• Title/Summary/Keyword: skin permeability

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External Lyogel Formulation of Prostaglandin E1 Ethyl Ester (프로스타글란딘 E1 에칠에스테르의 외용 리오겔 제제 설계)

  • Yang, Sung-Woon;Lee, Jin-Kyo;Lee, Ji-Eun;Kim, Hee-Kyu;Park, Hye-Sook;Kim, Jong-Seok;Choi, Han-Gon;Yong, Chul-Soon;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.34 no.2
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    • pp.107-114
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    • 2004
  • External lyogels containing prostaglandin $E_1$ ethyl ester $(PGE_1-EE)$, a prodrug of prostaglandin $E_1\;(PGE_1)$ as a therapeutic agent for erectile dysfunction, were formulated to overcome the aqueous instability and enhance the percutaneous absorption. Lyogels of $PGE_1-EE$ were prepared with ethanol (EtOH)/proplyene glycol (PG) cosolvent system as a vehicle, cineol as an enhancer, and hydroxypropylcellusose as a gelling agent. In vitro percutaneous absorption studies were performed to determine the rate of $PGE_1$ absorption through rat or hairless mouse skin. The permeability of $PGE_1-EE$ lyogel with enhancer was 16-fold greater than that of lyogel without enhancer. Cosolvent produced 9-fold increase in percutaneous absorption. Pharmacodynamic effects of lyogels were evaluated in mature male cats in terms of intracavernosal pressure (ICP). Lyogels containing 0.1 % of $PGE_1-EE$ showed higher ICP compared to intraurethral preparation of $PGE_1$ (1 %) and enhancer-free control lyogel. The shelf-life $(t_{10%})$ of lyogel at refrigerated condition $(4^{\circ}C)$ was calculated as 928 days, which is 4.2 times longer than that of control hydrogel. As a result, $PGE_1-EE$ was formulated successfully to a lyogel system with a selective enhancer and cosolvent system for the topical delivery of $PGE_1$.

Study of Superparamagnetic Microneedles containing Iron Oxide Nanoparticles (산화철 나노입자를 함유한 초상자성 마이크로니들에 관한 연구)

  • Lee, Seung-Jun
    • Applied Chemistry for Engineering
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    • v.32 no.5
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    • pp.556-561
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    • 2021
  • Recently, iron oxide nanoparticles have been used as the subject of many studies on drug delivery system (DDS) due to their excellent magnetic properties and biocompatibility in response to external magnetic fields. In this study, hyaluronic acid-superparamagnetic microneedles (HA-SMNs) and carboxy methyl cellulose-superparamagnetic microneedles (CMC-SMNs) containing superparamagnetic iron oxide nanoparticles (SIONs) were prepared with HA and CMC as a matrix materials of MNs (microneedles). Various properties of SMNs were then investigated with scanning electron microscopy (SEM), superconducting quantum interference device-vibrating sample magnetometer (SQUD-VSM), frequency mixing magnetic detection (FMMD), and polymer/bio membrane. The SQUID-VSM measurements showed superparamagnetism of HA-SMNs and CMC-SMNs containing SIONs. The FMMD results demonstrated that the signal intensity changed significantly as the concentration of SIONs increased. In addition, SMNs exhibited the average skin permeability intensities on the bio membrane for HA-SMNs and CMC-SMNs were 92.5 and 98.5%, respectively. These results suggested that SMNs could be utilized as deliver materials for a TDDS and MR molecular imaging.

A Study on the Application of Medical Compression Arm Sleeves Using a MRT(Moisture Responded Transformable) Fibers (MRT(Moisture Responded Transformable)섬유의 의료용 압박소매 적용에 관한 연구)

  • Cho, Daehyun;Jung, Taedu;Park, Eunhee;Park, Youngmi
    • Textile Coloration and Finishing
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    • v.33 no.2
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    • pp.87-95
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    • 2021
  • In this study, the application of a medical compression sleeve of Moisture Responded Transformable(MRT) fibers to the treatment of lymphedema after surgery in breast cancer patients was investigated. MRT fibers were manufactured with PET and Nylon6 bi-component cross-section yarns, and compression sleeves of sleeves 1, 2, 3, and 4 were knitted in order of size, and then the physical properties and clinical tests were evaluated. As a result, the pressure of compression sleeve in wrinkle was the lowest in sleeve 1 with 3.81 kPa, and the highest in sleeve 4 with 5.22 kPa. Elastic recovery rate is that all parts except the top of the sleeve 1 exhibited 100%. The air permeability was good at 12.1 ~ 16.1 cm3/cm2/sec, and peeling was also comparatively excellent as grade 3. In addition, the weight of the compression sleeves 1, 2, and 3 decreased as 18.3 ~ 23.0 g/m2 depend on size, while the compared sample was heavier with 17.39 ~ 32.61 g/m2. In lymphoscintigraphy test, it was confirmed that the function of remaining lymph node was good in all patients. Although there were no differences between samples in skin irritation and tightness in wearing comfort, the manufactured sleeves showed better fit, lightness, fashion and breathability than the comparable sleeves.

Inhibitory Effect of Steviol and Its Derivatives on Cell Migration via Regulation of Tight Junction-related Protein Claudin 8 (스테비올 및 그 유도체의 세포연접 관련 클라우딘 8 발현 조절을 통한 세포이동 저해효과)

  • Choi, Sun Kyung;Cho, Nam Joon;Cho, Uk Min;Shim, Joong Hyun;Kim, Kee K.;Hwang, Hyung Seo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.42 no.4
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    • pp.403-412
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    • 2016
  • The tight junction, one of Intercellular junctions, performs a variety of biological functions by bonding adjacent cells, including the barrier function to control the movement of the electrolyte and water. Recent studies have revealed that unusual expression of tight junction-related genes have been shown to be related in cancer development and progression. Recently, there are many reports that control of tight junction proteins expression is closely related to the skin moisture. In this study, we are focusing on the regulating mechanism of tight junction-associated genes by the steviol and its derivatives. Steviol, used as a sweetner, is known to chemical compound isolated from stevia plant. The MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt) assay was carried out in HaCaT cells (human keratinocyte cell line) in order to determine the cytotoxicity. As a result, while steviol showing cytotoxicity from $250{\mu}M$, steviol derivatives are not cytotoxic more than $250{\mu}M$ concentration. We have observed a change in the tight junction protein via quantitative real-time PCR. Claudin 8 among tight junction proteins is only significantly reduced up to 30% in the presence of steviol. In addition, cell migration was inhibited by steviol, not by stevioside and rebaudioside. Finally, we could observe that steviol, not stevioside and rebaudioside, is able to increase the skin barrier permeability through the transepithelial electric resistance (TEER) measurements. These results suggest that the steviol and its derivatives are specifically acts on the tight junction related gene expression, but steviol derivatives are more suitable as a cosmetic material.

The Anti-bacterial Effects and Epidermal Permeability Barrier Function of Red Onion Juice Produced in Jeon-Nam province in Korea (전남 함평산 자색양파 추출물의 항균효과와 피부장벽 보호효과)

  • Youn, Dae-Hwan;Shin, Heon-Tae
    • Journal of Society of Preventive Korean Medicine
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    • v.16 no.1
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    • pp.43-56
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    • 2012
  • Objective : In this study, we assessed the anti-bacterial effects and epidermal permeability barrier function of red onion juice comparing to yellow onion juice and $Houttuynia$ $cordata$ extract $in$ $vitro$. Methods : 3types of red and yellow onion juice were prepared as antibacterial agent candidates with Houttuynia cordata hot water extract using 4 different bacterial strains ($Escherichia$ $coil$, $Salmonella$ $enterica$ $subsp.$ $enterica$, $Staphylococcus$ $epidermidis$, $Staphylococcus$ $aureus$ $subsp$) by colony counting method. The expression of filaggrin, a marker of keratinocyte differentiation, and serine palmitoyl transferase (SPT), a marker of the formation of the stratum corneum lipid barrier, in human HaCat keratinocytes were analyzed using HaCaT cell line. The expression of COX-2 and AP-1 which is a factor of COX-2 transcription were also analyzed by western blotting method. Results : There was detectable anti-bacterial effects on $Staphylococcus$ $epidermidis$, $Staphylococcus$ $aureus$ $subsp$ among 1%, 5%, 10% extracts of yellow and red onion.(81%-100%) The bacteriocidal effects were not shown on $Escherichia$ $coil$, $Salmonella$ $enterica$ $subsp.$ $enterica$ among $Houttuynia$ $cordata$, yellow onion and red onion extracts. The in vitro results showed the concentration-dependent effects on the expression of both filaggrin and SPT in HaCat cells among 0.01%, 0.05%, 0.1%, 0.5% extracts in Houttuynia cordata and red onion, reflecting the notion that $Houttuynia$ $cordata$ and red onion can induce epidermal keratinocyte differentiation and improve the recovery of skin barrier functions. The concentration-dependent effects also have been shown on the expression of both COX-2 and AP-1 among 0.01%, 0.05%, 0.1%, 0.5% extracts in $Houttuynia$ $cordata$ and red onion, while slight effect in yellow onion. Conclusion : Red onion juice could be a potential candidate enhanser for the skin care and cosmetology.

Cellular Protective Effect and Liposome Formulation for Enhanced Transdermal Delivery of Persicaria hydropiper L. Extract (여뀌 추출물의 세포 보호 작용과 피부 흡수 증진을 위한 리포좀 제형 연구)

  • Kim, Jung-Eun;Lee, Hye-Jin;Lim, Myoung-Sun;Park, Min-A;Park, Soo-Nam
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.38 no.1
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    • pp.15-31
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    • 2012
  • In our previous studies, the antioxidant, anti-aging, and antibacterial activities of Persicaria hydropipier L. extract, and the moisturizing effect of cream containing P. hydropipier extract were investigated. In this study, the cellular protective effects of P. hydropipier extract and isoquercitrin, main component from P. hydropipier in $^1O_2$-induced photohemolysis of human erythrocytes and ultraviolet B (UVB)-exposed HaCaT cells were investigated. Liposomes such as ethosome and elastic liposome for enhanced transdermal delivery were prepared. Size, loading efficiency, stability, and cumulative permeated amounts of ethosomes and elastic liposomes were evaluated. P. hydropipier extract and isoquercitrin showed more prominent cellular protective effect than (+)-${\alpha}$-tocopherol, known as lipid antioxidant at $5{\mu}g/mL$. P. hydropipier extract didn't show any characteristics of cytotoxicity at $50{\mu}g/mL$. When HaCaT cells were exposed to a single large dose ($400mJ/cm^2$) of UVB, the extract protected the cells against UVB radiation in a concentration dependent manner ($12.5{\sim}50{\mu}g/mL$). Cell viability of HaCaT cells exposed to UVB $400mJ/cm^2$ was increased by treatment with P. hydropipier extract or isoquercitrin from 36 % (cell viability of positve control groups) to 90 % (cell viability of P. hydropipier extract or isoquercitrin- treated groups). The size of 0.04 % P. hydropiper extract loaded ethosomes was 173.0 nm and the loading efficiency was 55.58 %. 0.04 % P. hydropiper extract loaded ethosomes were stable with as monodisperse particles for 1 week. The ethosome exhibited more skin permeability than general liposome and ethanol solution. The optimal ratio of lipid to surfactant ($Tego^{(R)}$ care 450) of 0.1 % P. hydropiper extract loaded elastic liposomes was observed to be 95 : 5. Vesicle size of 0.1 % P. hydropiper extract loaded elastic liposome was 176.5 nm. The deformability index of the elastic liposome was 16.4. The loading efficiency was 68.8 %. The elastic liposome containing P. hydropiper extract showed more skin permeability than liposome without surfactant ($Tego^{(R)}$ care 450).

Activation of transient receptor potential vanilloid 3 by the methanolic extract of Schisandra chinensis fruit and its chemical constituent γ-schisandrin

  • Nam, Yuran;Kim, Hyun Jong;Kim, Young-Mi;Chin, Young-Won;Kim, Yung Kyu;Bae, Hyo Sang;Nam, Joo Hyun;Kim, Woo Kyung
    • The Korean Journal of Physiology and Pharmacology
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    • v.21 no.3
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    • pp.309-316
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    • 2017
  • Transient receptor potential vanilloid 3 (TRPV3) is a non-selective cation channel with modest permeability to calcium ions. It is involved in intracellular calcium signaling and is therefore important in processes such as thermal sensation, skin barrier formation, and wound healing. TRPV3 was initially proposed as a warm temperature sensor. It is activated by synthetic small-molecule chemicals and plant-derived natural compounds such as camphor and eugenol. Schisandra chinensis (Turcz.) Baill (SC) has diverse pharmacological properties including antiallergic, anti-inflammatory, and wound healing activities. It is extensively used as an oriental herbal medicine for the treatment of various diseases. In this study, we investigated whether SC fruit extracts and seed oil, as well as four compounds isolated from the fruit can activate the TRPV3 channel. By performing whole-cell patch clamp recording in HEK293T cells overexpressing TRPV3, we found that the methanolic extract of SC fruit has an agonistic effect on the TRPV3 channel. Furthermore, electrophysiological analysis revealed that ${\gamma}$-schisandrin, one of the isolated compounds, activated TRPV3 at a concentration of $30{\mu}M$. In addition, ${\gamma}$-schisandrin (${\sim}100{\mu}M$) increased cytoplasmic $Ca^{2+}$ concentrations by approximately 20% in response to TRPV3 activation. This is the first report to indicate that SC extract and ${\gamma}$-schisandrin can modulate the TRPV3 channel. This report also suggests a mechanism by which ${\gamma}$-schisandrin acts as a therapeutic agent against TRPV3-related diseases.

The antimicrobial activity of Hwangheuk-san and synergy effect with oxacillin against methicillin-resistant Staphylococcus aureus (황흑산(黃黑散)의 메티실린 내성 황색포도상구균에 대한 항균 활성과 옥사실린과의 시너지 효과)

  • Choi, Sung-Hoon;Kang, Ok-Hua;Zhou, Tian;Kong, Ryong;Lee, Seung-Jin;Kang, Dam-Hee;Jung, Hye-In;Lee, Young-Seob;Kwon, Dong-Yeul
    • The Korea Journal of Herbology
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    • v.31 no.5
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    • pp.93-98
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    • 2016
  • Objectives : Hwangheuk-san is a complex prescription composed of oriental traditional medicine and has been reported for antioxidant, antimicrobial and anticancer effects in the recent study. Methicillin-resistant Staphylococcus aureus (MRSA) is one of important causes of fatal infectious diseases such as septicemia, endocarditis, toxic shock syndrome, pneumonia, skin and soft tissue infections (SSTIs). S. aureus is reported as being for a variety of human diseases and its epidemiological relevance is mainly due to their ability of becoming highly resistant to common antimicrobials such as tetracycline, penicillin, cphalosporin and aminoglycoside. The objective of this study is to determine the antimicrobial effect of Hwangheuk-san ethanol extracts (HHS) and synergistic effects with antibiotics oxacillin against MRSA.Methods : The antimicrobial activity of HHS was measured by the disc diffusion method, broth microdilution method and the checkerboard dilution test, time-kill curve assay was performed to investigate synergistic effects with antibiotics oxacillin against MRSA.Results : HHS showed antimicrobial activity against MRSA with a MIC value of 125 ㎍/㎖. In the checkerboard test, the interaction of HHS with antibiotics oxacillin produced almost synergy or partial synergy against MRSA. This study showed that HHS reduced the MICs of oxacillin tested, and a remarkable antibacterial effect of HHS, with membrane permeability enhancers.Conclusions : These results suggest that HHS has the antimicrobial effect and synergistic effects with antibiotics oxacillin against MRSA. This study thus can be a valuable source for the development of a new drug with low MRSA resistance.

Fabrication of edible gelatin-based films by heat pressing (열 압착을 이용한 가식성 젤라틴 필름 제조)

  • Kim, Eui Hyun;Song, Ah Young;Min, Sea Cheol
    • Korean Journal of Food Science and Technology
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    • v.54 no.2
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    • pp.179-184
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    • 2022
  • In this study, edible films made of fish and mammalian gelatins were produced using heat pressing, and their physical properties were investigated. Transparent and smooth films were formed continuously and uniformly using a mixture of fish skin gelatin (FG) or mammalian gelatin (MG), glycerol, and water under the process of heat pressing at 90℃ and 20 MPa for 5 min. Heat-pressed FG films possessed lower light transmittance and tensile strength than heat-pressed MG films; however, their appearance, surface morphology, water vapor permeability, lightness, and redness were not different from those of heat-pressed MG films. Although heat-pressed FG films had lower tensile strength, they had a flatter and more uniform surfaces and demonstrated higher transparency and moisture barrier properties compared to the casted FG films. These results demonstrate the potential utility of heat pressing for the large-scale production of edible films using both FG and MG.

Type of Oil and Effect of Required HLB on Nanoemulsion Formation (오일의 종류 및 required HLB가 나노에멀젼 형성에 미치는 영향)

  • Da-yeon Lee;Hye-yun Hwang;Su-min Lim;Hy-ein Jang
    • Journal of the Korean Applied Science and Technology
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    • v.40 no.6
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    • pp.1533-1546
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    • 2023
  • Nanoemulsion is an emulsion with a particle size of about 20 ~ 200 nm and has the advantage of having a transparent or translucent appearance and improving the skin permeability of an effective material with a small particle size, so it is applied in various fields. In this study, eight oils with different types of HLB and 16 oils with different types of required HLB were selected to investigate the effect of the required HLB and the type on the formation of nanoemulsion. The surfactants used at this time were Polysorbate 60 (HLB 14.9), Sorbitan state (HLB 4.7), PEG-60 hydrogenated castor oil (HLB 14.0), which were mixed with Polysorbate 60 and Sorbitan state, fixed with HLB 14.0, and Polysorbate 60 and PEG-60 hydrogenated castor oil, respectively. The formation of nanoemulsion was different depending on the type of oil, and oil with an ester structure showed a relatively excellent nanoemulsion formation ability. In particular, it was confirmed that a stable nanoemulsion was formed without a significant change after Cetyl ethylhexanoin was produced in a small size of 40 nm or less on average. In addition, it was found that using a mixture of Polysorbate 60 and Sorbitan stearate has a superior nanoemulsion formation ability than using PEG-60 hydrogenated castor oil or Polysorbate 60 alone.