• Title/Summary/Keyword: Skin concentration

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Iontophoretic Transport of Donepezil Hydrochloride through Skin: Flux Enhancement by Chemical Enhancer and Iontophoresis

  • Oh, Seaung-Youl
    • Journal of Pharmaceutical Investigation
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    • 제41권6호
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    • pp.337-345
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    • 2011
  • The objective of this work is to investigate the effect of chemical enhancer and current on the flux of donepezil hydrochloride (DH) through skin. Ethanol and N-methyl pyrrolidone (NMP) were used as chemical enhancers in combination with iontophoresis. We also have studied the effect of pH on flux and evaluated the role of electroosmosis. In vitro flux study was performed at $33^{\circ}C$, using side-by-side diffusion cell and full thickness hairless mouse skin. Passive flux of DH without enhancer was very small. As the concentration of enhancer increased, passive flux increased. After current application, flux increased markedly and the time to reach maximum decreased. Without enhancer, maximum flux was about 50 fold larger than that obtained without current. These results indicate that electromigration is playing a major role for the transport. As the enhancer concentration increased, flux also increased. NMP and ethanol increased not only the passive delivery, but also the iontophoretic delivery. Flux results indicate that ethanol has better ability than NMP in enhancing the transport of DH. The magnitudes of increase in flux by these enhancers indicate that there is a large synergistic effect in flux enhancement. Flux results from pH study showed that electroosmotic flow is reversed at low pH and the flux is hindered. These results provided some information on the flux enhancing ability of ethanol and NMP in combination with iontophoresis. The data also provided some mechanistic insights into the role of electromigration and electroosmosis on flux through skin.

Formulating for efficacy

  • Johann W. Wiechers;Caroline L. Kelly;Trevor G. Blease;Chris Dederen
    • 대한화장품학회:학술대회논문집
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    • 대한화장품학회 2003년도 IFSCC Conference Proceeding Book I
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    • pp.457-468
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    • 2003
  • Active ingredients have been around in cosmetics for a long time but have they really resulted in active cosmetic products\ulcorner In order to achieve this, the right active needs to be delivered to the right location at the right concentration for the correct period of time. And the extent (and therefore the concentration) of this delivery depends on the formulation. From a rather theoretical approach based on the polarity of the active ingredient, the stratum corneum and the oil phase, the Relative Polarity Index was established that enables the selection of a suitable emollient for ensuring skin penetration of the active ingredient. Practical examples subsequently show the validity of this approach that demonstrates that one can regulate the delivery of an active molecule (and therefore the efficacy of a cosmetic formulation) by selection and control of the emollient system. Cosmetic formulations are generally quite complex mixtures and subsequent experiments using different emulsifier systems indicated that this component of a cosmetic formulation could also have an impact on steering the active ingredient to the right layer of the skin, although it is too early to be able to derive general rules from this.

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The Safety Evaluation of a Potent Angiogenic Activator, Synthetic Peptide (SFKLRY-NH2) for the Skin Application

  • Kim, Dong-Ha;Lim, Yun-Young;Kim, Hyeong-Mi;Kim, So-Young;Kim, Beom-Joon;Park, Sung-Gil;Lee, Tae-Hoon;Cho, Soo-Muk
    • Toxicological Research
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    • 제28권1호
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    • pp.51-56
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    • 2012
  • A novel synthetic hexapeptide (SFKLRY-$NH_2$) that displays angiogenic activity has been identified by positional scanning of a synthetic peptide combinatorial library (PS-SPCL). This study was carried out to investigate the irritation of the SFKLRY-$NH_2$ on the skin. The tests were performed on the basis of Korea Food and Drug Administration (KFDA) guidelines. In results, cell toxicity is not appeared for SFKLRY-$NH_2$ in HaCaT cells and B16F10 cells. SFKLRY-$NH_2$ induced no skin irritation at low concentration ($10{\mu}m$), mild irritation at high concentration (10mM). We consider that this result is helpful for saying about the safety of SFKLRY-$NH_2$ in clinical use.

Non-polar Solvents (Toluene and Styrene) Enhance Methanol Skin Absorption

  • Lim, Cheol-Hong;Yu, Il-Je
    • Toxicological Research
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    • 제17권1호
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    • pp.7-9
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    • 2001
  • The quantitative assessment of the penetration of organic solvents through skin is necessary for the evaluation of health hazards in occupational environments. We investigated the rate of dermal penetration when mixed or single forms of organic solvents were placed into a diffusion cell in vitro or into an experimental animal in vivo. The diffusion rates of methanol. toluene, and styrene were 6.07, 0.129, and 0.046 mg/$cm^2$/h, respectively. When skin was exposed to the mixed solvent of methanol and toluene, the penetration rate of toluene did not change significantly (0.110 mg/$cm^2$/h). However, the rate of methanol penetration increased to 43.90 mg/$\textrm{cm}^2$/h. The penetration rate of methanol also increased significantly to 54.69 mg/$cm^2$/h by mixing it with styrene. The concentration of methanol in the blood was monitored during the epicutaneous exposure in rats. The blood concentration of methanol was increased by mixing methanol with toluene as seen in the in vitro experiments. These results showed that the penetration rate of organic solvents would be enhanced by mixing them with other solvents.

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마우스에서 황금 유래 Wogonin의 Th1과 Th2 사이토가인 조절 효과 (Immunosuppressive Activity of Wogonin from Scutellaria Radix on DNFB-induced Delayed Type Hypersensitivity in Mice)

  • 김용준;이정치;김홍용;설광화;윤용갑;장선일
    • 동의생리병리학회지
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    • 제19권4호
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    • pp.1027-1031
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    • 2005
  • In the present study, wogonin, a major flavone isolated from Scutellaria Radix were examined for its imunosuppressive activity on the 2,4-dinitro-fluorobenzene (DNFB)-induced delayed type hypersensitivity (DTH) in C3H/HeN mice. This compound inhibited selectively $TNF-\alpha$ and IL-4, but not IL-6, IL-10 and $IFN-\gamma$ on DNFB-induced Th1 and Th2 cytokines in a concentration-dependent manner. Interestingly, this compound increased the expression of heme oxygenase-1 (HO-1) in a concentration-dependent manner The above results reveal that wogonin possesses anti-inflammatory, humoral and cellular immunomodulatory, and stress reducing activities on the DNFB-induced DTH in mice and these properties may contribute to the anti-atopic dermatitis activity of Scutellaria Radix.

케토프로펜 패취제의 제제설계 및 피부 투과 특성 (Formulation and Skin Permeation Characteristics of Ketoprofen Patches)

  • 오흥설;이용석;김하영;이광표
    • 약학회지
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    • 제45권5호
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    • pp.506-512
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    • 2001
  • Ketoprofen (KP) was formulated as a transdermal patch using the percutaneous penetration enhancers sorbitan monmmleate(SMO), polyvinylpyrrolidone(PVP). The control patch without penetration enhancers showed a KP flux of 8.9$\pm$0.75$\mu\textrm{g}$/$\textrm{cm}^2$/h The flux was increased in proportion to the concentration of SMO added. Furthermore, lag times were decreased upon addition of SMO. Conversely; the skin flux of KP was decreased in proportion to the concentration of PVP added. Pharmacokinetic parameters including $C_{max}$, $T_{max}$, and AUC were increased when SMO was added. However, $C_{mas}$ significantly decreased by the addition of PVP. $T_{max}$ was not significantly different in 2%, 4%, and 8% PVP patches. Patches containing 4% PVP showed the highest AUC value (19.158$\mu\textrm{g}$.h/ml). We found that the effectiveness of the two percutaneous penetration enhancers for topical KP patches was similar, with the addition of appropriate amounts of HPC modifying both skin flux and lag time of KP in the patches. In conclusion, it is possible to manufacture KP patches exhibiting high AUC, high skin flux, and short lag time using percutaneous penetration enhancers of SMO and PVP.

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Antibacterial Activity of Panduratin A and Isopanduratin A Isolated from Kaempferia pandurata Roxb. against Acne-causing Microorganisms

  • Song, Min-Soo;Shim, Jae-Seok;Gwon, Song-Hui;Lee, Chan-Woo;Kim, Han-Sung;Hwang, Jae-Kwan
    • Food Science and Biotechnology
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    • 제17권6호
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    • pp.1357-1360
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    • 2008
  • Propionibacterium acnes is the predominant organism in sebaceous regions of the skin and is thought to play an important role in the pathogenesis of inflamed lesions. Antibacterial compounds against P. acnes were isolated from the ethanol extract of Kaempferia pandurata Roxb. and identified as panduratin A and isopanduratin A. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of panduratin A for P. acnes were 2 and $4{\mu}g/mL$, respectively, while those of isopanduratin A were 4 and $8{\mu}g/mL$, respectively. The time-dependent killing effect showed that panduratin A and isopanduratin A completely inhibited the growth of P. acnes at 4 and $8{\mu}g/mL$ in 48 hr, respectively. Panduratin A and isopanduratin A demonstrated high antibacterial activities not only against P. acnes but also other skin microorganisms. The results suggest that panduratin A and isopanduratin A could be employed as natural antibacterial agents to inhibit the growth of acne and skin disease causing microorganisms.

오배자의 항 주름 효과 및 미백 효과에 미치는 실험적 연구 (The Anti-wrinkle Effects and Whitening Effects of Galla Rhois)

  • 박진미;김경준
    • 한방안이비인후피부과학회지
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    • 제23권1호
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    • pp.135-148
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    • 2010
  • Recently, the demands for the effective and safe depigmentating and anti-aging agents of the skin have increased due to the medical, pharmaceutical and cosmetic reasons. The aim of this study is to search Galla Rhois (GR) inhibitory activity against aging process of skin in vitro. GR was screened for their inhibitory activity against elastase. GR (final concentration 1 mg/ml) appeared over 40% of inhibition of elastase activity. So we investigated anti wrinkle effects of GR look through MMP-1 inhibition activity. Also Extracts of GR showed higher anti-tyrosinase activity than arbutin (final concentration 1 mg/ml). These results suggest that GR could be potential sources of anti-aging and whitening effects for the skin. Objective : Galla Rhois extracts, Elastase (pancreatic from porcine pancreas), N-Succinyl-(Ala)3-p-nitroanilide, Ursolic acid, mushroom tyrosinase, L-tyrosine, arbutin, Amicon Ultra, Hand Hold UV lamp, MMP-1 primary antibody, MMP-1 secondary antibody Result : 1. GR appeared over 40% of elastase inhibitory activity. 2. GR had MMP-1 inhibition activity. 3. GR showed higher anti-tyrosinase activity than arbutin. Conclusion : According to above results, it is supposed that Galla Rhois could be strong potential sources of anti-aging and whitening effects for the skin.

Evaluation of Pork Myofibrillar Protein Gel with Pork Skin Gelatin on Rheological Properties at Different Salt Concentrations

  • Lee, Chang Hoon;Chin, Koo Bok
    • 한국축산식품학회지
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    • 제39권4호
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    • pp.576-584
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    • 2019
  • This study was performed to evaluate the physicochemical properties of myofibrillar protein (MP) gels containing pork skin gelatin at different salt concentrations. MP gels were prepared to the different salt levels (0.15, 0.30, and 0.45 M) with or without 1.0% of pork skin gelatin. Cooking yield (CY), gel strength, shear stress were measured to determine the physical properties, and SDS-polyacrylamide gel electrophoresis, scanning electron microscopy, fourier transform infrared spectroscopy, sulfhydryl group and protein surface hydrophobicity was performed to figure out the structural changes among the proteins. The addition of gelatin into MP increased CYs and shear stress. MP at 0.45 M salt level had the highest CY and shear stress, as compared to MPs at lower salt concentrations. As the salt concentration of MP gels increased, the microstructure became the compact and wet structures, and decreased the amount of ${\alpha}-helix$/unordered structures and ${\beta}-sheet$. MP with gelatin showed a decreased amount of ${\alpha}-helix$/unordered structures and ${\beta}-sheet$ compared to MP without gelatin. The addition of gelatin to MP did not affect the sulfhydryl group, but the sulfhydryl group decreased as increased salt levels. MP mixtures containing gelatin showed a higher hydrophobicity value than those without gelatin, regardless of salt concentration. Based on these results, the addition of gelatin increased viscosity of raw meat batter and CY of MP gels for the application to low salt meat products.

만성 피부 질환으로 발생하는 스트레스 개선을 위한 호박, 작약, 타트체리 복합물의 효능 연구 (Study on the Efficacy of Paeonia Japonica, Cucurbita Moschata and Prunus Cerasus Complex Extract for Alleviating Stress Associated with Chronic Skin Conditions)

  • 박수진;김동희;곽기성;김현정
    • 한국응용과학기술학회지
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    • 제41권2호
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    • pp.459-471
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    • 2024
  • 현대사회에서 스트레스와 긴장감은 피할 수 없는 요인이다. 다양한 피부질환은 스트레스를 일으키는 중요한 요인으로 언급되고 있다. 피부질환을 가진 환자들은 수면상태가 원활하지 않아 전반적으로 수면 효율이 낮다. 또한 피부질환으로 인해 심리적 스트레스 수치가 높아지고, 이와 같은 과정은 반복적으로 발생하고 있다. 피부질환과 스트레스는 상호적으로 연관되어 있으며, psychodematology에 대한 연구가 증가하고 있다. 이에 본 연구에서는 피부질환을 저하 시킬 수 있는 호박, 작약, 타트체리 복합물을 활용하여 피부 각질 형성 세포에서 스트레스로 인한 만성 피부질환을 개선할 수 있는 소재를 개발하고 효능을 입증하고자 하였다. HaCaT 각질형성세포에 복합 추출물은 12.5, 25, 50, 100 ㎍/mL 농도 의존적으로 TNF-α, IL-1β, IL-6, MDC, TARC 발현량이 저해되었으며 특히 IL-1β의 경우, 100 ㎍/mL의 농도에서 40% 이상 저해하는 우수한 효능을 확인하였다. 또한 AQP-3, HA, filaggrin의 생성량 농도 의존적으로 유의미한 증가를 보이며 TNF-α/IFN-γ로 증가된 p-ERK, p-JNK, p-p38의 단백질 발현은 복합 추출물의 처리로 유의하게 감소시 키는 것으로 나타났다. 이를 통하여 해당 복합 추출물은 피부질환을 치료 및 예방할 수 있는 소재로서 활용가치가 있는 것으로 판단되며, 이는 피부질환과 스트레스 간의 상호 관계의 악영향을 낮춰 줄 것으로 판단된다.