• Title/Summary/Keyword: transdermal

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Transdermal Delivery of Ceramide Using Sodium Deoxycholate-based Deformable Liposomes

  • Kim, Dong-Chan;Noh, Sang-Myoung;Kim, Young-Bong;Baek, Kwang-Hyun;Oh, Yu-Kyoung
    • Journal of Pharmaceutical Investigation
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    • v.38 no.5
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    • pp.319-323
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    • 2008
  • For transdermal delivery of ceramides, various liposomes formulations were studied and evaluated. Sodium deoxycholate (SDC), Tween 20 and Span 85 were used as edge activators. The skin permeation of ceramides was performed using a Franz cell apparatus with hairless mouse skin. Among edge activators, SDC showed the higher values of deformability index and skin permeation than did others. For optimization of formulations, we varied the ratios of lipids to edge activators and the compositions between phosphatidylcholine (PC) and ceramides. The optimal ratio of lipid to SDC was observed to be 6:1 (w:w) and that of PC and ceramide was 1:1. Our results suggest that the skin permeation of ceramides could be enhanced by optimized deformable formulations of liposomes containing SDC as a major edge activator.

Transdermal Delivery of Diclofenac Using Microemulsions

  • Kweon, Jang-Hoon;Chi, Sang-Cheol;Park, Eun-Seok
    • Archives of Pharmacal Research
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    • v.27 no.3
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    • pp.351-356
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    • 2004
  • A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol: ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.

Evaluation of Ulcerogenic Activity of Ketoprofen Gel (케토프로펜 겔의 궤양형성작용 평가)

  • Tan, Hyun-Kwang;Chi, Sang-Cheol;Jun, H.-Won
    • Journal of Pharmaceutical Investigation
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    • v.24 no.2
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    • pp.105-108
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    • 1994
  • The ulcerogenic activity of a 3% ketoprofen gel (ID-GEL) after its transdermal application in rats was determined with the Litchfield and Wilcoxon method in reference to the oral administration of ketoprofen in a suspension. The $UD_{50}$ (dose producing ulcers in 50%, of the rats tested) of ID-GEL after its transdermal application was approximately 4 times greater than that after the oral administration of the drug, indicating that the ulcerogenic activity of ketoprofen was much lowered with its transdermal application.

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Effects of Oil type on the Stability of Oil-in-Water Lipid Nanoemulsion

  • Lee, Seung-Jun;Han, Sa Ra;Jeong, Jae Hyun;Kim, Jong-Duk
    • Journal of the Korean Applied Science and Technology
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    • v.33 no.4
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    • pp.667-675
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    • 2016
  • Nanoemulsions are actively used in several applications for pharmaceutical, cosmetic and chemical industries. In this study, we propose the use of microfluidizer known as high pressure homogenizer to prepare lipid nanoemulsion as a potent cosmetic delivery carrier. The lipid nanoemulsions were prepared by O/W emulsion with hydrogenated lecithin and different type of oils. Effects of oil type on the stability of the lipid nanoemulsion were investigated with Dynamic Light Scattering (DLS) and Zeta-potential. Arbutin was used as model drug for transdermal administration through hairless mouse skin. Transdermal arbutin delivery using the lipid nanoemulsions was studied with HPLC method.

Low-frequency Ultrasound Enhanced Transdermal Drug Delivery Across Rat Skin

  • Lee, Hwa-Jin;Kim, Jong-Youl;Park, Jin-Nam;Shin, Young-Hee
    • Journal of Pharmaceutical Investigation
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    • v.37 no.6
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    • pp.365-368
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    • 2007
  • The primary aim of this study was to investigate the enhancement effect of low-frequency ultrasound on skin permeation. In vitro permeation experiments were performed using Franz modified diffusion cells with ketoprofen as model drug. The effect of various ultrasound factors-ultrasound application mode (continuous mode and discontinuous mode), ultrasound intensity (0.26 $W/cm^2$, and 0.29 $W/cm^2$) and duty cycle (3%, 16%, 50%, and 83%) were studied. The highest permeation was observed at 0.29 $W/cm^2$ intensity, 50% duty cycle, and discontinuous mode. The result suggested the feasibility of low frequency ultrasound application for the phonophoretic transdermal drug delivery system.

Establishment Percutaneous Administration Method in Beagle Dog

  • Han, Su-Cheol;Bae, Ju-Hyun;Cha, Shin-Woo;Jiang, Cheng-Zhe;Tarumoto Y.;Kim, Choong-Yong;Chung, Moon-Koo
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2003.10b
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    • pp.154-154
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    • 2003
  • The primary routes of drug administration include oral, intramuscular, subcutaneous and intravenous dosing for toxicological risk assessment purpose in dog. There has been an increase applying transdermal patches as an alternate method for systemic delivery. The present study was performed to establish the transdermal delivery method of medicated ointment, liquid and powder material to beagle dog.(omitted)

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Skin Irritation Test of Clonidine Patch (Clonidine Patch에 피부자극성 시험)

  • 이영순;박우일;고광호
    • Biomolecules & Therapeutics
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    • v.4 no.2
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    • pp.202-204
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    • 1996
  • Clonidine, an antihypertensive drug, stimulates postsynaptic $\alpha_2$adrenergic receptors in the CNS and lowers arterial pressure by erects on both cardiac output and peripheral resistance. However, many patients experience that sedation and xerostomia occured upon oral administration of clonidine. These side effects are due to high plasma peak concentration and can be avoided when clonidine is given transdermally. In this study, we performed the skin irritation test for transdermal administration of clonidine patch on New Zealand white rabbits. Twelve New Zealand white rabbits were divided into two groups according to the dose levels, respectively. After transdermal administration of clonidine patch with two doses, clinical manifestations, body weight loss and postmortem findings were observed. We could not find any significant evidence of skin irritation by transdermal administration of clonidine patch.

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Transdermal Permeation Characteristics of Anti Cholesterol Ointment using Nicotinic acid N-oxide (Nicotinic acid N-oxide를 이용한 항콜레스테롤 연고의 경피 투과 특성)

  • Jung, Duck-Chae;Kim, Kyu-Won
    • Journal of the Korean Applied Science and Technology
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    • v.25 no.2
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    • pp.123-129
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    • 2008
  • Transdermal therapeutic system(TTS) is often used as the method of drug dosage into the epidermic skin. Natural polymer were selected as ointment material of TTS. We investigated the permeation of natural polymer ointment containing drug in rat skin using horizontal membrane cell model. Permeation properties of materials were investigated for water-soluble drug such as Nicotinic acid N-oxide in vitro. These results showed that skin permeation rate of drug across the composite was mainly dependent on the property of ointment base and drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate. This result suggests a possible use of natural polymer ointment base as TTS of antihyperlipoproteinemic agent.

Progressive nicotine poisoning by multiple transdermal nicotine patches

  • Kang, Jeong Ho;Lee, Sung Kgun
    • Journal of Medicine and Life Science
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    • v.18 no.2
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    • pp.31-34
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    • 2021
  • The pharmacokinetic properties of transdermal nicotine patches (TNPs) are different from those of other routes of nicotine administration; further, acute nicotine poisoning by TNPs may present with different clinical features. In the present report, we describe the case of a 23-year-old woman who was admitted to emergency department (ED) at Jeju National University Hospital with loss of consciousness. Five hours before the ED visit, she used multiple TNPs to attempt suicide. Initially, nausea and vomiting occurred, and the symptoms worsened over time. We immediately removed the TNPs, and the application sites were gently washed with sterile water. The patient's level of consciousness gradually improved, and she fully recovered an altered mental status 5 hours later. Her initial urinary cotinine level was 324 ng/mL. Physicians should be aware that acute nicotine poisoning by TNPs can cause various toxic symptoms.

Enhanced Transdermal Delivery of Procaine Hydrochloride by lontophoresis -Comparison of Synergic Effect of High Voltage Current and Ultrasound- (이온도입에 의한 염산프로카인의 경피전달 증대 -고전압전류 및 초음파 병행의 상승효과 비교-)

  • Lee, Jong-Sook;Kim, Kyoung-Won;Lee, Jae-Hyoung;Choi, Yeong-Wook;Lee, Jae-Hwi
    • Journal of Pharmaceutical Investigation
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    • v.36 no.3
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    • pp.185-192
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    • 2006
  • The purpose of this study was to determine the effects of iontophoresis on transdermal delivery of procaine hydrochloride in healthy volunteers, as well as to the synergic effect of high voltage current or ultrasound on the efficacy of transdermal delivery of iontophoresis. Forty healthy volunteers were randomly assigned to four groups topical application group (TA), iontophoresis group (IT), pre-treatment of high voltage current stimulation with iontophoresis (HVS + IT), and pre-treatment of ultrasound application with iontophoresis (US + IT). All subjects received procaine iontophoresis on the forearm using direct current with 4 mA f3r 15 minutes. All subject was measured the duration of local anesthesia, pressure pain threshold, pain perception threshold using rectangular wave at 0.2 ms, 1 ms, 50 ms of rectangular current stimulation after procaine iontophoresis. For comparisons of the sensory characteristics and efficacy of iontophoresis between the groups, an one-way ANOVA and Kruskal-Wallis were used. The significant difference the duration of local anesthesia were found between the groups (p<0.001). The local anesthetic duration of IT, HVS+IT were significantly longer than TA. Meanwhile, the local anesthetic duration of US+IT was significantly longer than HVS+IT, IT and TA group (p<0.05). Also, the pressure pain threshold, pain perception threshold at 0.2 ms, 1 ms, 50 ms were significant difference between the groups (p<0.001). All sensory characteristics including pressure pain threshold, pain perception threshold of IT, HVS+IT was significantly increased than TA, whereas, US+1T was significantly increased HVS+1T, IT and TA (p<0.05). This study showed that the procaine iontophoresis have increase the duration of local anesthesia concomitantly pressure pain threshold and pain perception threshold of sensory nerve fibers such as $A-{\beta}$, $A-{\delta}$ and C fiber. This findings suggest that the iontophoresis enhanced the transdermal delivery of drug ions in vivo. The combination of ultrasound application and iontophoresis synergized the transdermal delivery of drug ions. It is suggests that an electric field, mechanical and heating property of ultrasound may contribute to synergic effect due to temporary changes of structure in the stratum corneum.