• Title/Summary/Keyword: enhancer

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Transport Characteristics and Screening of Penetration Enhancer through Buccal Mucosa of Butorphanol Tartrate from [P(AA-co-PEGMM)] Copolymer Films ([P(AA-co-PEGMM)] 공중합체 필름으로부터 Butorphanol Tartrate의 구강점막 투과 특성 및 투과촉진제의 검색)

  • Kim, Joun-Sik;Park, Jeong-Sook;Jeong, Yeon-Bok;Han, Kun
    • Journal of Pharmaceutical Investigation
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    • v.33 no.3
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    • pp.157-162
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    • 2003
  • The feasibility of [P(AA-co-PEGMM)] film as a buccal mucoadhesive patch was previously reported by estimating mucoadhesiveness and release characteristics. To find a rational penetration enhancer of [P(AA-co-PEGMM)] film containing butorphanol tartrate (Bt), penetration of Bt from [P(AA-co-PEGMM)] film which contained various additives was estimated by measuring its flux, Papp and lag tme in in vitro buccal membrane of porcine. EDTA showed almost no increase of Bt permeability, wherease SGC, STDHF and SLS increased the permeability of Bt with the order of SGC > STDHF > SLS. The rational additive concentration of SGC was 4% and its Papp and lag time were $1.93{\times}10^{-4}{\pm}4.21{\times}10^{-6},\;126.60{\pm}21.88min\;(control\;:\;Papp\;0.45{\times}10^{-4};\;lag\;time\;211.01{\pm}16.77\;min)$, respectively.

Increase of Permanent Wave Efficacy and Decrease of Hair Damage by using Enhancer of Permanent Wave Lotion (흡수촉진제를 이용한 펌제의 웨이브 효율 증가 및 모발손상 억제)

  • Song Hee-Ra;Park Myung-Hee
    • Journal of the Korean Society of Costume
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    • v.56 no.4 s.103
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    • pp.124-133
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    • 2006
  • Human hair could be damaged by various physicochemical conditions and treatment. Permanent and decoloring treatment were the most serious factor on hair damage. The new permanent wave lotion containing Permeation enhancers such as Cremophor EL, Transcutol and propylene glycol based on cysteine permanent wave lotion were prepared. Efficiency of permanent wave and hair damage following pH of permanent wave lotion and addition of permeation enhancer were investigated. PH of solution, wave efficiency, loss of protein from hair, morphology of hair by SEM and solubility of alkaline solution were evaluated. The addition of Cremophor EL and Transcutol with ethanol increased permanent wave efficacy and decreased hair damage effectively. They diminished permanent wave lotion's pH and augmented permanent wave lotion's penetration compare to cysteine permanent wave lotion. new permanent wave lotion containing permeation enhancers such as Cremophor EL could be a good candidate for a new permanent wave lotion.

Development of Clotrimazole Gels for Enhanced Transdermal Delivery

  • Cho, Hwa-Young;Kim, Dal-Keun;Park, ung-Chan;Kang, Chung;Oh, In-Joon;Kim, Seong-Jin;Shin, Sang-Chu
    • Journal of Pharmaceutical Investigation
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    • v.39 no.6
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    • pp.437-443
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    • 2009
  • To develop a topical bioadhesive formulation of clotrimazole for enhanced transdermal delivery, hydroxypropyl methylcellulose gel containing permeation enhancer was formulated and permeation studies were carried out. The release characteristics of the drug from the gel formulation were examined according to the receptor medium, drug concentration, and temperature. The rate of drug release from the gel increased with increasing drug concentration and temperature. The activation energy (Ea) of drug permeation, which was calculated from the slope of log P versus 1/T plots, was 14.41kcal/mol for a 1%(w/w) loading dose. The enhancer, such as saturated, unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants, were incorporated onto the gels to increase the amount of drug permeation into the skin. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest level of enhancement. These results show that clotrimazole gels containing polyoxyethylene 2-oleyl ether could be used for the enhanced transdermal delivery of clotrimazole.

Effect of L-Menthol on the Percutaneous Absorption of Ketorolac Tromethamine Across Human Cadaver Skin (사람 카다베르 피부를 통한 케토롤락 트로메타민의 경피 흡수에 L-menthol이 미치는 영향)

  • Lee, Yong-Seok;Oh, Heung-Seol;Kim, Ha-Hyung;Lee, Kwang-Pyo
    • YAKHAK HOEJI
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    • v.44 no.6
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    • pp.595-600
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    • 2000
  • Transdermal delivery of ketorolac tromethamine, a potent non-narcotic analgesic, through human cadaver skin was investigated in vitro. A mixture of ethanol/water (40/60) containing 0, 1, 3, 5, and 8 (w/v)% L-menthol were used as a vehicle and penetration enhancer respectively. The permeation of ketorolac through human cadaver skin from saturated drug solution was evaluated at $37^{\circ}C$ with modified Franz diffusion cell. The in vitro skin flux and lag time were $1.23\;{\pm}\;0.11\;{\mu}g/cm^2{\cdot}hr$ and $5.56\;{\pm}\;0.34\;hr$, respectively. The cumulative amount of penetrated ketorolac containing L-menthol in ethanol/water (40/60) binary system was increased by the following order; 3%, 5%, 8%, 1%, 0%, and the lag time was decresed by the following order; 3%, 5%, 8%, 0%, 1%. The results suggested that a potential use of 3% L-methol is an effective penetration enhancer of ketorolac tromethamine through the human cadaver skin.

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A Korean case of neurofibromatosis type 1 with an exonic splicing enhancer site mutation

  • Park, Sangwook;Sohn, Young Bae;Chung, In-Soon;Hong, Ji-Hee;Jung, Eun-Jung;Jeong, Seon-Yong;Jin, Hyun-Seok
    • Journal of Genetic Medicine
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    • v.11 no.1
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    • pp.40-42
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    • 2014
  • Neurofibromatosis type 1 (NF1) is an autosomal dominant disease characterized by neurological, cutaneous, and ophthalmological manifestations. A 33-year-old woman with typical symptoms of NF1 visited Ajou University Hospital. Screening of the whole-messenger RNA region of NF1 at the complementary DNA level by polymerase chain reaction-direct sequencing confirmed the presence of an NF1 mutation at the genomic level. The mutation analysis revealed an in-frame skipping of exon 46 (c.6757_6858del) caused by a point mutation (c. 6792C>A) in exon 46. In this report, we have described the first Korean case of a proband with NF1 that carries an allele with an exon 46 deletion caused by an exonic splicing enhancer site mutation, leading to the skipping of the whole of exon 46 (c.6757_6858del).

Iontophoretic Transport of GHRP-6 (성장호르몬방출펩타이드-6 (GHRP-6)의 경피투과)

  • Choi, Bo-Kyung;Oh, Seaung-Youl
    • Journal of Pharmaceutical Investigation
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    • v.31 no.4
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    • pp.273-279
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    • 2001
  • The purpose of this study is to characterize the iontophoretic transport of growth hormone releasing peptides (GHRP-6) through hairless mouse skin from aqueous solution. The effect of various factors, such as pH, poloarity, current profile, current density, current duration, ionic strength, drug concentration, and enhancer application was studied to obtain basic knowledge on the transport. We have also studied the stability of GHRP-6 in solution with/without current. The donor chamber was filled with phosphate buffer solution containing GHRP-6 and the receptor chamber was filled with phosphate buffer solution (pH 7.4). Ag/AgCl electrode was used for their stability and reversibility. At a predetermined time interval, sampling was made and the concentration of drug was analysed using HPLC system. The results showed that, compared to passive flux, the total amount of drug transported increased markedly by the application of anodal current. Cathodal flux was similar to passive flux. Flux increased with the current density, the duration of current application and drug concentration. The effect of enhancers on the flux was studied using hydrophilic (5% N-methyl pyrrolidone) and hydrophobic (5% propylene glycol monolaurate, 5% oleic acid) enhancers. Application of enhancer also increased the flux.

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Properties of BE0623 to serve as a growth factor of Bifidobacterium

  • Cho, Young Hoon;Sim, Jae Young;Nam, Myoung Soo
    • Korean Journal of Agricultural Science
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    • v.47 no.3
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    • pp.445-457
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    • 2020
  • Prebiotics are defined as "Nondigestible food ingredients that beneficially affect the host by selectively stimulating the growth and activity of bacteria in the intestine" and as defined improve host health. This study was carried out to investigate the effects of bifidobacteria (Bifidobacterium lactis BB12 and Bifidobacterium longum BB536) growth enhancer (BE0623) supplement as a prebiotic. The addition of BE0623, a growth promoting material for bifidobacteria, significantly increased bifidobacteria viable cells counts in fermented milk by about 45 to 75 times compared to the non-added control group. In addition, microscopic observation showed a significant effect on proliferation of bifidobacteria in fermented milk with added BE0623. The viable cell counts in bifidobacteria also increased roughly 102-fold compared to the control group (non-added BE0623) and was higher than that of commercial growth promoters. Each fraction obtained though the purification of BE0623 influenced the increase of bifidobacteria growth. Culturing bifidobacteria with a combination of fractions of BE0623 had a synergistic effect compared to culturing bifidobacteria with each fraction individually. When any of the fractions were not added, the effect of the growth enhancer on bifidobacteria was reduced. These results indicate that all fractions contain substances that promote the growth of bifidobacteria. Therefore, BE0623 is considered to be available as a growth promoting material for bifidobacterium.

Enhanced Transmucosal Permeation of Thyrotropin-releasing Hormone (치로트로핀 유리 호르몬의 점막 투과 증진)

  • 전인구;신동원
    • Biomolecules & Therapeutics
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    • v.7 no.3
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    • pp.263-270
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    • 1999
  • The in vitro permeation of thyrotropin-releasing hormone (TRH) through rabbit nasal, rectal and duodenal mucosae was studied in the absence and presence of an enzyme inhibitor and permeation enhancer. TRH in the donor and receptor solutions was assayed by HPLC. When thimerosal (TM, 0.5 mM) was added to the donor cell as an inhibitor, the permeation rate of TRH (200 $\mu\textrm{g}$/ml) increased linearly as a function of time. Fluxes of TRH through the nasal, rectal and duodenal mucosae were found to be 33.3$\pm$5.9, 11.8$\pm$1.9 and 9.6$\pm$0.7 $\mu\textrm{g}$/$\textrm{Cm}^2$/hr, respectively. The addition of sodium glycocholate, glycyrrhizic acid ammonium salt, sodium taurodihydrofusidate or L-$\alpha$-lysophosphatidylcholine to the donor solution containing TM did not result in the significant increase of permeation flux except for the duodenal mucosa, comparing with that in the presence of TM alone. Consequently, it was suggested that the nasal route was advantageous for systemic delivery of TRH, and the addition of TM and/or an enhancer was necessary to maximize the transmucosal permeation of TRH.

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The RUNX1 Enhancer Element eR1: A Versatile Marker for Adult Stem Cells

  • Chuang, Linda Shyue Huey;Osato, Motomi;Ito, Yoshiaki
    • Molecules and Cells
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    • v.43 no.2
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    • pp.121-125
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    • 2020
  • The identification of adult stem cells is challenging because of the heterogeneity and plasticity of stem cells in different organs. Within the same tissue, stem cells may be highly proliferative, or maintained in a quiescent state and only to be activated after tissue damage. Although various stem cell markers have been successfully identified, there is no universal stem cell marker, which is exclusively expressed in all stem cells. Here, we discuss the roles of master developmental regulator RUNX1 in stem cells and the development of a 270 base pair fragment of the Runx1 enhancer (eR1) for use as stem cell marker. Using eR1 to identify stem cells offers a distinct advantage over gene promoters, which might not be expressed exclusively in stem cells. Moreover, RUNX1 has been strongly implicated in various cancer types, such as leukemia, breast, esophageal, prostate, oral, skin, and ovarian cancers-it has been suggested that RUNX1 dysfunction promotes stem cell dysfunction and proliferation. As tissue stem cells are potential candidates for cancer cells-of-origin and cancer stem cells, we will also discuss the use of eR1 to target oncogenic gene manipulations in stem cells and to track subsequent neoplastic changes.

Histone H3 Lysine Methylation in Adipogenesis (Adipogenesis에서 히스톤 H3 lysine methylation)

  • Jang, Younghoon
    • Journal of Life Science
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    • v.30 no.8
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    • pp.713-721
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    • 2020
  • Adipogenesis as a model system is needed to understand the molecular mechanisms of human adipocyte biology and the pathogenesis of obesity, diabetes, and other metabolic syndromes. Many relevant studies have been conducted with a focus on gene expression regulation and intracellular signaling relating to Peroxisome proliferator-activated receptor gamma (PPARγ) and CCAAT/enhancer-binding protein alpha (C/EBPα), which are master adipogenic transcription factors. However, epigenome regulation of adipogenesis by epigenomic modifiers or histone mutations is not fully understood. Histone methylation is one of the major epigenetic modifications on gene expression in mammals, and histone H3 lysine methylation (H3Kme) in particular implicates cell differentiation during various tissue and organ development. During adipogenesis, cell type-specific enhancers are marked by histone H3K4me1 with the active enhancer mark H3K27ac. Mixed-lineage leukemia 4 (MLL4) is a major H3K4 mono-methyltransferase on the adipogenic enhancers of PPARγ and C/EBPα loci. Thus, MLL4 is an important epigenomic modifier for adipogenesis. The repressive mark H3K27me3 is mediated by the enzymatic subunit Enhancer zeste homolog 2 (EZH2) of the polycomb repressive complex 2. EZH2-mediated H3K27 tri-methylation on the Wnt gene increases adipogenesis because WNT signaling is a negative regulator of adipogenesis. This review summarizes current knowledge about the epigenomic regulation of adipogenesis by histone H3 lysine methylation which fundamentally regulates gene expression.