. abscessus in water.