• Title/Summary/Keyword: Transdermal System

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EFFECT Of PYRROLIDONE DERIVATIVES ON MULTILAMELLAR LIPOSOMES OF STRATUM CORNEUM LIPID: A STUDY BY UV SPECTROSCOPY AND DIFFERENTIAL SCANNING CALORIMERY

  • Hong, Myo-Sook;Kim, Chong-Kook
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.286-286
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    • 1996
  • In order to elucidate the mechanism of action of transdermal absorption-enhancing compounds, i.e., pyrrolidone derivatives (2-pyrrolidone, 1-methyl-2-pyrrolidone, 1-ethyl-2-pyrrolidone, 1,5-dimethyl-pyrrolidone and 5-methyl-2-pyrrolidone), multilamellar liposome was prepared from the simulated stratum corneum lipid and employed as a model system for the barrier function of the stratum corneum. The liposomal membrane of the stratum corneum lipid liposome (SCLL) behaves as an osmometer and has an excellent barrier function. In addition, its phase transition temperatures are similar to those of human stratum corneum intercellular lipid region. Therefore, SCLL seems to be a useful skin model. To estimate the barrier function of SCLL, the osmotic behavior of SCLL was measured in the presence of pyrrolidone derivatives and the effect on the phase transition temperature of SCLL was also investigated using differential calorimetry. Above a certain concentration (MLAC), enhances perturb the barrier function of the liposome. The relationship between MLACs and the partition coefficient of the pyrrolidone derivatives was observed; the greater the partition coefficients, the smaller the MLAC. This suggests that the more hydrophobic enhancers penetrate into the lipid layer more easily and reduce the barrier function of membrane more effectively. The results of differential scanning thermograms of the SCLL suggest that the pyrrolidone derivatives had incorporated into the lipid layer in the liposome and increased the fluidity of the lipid layer in the liposome. Such activity might have some correlation with the transdermal absorption-enhancing activity these compounds.

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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.

Transdermal Delivery System of Effective Ingredients for Cosmeceuticals (기능성화장품을 위한 유효성분의 경피 전달 시스템)

  • Cho, Wan-Goo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.37 no.2
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    • pp.97-119
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    • 2011
  • World consumers are now focusing on their health, well-being and appearance more than ever before. This trend is creating heightened demand for products formulated as cosmeceuticals with active ingredients. A significant number of innovative formulations are now being used in cosmetics with real consumer-perceivable benefits and optimized sensory attributes, resulting in an economic uplift of cosmetic industry. To obtain skin care formulations with real consumer-perceivable benefits through dermal delivery of active ingredients, formulators are resorting to technology that until recently was used in pharmaceutical products. These various delivery systems are now being used in cosmecuetical formulations. Novel delivery systems reviewed here possess enormous potential as next-generation smarter carrier systems.

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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New Formulation of Vitamin A Transdermal Therapeutic System

  • Han, Jin-Woo;Lee, Dong;Lee, Kee-Myoung;Park, Eun-Seok;Chi, Sang-Cheol
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.409.2-409.2
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    • 2002
  • Retinol is widely used for skin care. the improvement of the appearance of aging. photo-damaged or oxidatively stressed skin. and especially for the improvement of the appearance of wrinkled skin. Retinol. however. is extremely sensitive to atmospheric oxygen. and easily decomposed by exposure to air. Retinol is commonly formulated as the ointments or creams for cosmetic preparations. (omitted)

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Formulation Design and Evaluation of Ketorolac Tromethamine Hydrogel for Transdermal Delivery System (경피흡수를 위한 케토롤락 하이드로겔의 제제설계 및 평가)

  • Cho, In-Sook;Lee, Gye-Won;Lee, Jong-Hwa;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.33 no.1
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    • pp.21-28
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    • 2003
  • Ketorolac tromethamine(KT) is a nonsteroidal agent with potent analgesic and moderate anti-inflammatory activity. The lipid-water partition coefficient of KT was evaluated and KT gel was formulated as a gel containing different pH, different concentrations of polymer (poloxamer 407, carbopol 941), propylene glycol, ethanol and various enhancers. The resulting KT gels were evaluated with respect to their viscosity, in vitro drug permeation rate through hairless mouse skin and stability. In n-octanol and chloroform, the lipid-water partition coefficient of KT was the highest at pH 4 phosphate buffer. The apparent viscosity of KT gel increased with an increase in gel pH, polymer and enhancer concentration. But the apparent viscosity of KT gel decreased with an increase in ethanol concentration. The permeation rate of KT through hairless mouse skin from gels different pH was maximum at pH 4 which is close to KT $pK_{a}$ 3.54. The permeation rate decreased with an increase in polymer, propylene glycol concentration. But the permeation rate increased with an increase in ethanol. The increase of drug concentration from 1 to 3% induced linear increase in permeation rate. The best enhancer was the combination of $Labrasol^{\circledR},\;Transcutol^{\circledR}$, oleic acid and l-menthol. In the accelerated stability test(25, 40 and $50{\circ}C$), pH 5 gel was most stable and pH 4 gel was most unstable for 90 days.

Skin Permeability of piroxicam Gel by Phonophoretic Transdermal Drug Delivery (음파영동 경피약물수송에 의한 Piroxicam Gel의 경피투과)

  • Choi Suk-Joo;Oh Myung-Hwa;Kim Tae-Youl
    • The Journal of Korean Physical Therapy
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    • v.14 no.4
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    • pp.147-162
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    • 2002
  • Transdermal permeation enhancer has been used to increased skin absorption. External control of drug release and skin absorption can also be achieved by iontophoresis or phonophoresis. However, because several problems with iontophoresis are that it has a risk to skin damage because of the change of pH and the increase of current density in applying it and that it can be applied only in the form of water solution, This study is to enhance drug permeation via skin following application of ultrasound. For this goal, in gel containing piroxicam, the degree of skin permeation in vitro and anti-inflammatory effect in in vivo were investigated. Permeation study using hairless mouse skin was performed at 37 $^{\circ}C$ using buffer saline as the receptor solution. The amount of piroxicam were quantified using a HPLC system consisting of solvent delivery system. Following adoption of ultrasound 1 MHZ, it showed relatively high permeation rate where it was compared with non treated by ultrasound. The influence of duty cycle having an effect on skin permeation rate was slight higher in the case of using pulsed mode. Skin permeation increase attended by intensity of ultrasound, the permeation of trice was accelerated at 2.0 W/$cm^{2}$ than 1.0 W/$cm^{2}$. The skin permeation of piroxicam was substantially influenced by ultrasound. Anti-inflammatory effects were determined using carrageenan-induced paw swelling method in SD rat. Paw swelling tests showed that pulsed phonophoresis group was more effective than control group and only gel application group. The conclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory effect in vivo.

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The Effect of Fatty Acids, Fatty Alcohols and Propylene Glycol on the Penetration of Clenbuterol through Hairless Mouse Skin (지방산, 지방 알코올 및 프로필렌글리콜이 클렌부테롤의 경피투과에 미치는 영향)

  • Lee, Yeong-Dae;Quan, Qi-Zhe;Jung, Si-Young;Rhee, Jong-Dal;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.29 no.4
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    • pp.329-335
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    • 1999
  • Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic bronchitis and pulmonary emphysema. For the purpose of developing a transdermal preparation for clenbuterol, we attempted to select an optimal solvent system and permeation enhancer among fatty acids and fatty alcohols which are known to accelerate the penetration of various drugs in permeation experiments using hairless mouse skin and Franz diffusion cell. Apparent partition coefficient of clenbuterol was increased as pH of buffer solution was increased and solubility of clenbuterol was increased as the percent of propylene glycol(PG) in buffer solution(pH 10) was increased. Permeability of clenbuterol from different buffer(pH 10)/PG solvent mixtures was decreased as the percent of PG in pH 10 buffer solution was increased and among the various enhancers studied, lauryl alcohol was found to be the most effective enhancer, increasing the permeability of clenbuterol approximately 76-fold compared with control. Lauryl alcohol$(0{\sim}2%)$ enhanced the permeability of clenbuterol concentration-dependently. In this study, the optimal solvent system for the penetration of clenbuterol was found to be 50/50 buffer(pH 10)/PG solvent mixture containing 2% lauryl alcohol.

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Subjective Skin Improvement and Safety of the Spicules-containing Cosmetics (스피큘을 함유한 화장품의 피부안전성 및 주관적 피부개선감 연구)

  • Han, Do-Sook;Kim, Gi-Sook
    • Journal of Convergence for Information Technology
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    • v.11 no.8
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    • pp.212-223
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    • 2021
  • This study has purposes : evaluating how safe the skin is when applied with the Spicules-containing cosmetic, and whether Diamond-spicules is permeated into the skin and showed the efficacy of the active ingredients well. For these aims, women in their 30s and 60s were surveyed for skin irritation and changes after applying cosmetics to their skin for four weeks. As a result, Spicules-containing cosmetics were safer on the skin than general functional cosmetics, and in particular, in the case of cosmetics containing Diamond-spicules, statistically significant results (p<.001) were obtained in improvement of anti-wrinkle, firmness, moisturizing, whitening, alleviation of inflammation, and sensitivity. Thus, It has been proved Diamond-spicules containing functional active ingredients, not only as transdermal delivery system, but also can be used as multifunctional cosmetic material.