• Title/Summary/Keyword: Transdermal Drug Delivery

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Anesthetic Effect of Lidocaine Gel by Phonophoretic Transdermal Delivery (음파영동 경피투과에 의한 Lidocaine Gel의 마취효과)

  • Kim, Tae-Youl;Choi, Sug-Ju;Lee, Joon-Hee;Kim, Young-Il;Chung, Kyu-Ho
    • Journal of the Korean Academy of Clinical Electrophysiology
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    • v.1 no.2
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    • pp.11-19
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    • 2003
  • The purpose of this study investigated the anesthetic effects of lidocaine gel by phonophoretic transdermal delivery. The anesthetic effects were evaluated by two aspects as quantitative sensory testing and sensory nerve conduction study. Twelve healthy males(aged $23.25{\pm}2.09$ years) were studied. Exclusion criteria were ; pain, history of sensory disturbances and skin conditions in the areas to be examined. The subjects were divided into two groups; group I(lidocaine gel without ultrasound) and group II(lidocaine gel with ultrasound). The following results were obtained; 1. In changes of tactile threshold and electrical pain threshold, all groups were significantly increased(p<0.05). 2. In changes of electrical pain threshold, it was significantly differenced between the groups(p<0.05). We conclude that the transdermal delivery of lidocaine gel by phonophoresis has a possibility to use for surface anesthesia and the pain control of the superficial tissue.

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Development of Bio-ballistic Device for Laser Ablation-induced Drug Delivery

  • Choi, Ji-Hee;Gojani, Ardian B.;Lee, Hyun-Hee;Jeung, In-Seuk;Yoh, Jack J.
    • International Journal of Precision Engineering and Manufacturing
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    • v.9 no.3
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    • pp.68-71
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    • 2008
  • Transdermal and topical drug delivery with minimal tissue damage has been an area of vigorous research for a number of years. Our research team has initiated the development of an effective method for delivering drug particles across the skin (transdermal) for systemic circulation, and to localized (topical) areas. The device consists of a micro particle acceleration system based on laser ablation that can be integrated with endoscopic surgical techniques. A layer of micro particles is deposited on the surface of a thin metal foil. The rear side of the foil is irradiated with a laser beam, which generates a shockwave that travels through the foil. When the shockwave reaches the end of the foil, it is reflected as an expansion wave and causes instantaneous deformation of the foil in the opposite direction. Due to this sudden deformation, the microparticles are ejected from the foil at very high speeds, and therefore have sufficient momentum to penetrate soft body tissues. We have demonstrated this by successfully delivering cobalt particles $3\;{\mu}m$ in diameter into gelatin models that represent soft tissue with remarkable penetration depth.

Development of Transdermal Delivery Systems Containing Clenbuterol (클렌부테롤 경피흡수제제의 개발)

  • Choi, Han-Gon;Quan, Qi-Zhe;Jung, Si-Young;Rhee, Jong-Dal;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.30 no.4
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    • pp.247-252
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    • 2000
  • The advantages of transdermal administration are avoiding hepatic first pass effect, minimizing inter- and intra-patient variation, maintaining steady-state plasma level to provide long-term therapy from a single dose, and allowing a rapid termination of drug input. Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease. For the development of transdermal systems containing clenbuterol, two limiting factors - long lag time and low flux - must be overcome. In this study, we attempted to select optimal formulation for preparation of clenbuterol patch using hairless mouse skin and flow-through diffusion cell. The flux of clenbuterol increased as the percent of clenbuterol dose dependently in the concentration range of 5-15%. Based on this result, we fixed the concentration of clenbuterol as 15%. The effect of various penetration enhancers on percutaneous absorption of clenbuterol through hairless mouse skin was investigated. Labrafil was the most effective enhancer, which increased the permeability of clenbuterol approximately 4-fold compared with the control without penetration enhancer. Optimal enhancer concentration was 3%. The effect of various adhesives on penetration of clenbuterol was also investigated. Among the adhesives studied, MA-31 was the most effective adhesive. Furthermore, the clenbuterol patch composed of 15% clenbuterol, 3% Labrafil and 82% MA-31, which gave most excellent penetration of drug in in vitro penetration study, maintained therapeutic plasma levels in in vivo study using S.D. rats. These studies demonstrated a good feasibility of clenbuterol administration through the intact skin using a transdermal patch, and show a possibility of the development of clenbuterol patches.

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Transdermal Permeation of Riboflavin in Ointment Bases Using Gums & Enhancers (Gum류의 연고제제와 흡수촉진제가 Riboflavin의 경피흡수에 미치는 영향)

  • 오세영;황성규;김판기
    • Journal of Environmental Health Sciences
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    • v.26 no.2
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    • pp.91-96
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    • 2000
  • We investigated characters of transdermal therapeutic system(TTS) and the skin permeability of that with applying drug delivery system(DDS). Natural gums were selected as material of TTS. The permeation of natural gums ointment containing drug in rat skin using diffusion cell model. Permeation properties of materials were investigated for water soluble drug such as riboflavin in vitro. We used glycerin, PEG 600 and oleic acid as enhancers. Since dermis has more hydration than the stratum corneum, skin permeation rate at steady state was highly influenced when glycerin was used in riboflavin. The permeation rate of content enhancer and drug was found to be faster than that of content riboflavin only. These results showed that skin permeation rate of drug across the composite was mainly dependent on the property of ointment base and drug. All the gum ointment tested showed good safety. Proper selection of the materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.

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Development of shock wave induced microparticle acceleration system based on laser ablation and its application on drug delivery (충격파를 이용한 레이저 어블레이션 기반의 마이크로 입자 가속 시스템 개발 및 약물전달 응용)

  • Choi, Ji-Hee;Gojani, Ardian B.;Lee, Hyun-Hee;Yoh, Jai-Ick
    • Journal of the Korean Society for Aeronautical & Space Sciences
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    • v.36 no.6
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    • pp.587-593
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    • 2008
  • Transdermal and topical drug delivery with minimal tissue damage has been an area of vigorous research for years. Our research team has initiated the development of an effective method for delivering drug particles across the skin (transdermal) for systemic circulation, and to localized (topical) areas. The device consists of a laser ablation based micro-particle acceleration system that can be integrated with endoscopic surgical techniques. We have successfully delivered 3μm size cobalt particles into gelatin models that represent soft tissue with remarkable penetration depth.

Percutaneous Absorption Characteristics of Tacrine in Alzheimer-type Dementia Treatment (Alzheimer형 치매치료제인 Tacrine의 경피 투과 특성 연구)

  • Lee, Han-Seob
    • Journal of the Korean Applied Science and Technology
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    • v.29 no.4
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    • pp.552-560
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    • 2012
  • Drug delivery technologies are patent protected formulation technologies that modify drug release profile, absorption, distribution, and elimination for the benefit of improving product efficacy and safety, as well as patient convenience and compliance. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stop if the drug dosage lead to side effect. Polysaccharide, such as karaya gum and locust bean gum(LBG)/water-soluble chitosan oligomer(WSCO) were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, tacrine contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in tacrine such as lipophilic drug in vitro. We used glycerin, PEG 400, and PEG 800 as enhancers. Therefore, transdermal absorption of tacrine could be improved by changing vehicle composition or by using penetration enhancers. Especially it would be anticipated that the high permeation efficacy could be obtained by using vehicle that has enhancing effect for itself and by adding enhancers to it.

Design of Transdermal Delivery System Using New Film-Forming Agents (신규 필름형성제를 이용한 경피흡수제제의 설계)

  • Choi, Yang-Gyu;Kim, Young-So;Kim, Jung-Ju;Sim, Young-Chul
    • Journal of Pharmaceutical Investigation
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    • v.33 no.3
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    • pp.163-169
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    • 2003
  • In order to develop a film-forming transdermal drug delivery system, polyurethane (PU) based on poly(ethylene glycol) and poly(tetramethylene oxide) was synthesized and characterized. The synthesized PU was blended with Gantrez ES 225 (GT) to improve the adhesion property of film-forming agent to the skin. When film-forming gel formulation containing 3% ketoprofen (KP) was applied, transparent thin film was obtained within 5 minutes and adhered to the skin for 8 hours. In vitro percutaneous absortion studies were performed to determine the rate of ketoprofen absorption through guinea pig skin. A prominent effect of limonene on the skin permeability of ketoprofen was observed among the various skin permeation enhancers investigated. Considering mechanica properties of film and skin permeability of ketoprofen, 2% of limonene was optimal content in the film forming transdermal formulation.

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.

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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Calcitonin Transport through Skin Using Iontophoresis

  • Kim, Kyung-Min;Oh, Seaung-Youl
    • Journal of Pharmaceutical Investigation
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    • v.41 no.1
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    • pp.9-17
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    • 2011
  • The objective of this work is to study transdermal delivery of calcitonin using iontophoresis and to evaluate various factors which affect the transdermal transport. We have studied the effect of polarity, current density, drug concentration, penetration enhancers (isopropyl myristate [IPM] and ethanol) and laser treatment on transdermal flux and the results were compared. We also investigated the iontophoretic flux from microemulsions containing calcitonin together with oleic acid (OA) or IPM. In vitro flux study was performed at $33^{\circ}C$, using side-by-side diffusion cell and full thickness hairless mouse skin. Anodal delivery at pH 3.0 was much larger than cathodal and passive delivery, due to the positive charge of calcitonin. Cumulative amount delivered (CUM) by cathodal or passive delivery was close to zero for 10 hours. The pretreatment of skin by neat IPM markedly increased the CUM anodically. CUM increased as the current density, drug concentration or the duration of IPM treatment increased. Microemulsion containing IPM or oleic acid was prepared and the phase diagram was constructed. CUM also increased when IPM was incorporated into a microemulsion. OA microemulsion showed similar enhancing effect to IPM microemulsion. The delivery of calcitonin from 70% (v/v) ethanol aqueous solution showed a large increase in flux. Laser treatment of skin before flux experiment exhibited about 2 fold increase in total calcitonin amount transported for 12 hours, when compared to that delivered by IPM microemulsion. Based on these results, we have evaluated the possibility of delivering enough amount of calcitonin to reach the therapeutic level. The data suggest that it is highly possible to deliver clinically effective amount of calcitonin using iontophoresis patch with small area (<10 $cm^2$).