• Journal of Pharmaceutical Investigation
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• 제37권2호
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• pp.85-94
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• 2007

The objective of this study is to prepare a stable delivery systems containing polyethoxylated retinamide(PERA) - derivatives of retinoic acid, effective anti-wrinkle and anti-acne agent. Cubic liquid crystalline phase gel (CLCPG) and cubosomes containing various concentrations of PERA were prepared to investigate the physicochemical properties. Furthermore, stability and transdermal absorption efficacy of the CLCPG containing PERA were investigated in comparison with oil-in-water (O/W) emulsions which are predominantly used as a topical formulation. CLCPG increase the stability of PERA in comparison with O/W emulsion. For tropical application, CLCPG containing PERA shows higher moisturizing effect than that of O/W emulsion. In skin permeation test, CLCPG shows higher PERA deposit on epidermis. With its specific physicochemical property caused by the glyceryl oleate, CLCPG itself could be used for stabilizer of various actives and applied as an effective delivery system for topical application. Cubosome, nano-sized dispersed CLCPG, is also expected to be applied in a various field of industry like food, cosmetics and pharmaceuticals.

• Journal of Pharmaceutical Investigation
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• 제32권4호
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• pp.259-265
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• 2002

Piroxicam is one of the NSAID, which is used in the systemic and topical treatment of a variety of inflammatory conditions. Conventionally, for topical use, the drug is formulated in gel. We designed an phonophoretic drug delivery system to investigate the piroxicam permeability and the influence of ultrasound application (continuous mode, pulsed mode), frequency (1.0 MHz, 3.0 MHz) and intensity $(1.0\;w/cm^2,\;1.5\;w/cm^2,\;2.0\;w/cm^2)$ with 0.5% piroxicam gel. Per cutaneous absorption studies were performed in vitro models to determine the rate of drug absorption via the skin. Permeation study using hairless mouse skin was performed at $37^{\circ}C$ using buffered saline (pH 7.4, 10% propylene glycol solution) as the receptor solution. Anti-inflammatory activity was determined using carrageenan-induced foot edema model in rat. A pronounced effect of ultrasound on the skin absorption of the piroxicam was observed at all ultrasound energy level studied. Ultrasound was carried out for 10 hr. The highest permeation was observed at intensity of $2.0\;w/cm^2$, frequency of 1.0 MHz and continuous output. The inclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory activity in vivo.

• International Journal of Precision Engineering and Manufacturing
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• 제9권3호
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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.

• Journal of Pharmaceutical Investigation
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• 제32권3호
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• pp.161-164
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• 2002

Gentisic acid is a skin-whitening agent which inhibits the tyrosinase activity, an essential enzyme in the process of biological synthesis of melanin. Since melanin is synthesized in melanocytes located between the viable epidermis and dermis layer, drug amount delivered into the epidermis/dermis layer can provide valuable information for the biological effect of skin-whitening agents. The purpose of this study was to prepare the gentisic acid patches with 2% dodecylamine as enhancer, and to observe the in vitro skin permeation and in vivo skin deposition of gentisic acid. Gentisic acid in DuroTak 87-2510 patch formulation permeated across hairless mouse skin at the rate of $40.79\;{\mu}g/cm^2/hr$. In vivo study showed that the gentisic acid amount in both the stratum corneum and the viable epidermis/dermis increased with the increase of application time. The amount of gentisic acid in the stratum corneum was higher than that in the epidermis/dermis layer, and was expected to provide a reservoir effect even after removing the patches. Thus, the patch formulation seems to be useful for the topical delivery of skin-whitening agent into the epidermis/dermis layer, the target site.

• Journal of Pharmaceutical Investigation
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• 제37권4호
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• pp.211-216
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• 2007

The bark of Alnus japonica has been used for the treatment of fever, hemorrhage and diarrehea in oriental traditional medicine. Recently, it was revealed that the diarylheptanoids from the bark of Alnus japonica possess anti-inflammatory activity and are expected to be applicable for atopic dermatitis. In this study, oregonin, one of major active components in the bark of Alnus japonica, was developed in the form of semisolid formulations for topical delivery. Oregonin was incorporated into four ointment bases: O/W cream, W/O cream, hydrophilic ointment and lipophilic ointment. Oregonin release from all formulation prepared was evaluated. Franz cell method and immersion method were employed to characterize the release patterns of drug from each formulation based on solvent availability. O/W cream showed a better release profile than the other formulations when evaluated with Franz cell method with an order of O/W cream, hydrophilic ointment, W/O cream and lipophilic ointment. In the immersion method, hydrophilic ointment showed the greatest release rate at times 1 hour exceeding compared to other bases with an order of hydrophilic ointment, O/W cream, W/O cream and lipophilic ointment. Hydrophilicity and solvent availability of formulation seems to significantly influence the release rate of oregonin from ointment bases. In this study, we successfully characterized the oregon in ointment and found that o/w cream is a promising formulation for the topical delivery of oregonin.

• Macromolecular Research
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• 제17권12호
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• pp.969-975
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• 2009

This article describes the topical delivery and localization of budesonide through the hairless mouse skin. Two poly(ethylene oxide)-block-poly($\varepsilon$-caprolactone)-block-poly(ethylene oxide) (PEO-PCL-PEO) triblock copolymers (T 222 and T 252) having different CL:EO ratios were added in the preparation of budesonide particles stabilized with poly(vinyl alcohol) (PVA) and Tween 80 under ultrasonication. For comparison, a commercial PEO-PPO-PEO triblock copolymer (F68) was studied under the same condition. To demonstrate the effects of the triblock copolymer, the particle size of budesonide emulsion, entrapment efficiency, and in vitro release were measured and compared. The budesonide particles stabilized by the triblock copolymers had a diameter of ca. 350 nm with entrapment efficiencies of 66-76%. The In vitro release profiles of all samples showed an initial burst followed by sustained release. The skin penetration and permeation of budesonide were analyzed by using a Frantz diffusion cell. T 222 and T 252 exhibited higher total permeation amounts, but lower budesonide penetration amounts, than F68. The results suggest that the partitioning of budesonide in each skin layer can be adjusted in order to avoid skin thinning and negative immune response arising from the penetration of budesonide in blood vessels.

• The Journal of Korean Physical Therapy
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• 제23권6호
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• pp.77-84
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• 2011

Purpose: The objectives of this study were to determine the enhancing effect of iontophoresis method as it transdermally deliver methylene blue (MB) using visual examination, in terms of penetration depth and tissue distribution in the skin, and to determine the effect of application duration on the efficacy of iontophoresis. Methods: Twenty-four male Sprague-Dawley rats were randomly divided into 5-, 10-, 20-, and 40-minute groups. These rats were exposed to either topical or anodic iontophoresis of 1% MB using a direct current of $0.5mA/cm^2$ for 5, 10, 20, and 40 minutes. Using cryosections of rat tissues, the penetration depth of MB was measured using light microscopy. Results: Significant differences in the penetration depth (F=54.20, p<0.001) were detected among the four groups. Post hoc comparisons of the penetration depth of MB data pooled across groups showed no significant difference between all topical application groups and 5-minute iontophoresis group, but did reveal a significant difference in the penetration depth between all topical application groups and 5-minute iontophoresis group versus 10-minute group, between the 10-minute and 20-minute group, and between the 20-minute and 40-minute iontophoresis group (p<0.05). Conclusion: The results demonstrate that iontophoresis enhances transdermal delivery of MB across stratum corneum of skin barrier by visual examination. Furthermore, the penetration depth of iontophoretic transdermal delivery of MB was dependent on the application duration. The duration of iontophoresis is one of the important factor in the efficacy of iontophoresis application.

• 한국항공우주학회지
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• 제36권6호
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• pp.587-593
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• 2008

본 연구의 목적은 신체 조직의 손상을 최소화할 수 있는 경피(transdermal) 및 국부적인(topical) 약물전달을 가능하게 하는 마이크로 입자가속시스템 개발에 있다. Ballistic 역학을 기반으로 하는 본 방법을 통하여 체순환을 위한 경피 및 국부적 약물 전달이 가능하다. 얇은 금속 포일의 한 쪽 면에 마이크로 입자들을 얹어놓고 뒷면에 레이저를 조사하면 충격파가 발생하고, 이 충격파는 포일을 통과하며 포일의 끝에서 금속-공기간의 acoustic impedance 차이로 expansion wave로 반사되어 포일이 반대 방향으로 변형을 일으키게 한다. 이 순간적인 변형으로 인해 포일에 붙어있던 마이크로 입자들이 가속되어 튕겨 나가게 된다. 입자들이 가속되는 속도가 굉장히 크기 때문에 이들은 신체 조직을 침투할 만한 충분한 운동량을 갖고 있다. 입자들의 침투 여부를 확인하기 위해 우리는 5${\mu}m$ 크기의 코발트 입자들을 연조직을 묘사하는 젤라틴에 가속시켰으며, 주목할 만한 침투 깊이를 얻으며 실험에 성공하였다.

• 약학회지
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• 제56권3호
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• pp.152-157
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• 2012

Angelica gigas is one of the most widely used herbal medicines in Asia. Root extract of Angelica gigas is known to have anti-oxidant activity and skin whitening effect. The aim of this study was to prepare microemulsion system of root extracts of Angelica gigas for topical delivery. Microemulsion was successfully prepared by using MCT (medium chain triglyceride) as an oil phase, Labrasol as a surfactant, and the mixture of propyleneglycol and phosphatidylcholine (4 : 1) as a cosurfactant. In vitro and in vivo skin permeation and deposition of decursin, as a marker, was determined using hairless mouse. Microemulsion significantly increased the in vitro skin permeation of decursin for up to 12 hours and was significantly higher than the control (water). Moreover, microemulsion formulation showed significantly higher skin deposition of decursin compared to the control in both in vitro and in vivo studies. Thus, microemulsion could be a useful vehicle for topical application of root extracts of Angelica gigas.

• BMB Reports
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• 제46권1호
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• pp.17-24
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• 2013

Transcutaneous immunization refers to the topical application of antigens onto the epidermis. Transcutaneous immunization targeting the Langerhans cells of the skin has received much attention due to its safe, needle-free, and noninvasive antigen delivery. The skin has important immunological functions with unique roles for antigen-presenting cells such as epidermal Langerhans cells and dermal dendritic cells. In recent years, novel vaccine delivery strategies have continually been developed; however, transcutaneous immunization has not yet been fully exploited due to the penetration barrier represented by the stratum corneum, which inhibits the transport of antigens and adjuvants. Herein we review recent achievements in transcutaneous immunization, focusing on the various strategies for the enhancement of antigen delivery and vaccination efficacy.