• Title/Summary/Keyword: Transdermal System

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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.

Development of Porous Cellulose-Hydrogel System for Enhanced Transdermal Delivery of Quercetin and Rutin (Quercetin과 Rutin의 피부 흡수 증진을 위한 셀룰로오스 다공성 하이드로젤 제형 개발)

  • Lee, Min Hye;Kim, Su Ji;Park, Soo Nam
    • Polymer(Korea)
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    • v.37 no.3
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    • pp.347-355
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    • 2013
  • In this study, the porous cellulose hydrogel as a carrier to enhance the skin delivery of quercetin and its glycoside, rutin known as flavonoid antioxidants was prepared and its properties were investigated. The optimum cellulose hydrogel for quercetin and rutin was made by the reaction of 2 wt% cellulose with 12% ECH. In the release test of the hydrogel containing the flavonoids, the release of quercetin was diffusion-controlled at $10{\sim}500{\mu}M$, but rutin was released by the erosion of hydrogel system at $10{\sim}50{\mu}M$. Both the encapsulation efficiency and release amount of rutin in hydrogel were higher than quercetin. However, in skin permeation experiment using Franz diffusion cell, quercetin showed higher skin permeation capacity than rutin. The hydrogel containing flavonoids showed remarkable transdermal permeation than the control group. These results suggest that porous cellulose hydrogel is potential drug delivery system to enhance transdermal permeation of water-insoluble flavonoid antioxidants.

Comparison of the Postoperative Pain Control Effects of a Buprenorphine Transdermal Patch on Total Knee Arthroplasty Surgery Patients according to Its Applied Sites: Retrospective Case-Control Study (슬관절 인공관절 전치환술 환자에서 부프레노르핀 경피 패치의 적용부위에 따른 수술 후 통증 조절 효과 비교: 후향적 환자-대조군 연구)

  • Kim, Ok-Gul;Lee, Sang-Wook;Kim, Hyun-Min
    • Journal of the Korean Orthopaedic Association
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    • v.55 no.6
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    • pp.527-533
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    • 2020
  • Purpose: This study compared the effects of a buprenorphine transdermal patch (BTDP) on the chest and knee for pain control after total knee arthroplasty (TKA). Materials and Methods: A retrospective case-control study was conducted from August 2018 to August 2019 on 231 patients who underwent TKA. Two hundred cases were selected considering age, sex, and body mass index. Before and after applying the BTDP, the Numeric Rating Scale (NRS), adverse effects and compliance were measured. All measurements in the chest application group (group A=100) and knee application group (group B=100) were compared. Results: NRS was similar in rest between the groups treated with BTDP, but at two days and three days afternoon, five, six, and seven days postoperatively in group B, the NRS was significantly lower than that of group A. The adverse effects of the central nervous system and gastrointestinal system after applying BTDP were significantly lower in group B than in group A. No significant differences in adverse effects of the cardiovascular system and skin were observed between the two groups. Regarding the maintenance of BTDP, group B was significantly higher than group A. Conclusion: The direct application of BTDP after TKA to painful knee joints showed excellent results in early postoperative pain control and can be a useful method for increasing patient compliance by reducing the frequency of adverse effects.

In Vitro Percutaneous Absorption of Ondansetron Hydrochloride from Pressure-sensitive Adhesive Matrices through Hairless Mouse Skin

  • Gwak, Hye-Sun;Oh, Ik-Sang;Chun, In-Koo
    • Archives of Pharmacal Research
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    • v.26 no.8
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    • pp.644-648
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    • 2003
  • To investigate the feasibility of developing a new ondansetron transdermal system, the effects of vehicles and penetration enhancers on the in vitro permeation of ondansetron hydrochloride (OS) from a pressure-sensitive adhesive (PSA) matrices across dorsal hairless mouse skin were studied. Vehicles employed in this study consisted of various ratios of propylene glycol monocaprylate (PGMC)-diethylene glycol monoethyl ether (DGME) co-solvents and PGMC-propylene glycol (PG) co-solvents with 3% oleic acid. $Duro-Tak^\circledR$ 87-2100 and $Duro-Tak^\circledR$ 87-2196 were used as PSAs. The concentration of DGME in PGMC-DGME co-solvent system affected the release rate; as the concentration of DGME increased, the release rate decreased. The cumulative release amount of OS increased as the ratio of PSA to drug solution decreased. The permeation flux was also primarily affected by the amount of PSAs; as the amount decreased, the permeation flux increased. The overall fluxes from matrix formulations were significantly lower when compared to those obtained from solution formulations. The ratio of PG to PGMC did not affect permeation flux, while the lag time decreased significantly from $5.14\pm3.31 to 0.31\pm0.12$ h as the PG increased from 40% to 60%.

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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Study on the Influence of Cubic Liquid Crystalline Phases of Monoolein on the Stability and Transdermal Delivery of Retinylpalmitate (Monoolein액정상이 Retinylpalmitate의 안정성과 경피전달에 미치는 효과에 관한 연구)

  • Lee, Kyoung-Gum;Kang, Myung-Joo;Choi, Young-Wook;Lee, Jae-Hwi
    • Journal of Pharmaceutical Investigation
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    • v.37 no.4
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    • pp.243-247
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    • 2007
  • Retinoids have many important and diverse functions and particularly, have been widely used as anti-aging agent and for the treatment of acne and psoriasis in cosmetics. However, retinoids have low stability against the air, light, water, oxygen and heat, thus, to stabilize the retinoids in formulations is very critical procedure. In this study, cubic liquid crystalline phase of monoolein was applied to stabilize the retinylpalmitate (RP) and to enhance the transdermal permeation. Cubic liquid crystalline phase significantly enhanced the stability of RP. After 15 days, the content of RP in the cubic formulation was 94.7% while the content of RP in ethanol solution was below 0.5% at room temperature. Although BHT containing crystalline phase showed the slightly increased stability of RP, there were no significant differences in RP stability between with or without antioxidants (ascorbic acid, ${\alpha}$-tocopherol, BHT, BHA) at $40^{\circ}C$. The skin retention of RP in crystalline formulations was approximately $5.3{\sim}6.4$ times greater than that of o/w cream formulation. Incorporation of RP into cubic liquid crystalline phase of monoolein effectively stabilized the RP and worked as excellent topical vehicle for RP. Liquid crystalline phase is considered to be suitable formulation for RP for topical delivery system as a stabilizer and permeation enhancing agent.

Formulation of Microemulsion Systems for Transdermal Delivery of Aceclofenac

  • Lee, Jae-Hwi;Lee, Yoon-Jin;Kim, Jong-Seok;Yoon, Mi-Kyeong;Choi, Young-Wook
    • Archives of Pharmacal Research
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    • v.28 no.9
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    • pp.1097-1102
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    • 2005
  • An O/W microemulsion system was developed to enhance the skin permeability of ace-clofenac. Of the oils studied, Labrafil? M 1944 CS was chosen as the oil phase: of the microemulson, as it showed a good solubilizing capacity. Pseudo-ternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, Cremophor ELP, and co-surfactant, ethanol, for micoemulsion formation. Eight different formulations with various values of oil of $6-30\%$, water of $0-80\%$, and the mixture of surfactant and co-surfactant (at the ratio of 2) of $14-70\%$. The in vitro transdermal permeability of aceclofenac from the microemulsions was evaluated using Franz diffusion cells mounted with rat skin. The level of aceclofenac permeated was analyzed by HPLC and the droplet size' of the microemulsions was characterized using a Zetasizer Nano-ZS. Terpenes were added to the microemulsions at a level of $5\%$, and their effects on the skin permeation of aceclofenac were investigated. The mean diameters of the microemulsions ranged between approximately $10\~100nm$, and the skin permeability of the aceclofenac incorporated into the microemulsion systems was 5-fold higher than that of the ethanol vehicle. Of the various terpenes added, limonene had the best enhancing ability. These results indicate that the microemulsion pystem studied is a promising tool for the percutaneous delivery of aceclofenac.

Study of stabilizing and efficacy evaluation in human of Oleanoic acid with poly-glyceryl nano emulsion system (올레아노익산의 폴리글리세릴계 나노에멀젼에서의 안정화 및 인체적용 유효성평가에 대한 연구)

  • Han, Sang-Keun;Lee, Dong-Kyu
    • Journal of the Korean Applied Science and Technology
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    • v.32 no.1
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    • pp.157-164
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    • 2015
  • Oleanolic acid is known as which anti-cancer, anti-sinhaeng angiogenic, anti-inflammatory, antioxidant and anti-wrinkle effects. We focused on the antioxidant activity of oleanolic acid was separated from the natural plant and It was confirmed that the whitening effect. In this study, oleanolic acid was stabilized by polyglyceryl surfactant which from natural origin with only a simple stirring operation, and compared with lecithin liposome that was manufactured with high cost facility. The transdermal transition rate of 0.4% oleanolic acid polyglyceryl nanoemulsion was 95%, and it was simillar with lecithin liposome of 92%. 65% of 3hr transdermal transition rate of polyglyceryl nanoemulsion indicate charistiristcs of quick release, compared with 45% of lecithin liposome's 3hr transdermal transition rate. In the in-vivo clinical trial test, polyglyceryl nanoemulsion of 0.4% oleanolic acid was higher 25% in 2nd week, 58% in 4th and 8th weeks than non-added oleanolic acid emulsion.

Transdermal Permeation Behavior of 5-FU using Microneedle (마이크로니들을 이용한 5-FU의 경피투과 거동)

  • Kim, Myoung-Jin;Park, Jung-Soo;Kim, Yun-Tae;Lee, Jun-Hee;Ahn, Sik-Il;Park, Jong-Hak;Mo, Jong-Hyun;Lee, Tae-Wan;Lee, Han-Koo;Khang, Gil-Son;Lee, Hai-Bang
    • Journal of Pharmaceutical Investigation
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    • v.38 no.1
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    • pp.45-50
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    • 2008
  • 5-Fluorouracil (5-FU) is an antimetabolic of the pyrimidine derivatives that is used in chemotherapy for the treatment of several types of cancer. 5-FU have poor oral absorption and short biological half-time and strong side effects. Microneedle introduced to find a solution of problems. Microneedle device with roll was manufactured for transdermal delivery of various drugs. 5-FU was mixed in non-ionic surfactant such as tween 20 and tween 80. Camscope was used to analysis the permeation magnitude of treated skin by microneedle and trypan blue staining. The 5-FU solution with surfactant measured by ZETA-potential analysis system for stability of solution. The skin permeation rate of 5-FU determined by HPLC. We confirmed that cross treated skin was dyed more deeply than parallel treated skin through trypan blue staining. The results indicate that skin permeation rate of 5-FU was increased with the treatment types and treatment times.