• Title/Summary/Keyword: permeation effect

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Effects of Glycerin and PEG 400 in Donor and Receptor Solutions upon Skin Permeation of Drug (In vitro 경피흡수 실험시 Donor와 Receptor용액중의 글리세린과 PEG 400이 약물의 경피투과도에 미치는 영향)

  • Cho, Ae-Ri
    • Journal of Pharmaceutical Investigation
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    • v.26 no.2
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    • pp.99-103
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    • 1996
  • Effects of glycerin and PEG 400 in donor and receptor solutions upon skin permeation of drug were investigated. Deoxycortisone was used as a model compound. In vitro skin permeation study with freshly excised hairless mouse skin was performed and the steady-state skin permeation rates of the drug were determined in different fractions of glycerin or PEG 400 in donor and receptor solutions. Glycerin in donor solution didn't show any effect on the skin permeation rate of deoxycortisone. However glycerin in receptor solution showed significant effect on the skin permeation rate of the drug. In glycerin, there's a critical concentration for balancing hydration and dehydration of skin. At low concentration, less than 20 %, glycerin showed the enhancement of the flux due to the hydration effect of skin. At high concentration, more than 30 %, glycerin retard the permeation rate which might be due to the dehydration effect on the dermis layer. Since dermis has more water content than the stratum corneum, the steady state skin permeation rates were more influenced when glycerin was in receptor solution than that of in donor solution. PEG 400 aqueous solutions doesn't affect the steady state permeation rate of deoxycortisone significantly.

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Transdermal permeation and Anti-inflammatory Effects of Piroxicam Gel by Phonophoresis (음프록시캄 겔을 이용한 음파영동이 경피투과와 염증에 미치는 효과)

  • Choi, Sug-Ju;Kim, Tae-Youl;Yoon, Se-Won
    • Journal of Korean Physical Therapy Science
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    • v.10 no.1
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    • pp.170-179
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    • 2003
  • This study was performed that how phonophoresis using ultrasound for piroxicam affects transdermal permeation and anti-inflammative effects. Transdermal permeation study conducted by using hairless mouse had two categories: control group and ultrasound group. Transdermal permeation was observed according to duty cycle and intensity. Anti-inflammatory effects were determined using in Sprague-Dawley rat. The subjects were divided into three groups of six SD rat each 24 hour, 48 hour, 72 hour. The results of this study were as follows: 1. Transdermal permeation of piroxicam was measured according to ultrasound duty cycle. This research demonstrates that ultrasound group retains more transdermal permeation than control group, and that pulsed ultrasound group holds a little more transdermal permeation than continuous ultrasound group. 2. The transdermal permeation of piroxicam is closely related with ultrasound intensity. Effect of each group of transdermal permeation was significant rises in proportion to ultrasound intensity. 3. By observing inflammation of the tissue caused by trauma, phonophoresis group showed more significant of anti-inflammatory effect. The conclusion of phonophoresis was found to improve significantly the transdermal permeation and the anti-inflammatory effect.

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Effect of Polyoxyethylene Alkyl Esters on Permeation Enhancement and Impedance of Skin

  • Kim, Hee-Sun;Oh, Seaung-Youl
    • Biomolecules & Therapeutics
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    • v.19 no.1
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    • pp.109-117
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    • 2011
  • In this work, we have investigated the effect of polyoxyethylene alkyl ester nonionic surfactants on percutaneous permeation enhancement of a model drug, ketoprofen. We also investigated the mechanism involved in the enhancement using impedance and solubility measurement. Three groups of nonionic surfactants with different ethylene oxide content were studied. The permeation results showed that all surfactants enhanced the percutaneous absorption, irrespective of the molecular weight. The permeation results from PEG-45 monostearate (PEGMS45) were rather unexpected. Impedance and solubility results indicate that the mechanism involved in the enhancement of permeation by PEG-10 monooleate (PEGMO10) and PEGMS45 is rather different. The results from PEGMS45 suggest that it could be a potential candidate as a skin penetration enhancer with high molecular weight, which may poses less skin irritation and systemic side effect than the smaller surfactant molecules. Overall, this work provided some useful information on percutaneous transport enhancement and the mechanistic insights involved in skin permeation for these nonionic surfactants.

The Effect of Synthetic Polymer Membranes on the Skin Permeation of Anti-AIDS Drugs (항에이즈 약물의 경피흡수에 미치는 합성고분자 멤브레인의 영향)

  • Lee, Kyung-Jin;Kim, Dae-Duk;Chien, Yie W.
    • Journal of Pharmaceutical Investigation
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    • v.28 no.1
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    • pp.1-5
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    • 1998
  • The effect of synthetic polymer membranes on the permeation rate of dideoxynucleoside-type anti-HIV drugs through hairless rat skin was studied using ethylene/vinyl acetate copolymer (EVA) and ethylene/methyl acrylate copolymer (EMA) membranes fabricated by solvent casting method. In vitro skin permeation kinetics study of DDC (2',3'-dideoxythymidine), DDI (2',3'-dideoxyinosine) and AZT (3'-azido-3'-deoxythymidine) across the (membrane/skin) composite was conducted for 24 hours at $37^{\circ}C$ using the Valia-Chien skin permeation system. The results showed that skin permeation rate of each drug across the (skin/membrane) composite was mainly dependent on the property of the membrane. Proper selection of the polymeric membrane which resembles hydrophilicity/lipophilicity of the delivering drug was important in controlling the skin permeation rate.

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Skin Permeability of piroxicam Gel by Phonophoretic Transdermal Drug Delivery (음파영동 경피약물수송에 의한 Piroxicam Gel의 경피투과)

  • Choi Suk-Joo;Oh Myung-Hwa;Kim Tae-Youl
    • The Journal of Korean Physical Therapy
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    • v.14 no.4
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    • pp.147-162
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    • 2002
  • Transdermal permeation enhancer has been used to increased skin absorption. External control of drug release and skin absorption can also be achieved by iontophoresis or phonophoresis. However, because several problems with iontophoresis are that it has a risk to skin damage because of the change of pH and the increase of current density in applying it and that it can be applied only in the form of water solution, This study is to enhance drug permeation via skin following application of ultrasound. For this goal, in gel containing piroxicam, the degree of skin permeation in vitro and anti-inflammatory effect in in vivo were investigated. Permeation study using hairless mouse skin was performed at 37 $^{\circ}C$ using buffer saline as the receptor solution. The amount of piroxicam were quantified using a HPLC system consisting of solvent delivery system. Following adoption of ultrasound 1 MHZ, it showed relatively high permeation rate where it was compared with non treated by ultrasound. The influence of duty cycle having an effect on skin permeation rate was slight higher in the case of using pulsed mode. Skin permeation increase attended by intensity of ultrasound, the permeation of trice was accelerated at 2.0 W/$cm^{2}$ than 1.0 W/$cm^{2}$. The skin permeation of piroxicam was substantially influenced by ultrasound. Anti-inflammatory effects were determined using carrageenan-induced paw swelling method in SD rat. Paw swelling tests showed that pulsed phonophoresis group was more effective than control group and only gel application group. The conclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory effect in vivo.

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Skin Permeation of Flurbiprofen through Excised Rat Skin from Poloxamer 407 Gel

  • Gil, Hyung-Jun;Lee, Woo-Young;Chi, Sang-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.24 no.3
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    • pp.27-32
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    • 1994
  • In order to reduce systemic side effects following oral administration, flurbiprofen was formulated as transdermal gels consisting of the drug, poloxamer 407 and ethanol in buffer solutions. The effect of formulation variables in the preparation of flurbiprofen gels on skin permeation of the drug was evaluated using Keshary-Chien diffusion cells fitted with excised rat skins. The permeation rate of flurbiprofen through rat skin was directly proportional to initial drug concentration (between 0.1% and 1.0%) in the gel while it was inversely proportional to poloxamer 407 concentration (between 17.5% and 25%). The skin permeation of flurbiprofen was substantially influenced by the gel pH between 3 and 7, exhibiting a maximum at pH 4. The concentration effect of ethanol on the permeation of the drug was negligible in the concentration range of $10{\sim}20%$.

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Analytical solutions for sandwich plates considering permeation effect by 3-D elasticity theory

  • Huo, Ruili;Liu, Weiqing;Wu, Peng;Zhou, Ding
    • Steel and Composite Structures
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    • v.25 no.2
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    • pp.127-139
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    • 2017
  • In this paper, an exact analytical solution for simply supported sandwich plate which considers the permeation effect of adhesives is presented. The permeation layer is described as functionally graded material (FGM), the elastic modulus of which is assumed to be graded along the thickness following the exponential law. Based on the exact three-dimensional (3-D) elasticity theory, the solution of stresses and displacements for each layer is derived. By means of the recursive matrix method, the solution can be efficiently obtained for plates with many layers. The present solution obtained can be used as a benchmark to access other simplified solutions. The comparison study indicates that the finite element (FE) solution is close to the present one when the FGM layer in the FE model is divided into a series of homogeneous layers. However, the present method is more efficient than the FE method, with which the mesh division and computation are time-consuming. Moreover, the solution based on Kirchhoff-Love plate theory is greatly different from the present solution for thick plates. The influence of the thickness of the permeation layer on the stress and displacement fields of the sandwich plate is discussed in detail. It is indicated that the permeation layer can effectively relieve the discontinuity stress at the interface.

Effect of Various Enhancers on Permeation of Scopolamine through Excised Rat Skin (스코폴라민의 흰쥐 피부투과에 대한 투과촉진제들의 영향)

  • Jung, Jae-Young;Kam, Sung-Hoon;Kim, Keon-Nam;Chi, Sang-Cheol;Park, Eun-Seok
    • Journal of Pharmaceutical Investigation
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    • v.33 no.2
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    • pp.141-144
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    • 2003
  • The transdermal therapeutic system (TTS) of scopolamine has various advantages over its oral dosage forms. The ideal scopolamine TTS requires high skin permeation rate in short time after it is applied on the skin. In order to increase the initial skin permeation rate of scopolamine from TTS, various permeation enhancers were employed. Enhancers employed were fatty acids (oleic and linolenic acids), cyclic monoterpenes (menthol, camphor, cineole and limonene) and others (isopropyl myristate, sodium lauryl sulfate and glyceryl monostearate). The concentration of enhancers in the base were fixed to 5% (w/w). While fatty acids had little enhancing effect on the skin permeation of scopolamine, cyclic monoterpenes, isopropyl myristate and sodium lauryl sulfate resulted in $1.5{\sim}2.6-fold$ higher skin permeation rate of the drug compared to the control. However, lag time was not affected by enhancers studied.

The Effect of Limonene on Skin Permeation and Localization of Ascorbic Acid

  • Lee, Sang-Kil;Woo, Rye-Seung;Choi, Sung-Up;Lee, Jae-Hwi;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.36 no.5
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    • pp.305-308
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    • 2006
  • Poloxamer-based hydrogel formulation for the topical delivery of ascorbic acid(AsA) was prepared and the effect of limonene on AsA skin permeation and localization was evaluated. In vitro rat skin permeation study, the AsA skin permeation of limonene-containing hydrogel was about 3 to 5 fold higher than control hydrogel. However the amount of permeated AsA was independent to the concentration of limonene. On the other hand the localized amount of AsA after 2 h increased proportion to the content of limonene. The increase in the ratio of localized AsA($Q_L$) to permeated AsA($Q_P$) was attributed to the limonene's ability of making polar pathway within stratum corneum by interacting on lipid domain of the skin and the AsA's hydration effect on the stratum corneum and effect on the protein domain of the skin.

Transdermal Delivery and Analgesic Effects of Lidocaine Hydrogel by Phonophoresis (초음파를 이용한 리도카인 수용성겔의 경피흡수 및 진통효과)

  • Yang, Jae-Heon;Kim, Dae-Keun;Song, Kyung-Suk;Yun, Mi-Young;Ahn, Hyo-Cho;Kim, Young-Il;Kim, Tae-Youl
    • Journal of Pharmaceutical Investigation
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    • v.37 no.3
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    • pp.149-158
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    • 2007
  • To investigate the permeability of lidocaine, percutaneous absorption studies were performed using excised hairless mouse skin and the penetration of lidocaine via the skin was determined. To increase the skin permeation of lidocine, the effects of $Labrasol^{(R)}$, $Labrafil^{(R)}$, $Labrafac^{(R)}$ and $Transcutol^{(R)}$ were investigated. The skin permeation of lidocaine was increased when $Labrasol^{(R)}$ and $Transcutol^{(R)}$ were used as permeation enhancer. To evaluate the influence of ultrasound, various factors such as application modes (continuous mode and pulsed mode), frequency (1.0 and 3.0 MHz) and intensity (1.0, 1.5 and 2.0 w/$cm^2$) were investigated with lidocaine hydrogel. The pronounced effect of ultrasound on the skin permeation of lidocaine was observed at all ultrasound energy levels. The influence of frequency having an effect on skin permeation rate was higher in the case of using 1 MHz, 2.0 w/$cm^2$ and continuous treatment. As the intensity of ultrasound increased, the permeation of lidocaine was accelerated. The in vivo anesthetic effects were evaluated by two aspects as mechanical threshold and electrical threshold. Six healthy volunteers consented to the randomized, double-blind, and cross-over designed study in each group. In each subject, 3 groups were adapted such as K group (ultrasound with gel base only), L group (lidocaine gel) and B group (ultrasound with lidocaine gel). In conclusion, lidocaine was potent anesthetic which could be block pain threshold effectively. And ultrasound could accelerate the skin penetration of lidocaine. The phonophoretic delivery system could be a good candidate for lidocaine as a local anaesthetic to improve the skin permeation and in vivo anaesthetic effect.