• Title/Summary/Keyword: Transdermal penetration

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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.

Enhanced Transdermal Delivery of Furosemide from the EVA Matrix through the Rat Skin

  • Chang, Ik-Hyeon;Cho, Hwa-Young;Noh, Jin-Hyung;Park, Jung-Chan;Park, Yong-Sun;Kim, Seong-Jin;Shin, Sang-Chul
    • Journal of Pharmaceutical Investigation
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    • v.39 no.1
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    • pp.19-21
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    • 2009
  • This study was performed to examine the possibility of increasing the level of furosemide permeation from the ethylene-vinyl acetate (EVA) matrix through the skin by incorporating various enhancers in the EVA matrix. The effects of the enhancers on the level of furosemide permeation through the skin were evaluated using Franz diffusion cells with intact excised rat skins. The enhancers examined were the fatty acids (saturated, unsaturated), the pyrrolidones, the propylene glycol derivatives, the glycerides and the non-ionic surfactants. Among the enhancers used, polyoxyethylene-2-oleyl ether (a non-ionic surfactant) showed the best enhancement. The polyoxyethylene 2-oleyl ether as a permeation enhancer could be used for development of furosemide-EVA transdermal matrix system.

Transdermal Delivery of Porcine Placenta Extracts using Linolenic Acid-based Emulsion Formulations

  • Kim, Dong-Chan;Noh, Sang-Myoung;Park, Ki-Tae;Kim, Young-Bong;Baek, Kwang-Hyun;Oh, Yu-Kyoung
    • Journal of Pharmaceutical Investigation
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    • v.37 no.5
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    • pp.281-286
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    • 2007
  • For transdermal delivery of porcine placenta extract (PPE), various emulsion formulations were prepared and evaluated. Polysorbate surfactants were used as emulsifiers and various C-18 unsaturated fatty acids as enhancers. The skin permeation of PPE was tested using a cellulose nitrate membrane-loaded Franz cell apparatus. Among emulsifiers, Tween 20 provided higher penetration effect than did Tween 80. Meanwhile, of various fatty acids, linolenic acid (18:3) revealed the highest skin permeation of PPE than the other C-18 unsaturated fatty acids. Stability of PPE emulsions was determined by cycles of freezing and thawing processes. The stability of emulsions depended on the percentage of Tween 20. Minimum 20% of Tween 20 was required to stabilize emulsions at room temperature for several days. Taken together, our results suggest that Tween 20 and linolenic acids might be key components to formulate PPE emulsion to provide the desirable skin permeability and stability.

Use of the Stratum Corneum Reservoir for the Prediction of Skin Penetration

  • Cholee, Ae-Ri;Tojo, Kakuji
    • Journal of Pharmaceutical Investigation
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    • v.23 no.3
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    • pp.1-8
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    • 1993
  • A simple and quick method based on the transient diffusion theory for predicting the steady state rate of penetration of a drug after transdermal drug administration was proposed. The amount of drug entering the stratum corneum was determined by 20 strippings with an adhesive tape. From the profile of the amount of drug as a function of the number of strippings, the quantity of drug on the surface of stratum corneum was extrapolated. Based on the amounts of drug entering the stratum corneum during two time intervals $(t_1\;and\;t_2)$ within 1 hour after the application, the diffusion and partition coefficient were determined. Once the diffusion coefficient of the drug in the stratum corneum and the partition coefficient (stratum corneum/vehicle) were determined from the present approach, the steady-state flux of penetration across the stratum corneum was calculated. The steady-state rates of penetration of ascorbic acid and estradiol across hairless mouse skin were evaluated from this approach and compared with those obtained from ill vitro penetration experiment using excised hairless mouse skin. The data confirmed that the proposed method can predict the steady-state rate of penetration of these drugs across the stratum corneum.

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The Effects of Enhancers on Transdermal Absorption of Ketoprofen Packs (케토프로펜 팩제제에서 경피흡수에 미치는 투과촉진제의 영향)

  • Cho, Su-Jin;You, Do-Ra;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.31 no.2
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    • pp.107-112
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    • 2001
  • In order to reduce the systemic side effects and gastrointestinal irritation after its oral adminitration, ketoprofen was formulated as water-soluble packs. The effects of fatty acids and fatty alcohols on the penetration of ketoprofen through excised rat skins were evaluated. The role of stratum corneum as a protective barrier was also investigated. Fatty acids and fatty alcohols were generally effective in promoting ketoprofen penetration. The flux of ketoprofen through rat skin was maximized when oleic acid or lauryl alcohol was used as an enhancer. As the concentration of fatty acids and fatty alcohols varied from 0% to 10%, the amounts of ketoprofen penetrated were in direct proportion to that of fatty acids but those had no relationship with that of fatty alcohols. The penetration of ketoprofen through stripped skin was enhanced compared to normal skin irrespective of enhancer type, which indicated that the action site of enhancers would be stratum corneum.

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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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Improving the Skin Penetration of Cosmetics Containing Omega 3 Fatty Acids

  • KIM, Han-Sook;HAN, Sien-Ho
    • Journal of Wellbeing Management and Applied Psychology
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    • v.4 no.4
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    • pp.15-25
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    • 2021
  • Purpose: The purpose of this study is to form a new cosmetic market through the development of a composition with high skin permeability after adding omega 3 to Aloe Vera soothing gel products. Research design, data and methodology: In this study, omega-3 fatty acids were added to cosmetic products in the form of soothing gels. By applying nanoparticle technology to rapidly increase the penetration of raw materials into the skin, characteristics related to skin moisture and regeneration were determined. Omega-3 was used as a raw cosmetic material. Then 5% and 15% nanoparticle aqueous products containing omega-3 were prepared. The developed water hydrate was subjected to skin permeability test using artificial skin. Results: 53 hours of artificial transdermal penetration of the developed composition, the ethanol-based omega-3 containing nanoparticle solubilized raw material was about three times higher penetration than the ethanol-based omega-3 containing nanoparticle solubilized raw material. Conclusions: The raw material product (SR-1901) containing 5% of omega-3 nanoparticle water hydrate has skin regeneration ability and pain reduction effect. It can be expected that the skin cosmetics market will be reorganized into a new distribution structure and opportunity through omega-3 supplemented soothing gel cosmetics with improved efficacy than existing cosmetics.

Transdermal Delivery of FITC-Ovalbumin with Microneedle System (마이크로 피부침을 이용한 FITC-OVA의 경피흡수)

  • Jang, Woo-Young;Lee, Chang-Rae;Seo, Seong-Mi;Lee, Bong;Kim, Moon-Suk;Khang, Gil-Son;Lee, Han-Gu;Lee, Hai-Bang
    • Journal of Pharmaceutical Investigation
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    • v.35 no.6
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    • pp.403-409
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    • 2005
  • For transdermal delivery of large molecular drugs such as vaccine and protein drugs, novel microneedle treatment device with roll was designed. The roll dimension is 1.43 cm diameter and 2.8 cm perimeter. Total number of microneedle on the roll is 3,360 with $230\;{\mu}m$ height and $740\;{\mu}m$ distance. The pore with $150\;{\mu}m$ depth and $35\;{\mu}m$ diameter on the skin was made by the designed microneedle device. This system could be achieved without pain. The permeation rates of FITC labelled ovalbumin (FITC-OVA, molecular weight: 45,000 g/mol) as a model protein were determined by modified Franz diffusion cells using skins of hairless mice or SD rats which were treated by using microneedle device two or four times. The average penetration fluxes of model protein increased from 674 to $872\;{\mu}g/cm^{2}{\cdot}hr$ as the number of treatment to make pore increased from two to four times. In conclusion, we confirmed the possibility of using the designed microneedle treatment device for transdermal delivery of the large molecular drugs.

Percutaneous absorption Characteristics of Anti hyperlipidemia Gel Ointment using Fibric acid (Fibric acid를 이용한 항고지혈증 겔 연고의 경피 흡수 특성)

  • Jung, Duck-Chae;Hwang, Sung-Kwy;Oh, Se-Young
    • Journal of the Korean Applied Science and Technology
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    • v.27 no.4
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    • pp.407-414
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    • 2010
  • New biological treatments were being developed at a record place, but their potential could be compromised by a significant obstacle: the delivery of these drugs into a body. Pharmaceutical delivery is now nearly as important as product. New systems are being developed, and Drug Delivery Markets Series cover these new systems. Transdermal Delivery System(TDS) is often used as a method of drug dosage into the epidermic skin. An approach used to delivery drugs through the skin for therapeutic use as an alternative to oral, intravascular, subcutaneous and transmucosal routes. Various transdermal drug delivery technologies are described including the use of suitable formulations, carriers and penetration enhancers. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other methods of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharides, such as karaya gum and glucomannan, were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, drug contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in fibric acid(ciprofibrate) such as lipophilic drug in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. 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. Especially, this result suggests a possible use of polysaccharide gel ointment matrix as a transdermal delivery system of anti-hyperlipoproteinemic agent.

The Effect of Methylsulfonylmethane on Hair Growth Promotion of Magnesium Ascorbyl Phosphate for the Treatment of Alopecia

  • Shanmugam, Srinivasan;Baskaran, Rengarajan;Nagayya-Sriraman, Santhoshkumar;Yong, Chul-Soon;Choi, Han-Gon;Woo, Jong-Soo;Yoo, Bong-Kyu
    • Biomolecules & Therapeutics
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    • v.17 no.3
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    • pp.241-248
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    • 2009
  • The purpose of this study was to evaluate the effect of methylsulfonylmethane (MSM) on hair growth promotion of magnesium ascorbyl phosphate (MAP) for the treatment of alopecia. Aqueous solutions of MAP 7.5% with or without MSM 1%, 5% or 10% were prepared and applied onto the depilated back skin of the male mice once a day for 20 days. The degree of hair growth was evaluated by visual scoring using hair growth quantification scale (0-5, 0 being initial state and 5 being complete hair growth). In vitro transdermal penetration and intradermal retention studies of MAP were performed with Franz diffusion cell using hairless mice skin. Hair growth in the group treated with the aqueous solution containing MAP 7.5% and MSM 10% was comparable to or better than the result in the group treated with minoxidil 5% solution. Hair growth promotion of MAP was dose-dependently increased by the presence of MSM used in combination with MAP 7.5% solution. The in vitro transdermal penetration of the MAP was decreased in proportion to the concentration of MSM. However, intradermal retention of MAP was profoundly and dose-proportionally increased as a function of MSM concentration, reaching 802 ${\mu}g/cm^2$ in the presence of MSM 10% (200-fold increase). The effect of MSM on hair growth promotion of MAP was dose-proportional to the concentration of MSM due to the enhanced intradermal retention of MAP in the presence of MSM. Therefore, topical application of MAP together with MSM appears to be useful for the treatment of alopecia.