• Title/Summary/Keyword: Transdermal Drug Delivery

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Transdermal Delivery System of Triamcinolone Acetonide from a Gel Using Phonophoresis

  • Yang Jae-Heon;Kim Dae-Keun;Yun Mi-Young;Kim Tae-Youl;Shin Sang-Chul
    • Archives of Pharmacal Research
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    • v.29 no.5
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    • pp.412-417
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    • 2006
  • Triamcinolone acetonide (TA) is a corticosteroid that is used in the systemic and topical treatment of many inflammatory diseases. In this study, a phonophoretic drug delivery system was designed to enhance the TA permeability and the influence of ultrasound was examined. In order to establish the transdermal delivery system for TA, a hydrophilic carbopol gel containing TA was prepared after adopting phonophoresis. A permeation study through mouse skin was performed at $37^{\circ}C$ using a Franz diffusion cell, and the ultrasound treatment was carried out for 10 h. The level of TA permeation through the skin was evaluated under various ultrasound conditions including the frequency (1.0, 3.0 MHz), intensity (1.0, $2.5W/cm^2 $), and duty cycle (continuous, pulse mode) using a 0.5% TA gel. The highest permeation was observed under the ultrasound treatment conditions of low frequency, high intensity, and in continuous mode.

Transdermal Permeation of Xanthan Gum Bases on the Water-soluble and Lipophilic Antihyperlipoproteinemic Drugs (수용성과 지용성 항고지단백혈증제에 대한 Xanthan Gum 기재에서의 경피투과)

  • 이석우;임윤택;공승대;황성규;이우윤
    • KSBB Journal
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    • v.16 no.3
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    • pp.253-258
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    • 2001
  • Recently, there were many studies not only to enhance drug delivery effect but to reduce side effect. Drug delivery system(DDS) is able to improve efficiency with decreasing side effect of drug dosage. Among these application fields, DDS is often used as the method of drug dosage into the epidermic skin. We investigated characters of transdermal therapeutic system(TTS) and the skin permeability of that with applying DDS. We investigated the permeation of xanthan gum containing drug in rat skin using borizontal membrane cell model. Permeation properties of materials were investigated for water-soluble drug with oxiniacic acid and also for lipophilic drug with clofibrate. The permeation rate of lipophilic drug was found to be faster than that of water-soluble drug in vitro. The rate differences of both water-soluble drug and lipophilic drug according to drug content were negligible. We used glycerin, PEG 600 and oleic acid as enhancers. These results showed that skin permeation rate of each drug across the composite was mainly dependent on the property of base and chemical property of drug etc.. 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 base as a transdermal delivery system of antihyperlipoproteinemic agent.

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Development and Characterization of Membrane for Local Delivery of Cephalexin

  • Shin, Sang-Chul;Oh, In-Joon;Cho, Seong-Jin
    • Archives of Pharmacal Research
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    • v.19 no.1
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    • pp.1-5
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    • 1996
  • Laminated films composed of drug-containing reservoir layer and drug-free membrane were prepared. Zero-order drug release with lag time was achieved by laminating drug-free film onto the reservoir layer, while burst effect was observed on cast-on film. The rate controlling membrane was either attached to or cast directly into the reservoir. The release rate was independent on the reservoir composition but dependent on the composition of rate-controlling membrane. In growth inhibitory test of cephalexin from Eudragit RS film to Streptococcus Mutans, the disk even after release test for 72 hours showed more bacterial growth inhibition than that of control. Permeation of drug through rat skin was proportional to the HPC fraction in the film. We could control the release of cephalexin from the film by changing the fraction of Eudragit RS, HPC and DEP content. Consequently, Eudragit RS/HPC film was found to be very effective system for local delivery of drugs.

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Preparation and Evaluation of Aceclofenac Microemulsion for Transdermal Delivery System

  • Yang, Jae-Heon;Kim, Young-Il;Kim, Kyung-Mi
    • Archives of Pharmacal Research
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    • v.25 no.4
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    • pp.534-540
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    • 2002
  • To develop novel transdermal formulation for aceclofenac, microemulsion was prepared for increasing its skin permeability. Based on solubiity and phase studies, oil and surfactant was selected and composition was determined. Microemulsion was spontaneously prepared by mixing ingredients and the physicochemical properties such was investigated. The mean diameters of microemulsion were approximately 90 nm and the system was physically stable at room temperature at least for 3 months. In addition, the in vitro and in vivo performance of microemulsion formulation was evaluated. Aceclofenac was released from microemulsion in acidic aqueous medium, and dissolved amounts of aceclofenac was approximately 30% after 240 min. Skin permeation of aceclofenac from microemulsion formulation was higher than that of cream. Following transdermal application of aceclofenac preparation to delayed onset muscle soreness, serum creatine phosphokinase and lactate dehydrogenase activity was significantly reduced by aceclofenac. Aceclofenac in microemulsion was more potent than cream in the alleviation of muscle pain. Therefore, the microemulsion formulation of aceclofenac appear to be a reasonable transdermal delivery system of the drug with enhanced skin permeability and efficacy for the treatment of muscle damage.

Multifunctional Transdermal Diffusion Test System (다기능 경피 확산 테스트 시스템 설계 및 제작)

  • Gao, Mengyan;Jin, Hu;Piao, Xiang Fan
    • Journal of the Korean Society of Manufacturing Process Engineers
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    • v.19 no.10
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    • pp.8-15
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    • 2020
  • The diffusion cell method is the main technique employed for the in vitro diffusion test of transdermal drug delivery preparations. Most existing transdermal diffusion devices use a water bath heating structure and direct current motor magnetic stirrer. However, these devices are confronted with problems, such as large volume, incompatible vertical and horizontal diffusion cells, few diffusion cell sets, and poor reliability. To overcome these deficiencies, the system adopts a dry heating method and uses a rotating magnetic field generated by the electromagnetic stirrer to drive the magnetic stirrer. Accordingly, the resulting device is characterized by a simple structure and small volume, convenient operation, compatible vertical and horizontal diffusion cells, and numerous diffusion cell sets. The reliability and practicability of the system is verified by the in vitro percutaneous permeability test of the bisoprolol patch.

Development of Micro-needle Device for Direct Drug Delivery into the Dermis (직접약물전달형 마이크로니들 장치)

  • Eum, Nyeon-Sik;Kim, Hyung-Kyung;Han, Jung Hyun;Kim, Su-Jeong;Park, Hee-Joon;Kang, Shin-Won
    • Journal of Biomedical Engineering Research
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    • v.33 no.4
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    • pp.202-206
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    • 2012
  • In this study, we developed transdermal direct drug delivery device using micro-needle painlessly. We has fabricated micro-needle that is 130 ${\mu}m$ thickness and 250 ${\mu}m$length with 10 ${\mu}m$ spiral groove for rolling down drug. Head part of micro-needle device is composed of 20ea micro-needles, an on-off valve and a protective cap. Glass bottle for containing drug is connected to head part of micro-needle device. We examined the puncture characteristic testing using porcine skin and drug delivery testing using porcine, rat skin with Indian Ink.

Proliposomal Clenbuterol Patch for Transdermal Delivery (프로리포솜을 이용한 클렌부테롤의 경피흡수 제제화)

  • Lee, Young-Joo;Chung, Suk-Jae;Lee, Min-Hwa;Shim, Chang-Koo
    • Journal of Pharmaceutical Investigation
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    • v.27 no.4
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    • pp.303-311
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    • 1997
  • Proliposomal patch of clenbuterol, ${\beta}_2-agonist$ bronchodilator, was prepared and its feasibility as a novel transdermal drug delivery system was examined. Proliposomal granules containing clenbuterol was prepared by a standard method using sorbitol and lecithin with (Rx 2) or without cholesterol (Rx 1). The porous structure of sorbitol in the proliposomes was maintained allowing tree flowability of the granules. Following contact with water, the granules were converted probably to liposomes almost completely within several minutes. It indicates that proliposomes may be hydrated, when they are applied on the skin under occlusive condition in vivo, by the sweat to form liposomes. Clenbuterol release from Rx 1 and Rx 2 proliposomes to pH 7.4 isotonic phospate buffer (PBS) across cellulose membrane (mol. wt. cut-off of 12000-14000) was retarded significantly compared with that from the mixture of clenbuterol powder and blank proliposomes. Interestingly, proliposomes prepared with lecithin and cholesterol (i.e., Rx 2 proliposomes) showed much more retarded release of clenbuterol than proliposomes prepared only with lecithin (i.e.. Rx 1 proliposomes), indicating that clenbuterol release from proliposomes can be controlled by the addition of cholesterol to the proliposomes. Proliposomal patches were prepared using PVC film as an occlusive backing sheet, two sides adhesive tape (urethane, 1.45 mm thickness) as a reservoir for proliposome granules and Millipore MF-membrane (0.45 mm pore size) as a drug release-controlling membrane. Rx 1 or Rx 2 proliposomes containing 4.6 mg of clenbuterol were loaded into the reservoir of the patch. Clenbuterol release from the patches to pH 7.4 PBS was determined using USP paddle (50 rpm)-over-disc release method. Clenbuterol release from the proliposomal patches was much more retarded even than from a matrix type clenbuterol patch (Boehringer Ingelheim ltd). Being consistent with clenbuterol release from the proliposomal granules, the release from the patches was highly dependent on the presence of cholesterol in the proliposomes : Patches containing Rx 2 proliposomes showed several fold slower drug release than patches containing Rx 1 proliposomes. When the patch containing Rx 1 proliposomes was applied on to the back of a hair-removed rat, clenbuterol concentration in the rat blood was maintained during 6-72 hrs. Transdermal absorption of clenbuterol from the patch was accelerated when the patch was prehydrated with 50 ml of pH 7.4 PBS before topical application. Above results indicate that sustained transdermal delivery of clenbuterol is feasible using proliposomal patches if the cholesterol content and pore size of the release rate-controlling membrane of patches, for example, are appropriately controlled.

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Transdermal Permeation of $[{^3}H]Acyclovir$ Using Niosome (니오솜을 이용한 $[^{3}H]$아시클로버의 경피투과)

  • Park, Sae-Hae;Lee, Soon-Young;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.28 no.1
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    • pp.43-50
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    • 1998
  • Niosomes are vesicles formed from synthetic non-ionic surfactants, offering an alternative to chemically unstable and expensive liposomes as a drug carrier. Non-ionic surfactant and cholesterol mixture film leads to the formation of vesicular system by hydration with sonication method. The formation of niosome was ascertained by negative staining of TEM. The entrapment efficiency of niosomal suspension was gradually increased with increasing the ratio of cholesterol to surfactant. It was found that the niosome with 6 : 4 (polyoxyethylene 2-cetyl ether: cholesterol) ratio was more stable than those with other ratios. The topical application of acyclovir(ACV) in the treatment of herpes simplex virus type 1(HSV-1) skin disease has a long history. There are an increasing number of reports, however, in which topical ACV therapy is not as effective as oral administration. Lack of efficacy with topical ACV has been hypothesized to reflect the inadequate delivery of drug to the skin. We investigated the permeation of niosome containing $[^{3}H]ACV$ in hairless mouse skin using Franz diffusion cell model. Permeation coefficient(P) of aqueous ACV was $6.7{\times}10^{-4}\;(cm/hr)$ and that of ACV in niosome was $23.4{\times}10^{-4}\;(cm/hr)$, suggesting about 3.5 times increase in the transdermal permeation.

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