• Title/Summary/Keyword: Skin permeation rate

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Preparation of Composite Membranes of Dense PAA-Poly(BMA-co-MMA) IPN Supported on Porous and Crosslinked Poly(BMA-co-MMA) Sublayer and Their Pervaporation Characteristics

  • Kim, Sung-Chul;Lim, Byung-Yun
    • Macromolecular Research
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    • v.11 no.3
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    • pp.163-171
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    • 2003
  • For the pervaporation of water-ethanol mixtures, new composite membranes having poly(acrylic acid)-poly (butyl methacrylate-co-methyl methacrylate) interpenetrati ng polymer network [PAA-P(BMA-co-MMA) IPN] skin layer supported on porous and crosslinked poly(BMA-co-MMA) were prepared. The morphology of the sub-layer of the composite membrane prepared in the presence of 60 wt% solvent showed cellular structure, on the other hand that of sublayer prepared in the presence of 70 wt% solvent presented very porous interconnected pore structure with macrovoids. Permeation rates of the composite membranes were largely influenced by the morphology of the sublayer. Separation factors increased with the increase of the degree of crosslinking of the PAA network. It was found that permeation rates could be increased by introducing anionic charges on carboxyl groups of the PAA. The permeation rate changes of the PAA-P(BMA-co-MMA) IPN composite membranes according to the feed compositions showed quite similar pattern with the swelling behavior in water-ethanol mixtures.

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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Transdermal Delivery of Bufexamac using Microneedle System (마이크로니들시스템을 이용한 부펙사막의 경피전달)

  • Mo, Jong Hyun;Kim, Yun Tae;Park, Jung Soo;Lee, Jun Hee;Lee, Tae-Wan;Khang, Gilson;Rhee, John Moon;Lee, Han-Koo;Lee, Hai Bang
    • Korean Chemical Engineering Research
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    • v.46 no.2
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    • pp.211-216
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    • 2008
  • Bufexamac which was used for treatment of atopic dermatitis is the drug which was made as the ointment. However, penetration rate of bufexamac was very low for the barrier effect of stratum corneum. Microneedle was used to increase transdermal delivery rate of the bufexamac. We tried to conjugate bufexamac and FITC for the detection of penetration rate of bufexamac. FITC-bufexamac was mixed in hydrogel for the treatment skin surface. Fluorescent spectrophotometer was used to analysis the concentration of FITC-bufexamac. Microscope using fluorescent filter was used to capture the image about location of FITC-bufexamac in the skin. We confirmed that permeation rate of bufexamac was increased with the treatment by microneedle and was increased by the increasing number treatment of microneedle.

In Vitro Percutaneous Absorption of Tenoxicam from Pressure-sensitive Adhesive Matrices across the Hairless Mouse Skin

  • Gwak, Hye-Sun;Chun, In-Koo
    • Archives of Pharmacal Research
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    • v.24 no.6
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    • pp.578-583
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    • 2001
  • To investigate the feasibility of developing a new tenoxicam plaster, the effects of vehicles and penetration enhancers on the in vitro permeation of tenoxicam from a pressure-sensititre adhesive (PSA) matrices across the dorsal hairless mouse skin were studied. Vehicles employed in this study were propylene glycol (PC)-oleyl alcohol (OAI), PG-oleic acid (OA), and diethylene glycol monoethyl ether (DCMI)-propylene glycol monolaurate (PCML) cosolvents with/without fatty acids. In this studys amines such as triethanolamine (TEA) and tromethamine (TM) were additionally used as a solubilized. Among PSAs used, $Duro-Tak^{\circledR}$87-2510 showed much higher release rate than either $Duro-Tak^{\circledR}$ 87-2100 or $Duro-Tak^{\circledR}$87-2196. The relatively high flux rate was obtained with the formulation of DCMI-PCML (40:60, v/v) with 3% OA and 5% TM, and the flux increased as a function of the dose;the initial flux up to 12 h was $4.98{\pm}1.38{\;}{\mu\textrm{g}}/{\textrm{cm}^2}/h$ at the tenoxicam dose of $50{\;} mg/70{\;}{\textrm{cm}^2}$. This flux was much higher than that of a commercial piroxicam patch ($Trast^{\circledR}$) ($1.24{\pm}0.73{\;}{\mu\textrm{g}}/$\textrm{cm}^2/hr$) with almost only one-third that of the commercial patch. Therefore, these observations indicated that these composition of tenoxicam plaster may be practically applicable.

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In Vitro and In Vivo Studies of Topical Delivery System of Gentisic Acid in Hairless Mice

  • Bian, Shengjie;Zheng, Junmin;Kim, Jung-Sun;Choi, Myeong-Jun;Chung, Ho-Kwon;Lee, Chi-Ho;Kim, Dae-Duk
    • Journal of Pharmaceutical Investigation
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    • v.32 no.3
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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.

Study on Optimization and Skin Permeation of PIT Nanoemulsion Containing α-Bisabolol (α-Bisabolol을 함유한 PIT Nanoemulsion의 최적화 및 피부흡수연구)

  • Kim, HuiJu;Yoon, Kyung-Sup
    • Journal of the Korean Applied Science and Technology
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    • v.37 no.6
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    • pp.1738-1751
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    • 2020
  • The skin is divided into three parts: the epidermis, the dermis, and the subcutaneous fat, and the stratum corneum, which is located at the top of the epidermis, acts as a barrier that prevents drug delivery. Nanoemulsions are known to be effective in transdermal delivery of drugs through intercellular lipids because of their unique small particle size. In this study, phase inversion temperature (PIT) nanoemulsion containing α-bisabolol was optimized using response surface methodology (RSM) for effective skin absorption of α-bisabolol. As a preliminary experiment, the 25-2 fractional factorial design method and the 23 full factorial design method were performed. Box-Behnken design was performed based on the results of the factorial design method. The content of surfactant (6.3~12.6%), co-surfactant (5.2~7.8%) and α-bisabolol (0.5~5.0%) were used as factors, and the dependent variable was the particle size of the nanoemulsion. PIT nanoemulsion optimization was performed according to the RSM results, and as a result, the optimal nanoemulsion formulation conditions were predicted to be 10.4% surfactant content, 6.3% co-surfactant content, and 5.0% α-bisabolol content. As a result of the skin absorption test, the final skin absorption rate of the PIT nanoemulsion was 35.11±1.01%, and the final skin absorption rate of the general emulsion as a control was 28.25±1.69%, confirming that the skin absorption rate of the PIT nanoemulsion was better.

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.

Characteristics of Percutaneous Absorption of Glycol ethers (Glycol ethers에 대한 피부 투과 특성)

  • Lee, Han-Seob;Choi, Sung-Boo;Kim, Nac-Joo;Keun, Jang-Hyoun;Hwang, Hyun-Suk;Baek, Jung-Hun;Choi, Jin-Ho;Lee, Ho-Joon
    • Journal of the Korean Applied Science and Technology
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    • v.30 no.1
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    • pp.116-126
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    • 2013
  • Glycol ethers are a group of solvents based on alkyl ethers of ethylene glycol commonly used in paints. These solvents typically have a higher boiling point, together with the favorable solvent properties of lower-molecular weight ethers and alcohols. The word "Glycol ethers" was registered as a United States trademark by Union Carbide Corp. Typically, glycol ethers are found in pharmaceuticals, sunscreens, cosmetics, inks, dyes and water based paints. On the other hand, glycol ethers are used in degreasers, cleaners, aerosol paints and adhesives. Most glycol ethers are relatively water soluble, biodegradable and only a few are considered toxic. Therefore, they are unlikely to pose an adverse risk to the environment. Recent study suggests that occupational exposure to glycol ethers is related to low motile sperm count in men, but the finding has been disputed by others. In this study, skin permeation of 3 types glycol ethers were studied in vitro using matrix such as solvent and detergent. The absorption of glycol ethers[methyl glycol ethers(MC), ethyl glycol ethers(EC) and butyl glycol ethers(BC)] has been measured in vitro through rat skin. Epidermal membranes were set up in Franz diffusion cells and their permeability to PBS measured to establish the integrity of the skin before the glycol ethers were applied to the epidermal surface. Absorption rates for each glycol ethers were determined and permeability assessment made to quantify any irreversible alterations in barrier function due to contact with the esters. Types of glycol ethers in vitro experimental results on MC> EC> BC quickly appeared in the following order: skin permeation was beneficial to the skin permeation small molecular weight, the difference in chemical structure, such as hydrophilic, because with the partition coefficient and solubility mechanisms and passive diffusion to increase the speed at which transmission is considered.

Transdermal Penetration of Synthetic Peptides and Their Penetration Enhancement Caused by Some Terpene Compounds

  • Ham, Seung-Wook;Kang, Myung-Joo;Park, Young-Mi;Oh, Il-Young;Kim, Bo-Gyun;Im, Tae-Jong;Kim, Sung-Hee;Choi, Young-Wook;Lee, Jae-Hwi
    • Bulletin of the Korean Chemical Society
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    • v.28 no.9
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    • pp.1535-1538
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    • 2007
  • The work presented in this paper represents a study of the rate and extent of transdermal penetration of three synthetic hexapeptides consisting only of glycine (Gly) and phenylalanine (Phe) as the constituent amino acids and they include Phe-Gly-Gly-Gly-Gly-Gly (Pep-1), Phe-Phe-Gly-Gly-Gly-Gly (Pep-2), and Phe-Phe-Phe- Gly-Gly-Gly (Pep-3). The present study demonstrated the extent to which the peptides having a high metabolic stability were transdermally transported from the various vehicles. The results of this study appear to indicate that minor differences in the lipophilicity of the synthetic hexapeptides have a slight influence on the rate and extent of transport. In the presence of terpene permeation enhancers, together with ethanol (i.e., menthone/ EtOH, carveol/EtOH or cineole/EtOH), the peptides were more rapidly penetrated through the skin and among the terpenes tested, cineole was the most effective for all three peptides. The maximum enhancement ratio of approximately 2 was achieved by cineole in 50% ethanol solution.

Skin permeability of the biosynthetic galactosylated 2-phenoxyethanol (생합성된 galactosylated 2-phenoxyethanol의 피부 투과도)

  • Su-Hong Kim;Sun-Beom Kwon;Jun-Sub Kim;Gi-Seong Moon;Kyung-hwan Jung;Hyang-Yeol Lee
    • Journal of the Korean Applied Science and Technology
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    • v.41 no.1
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    • pp.1-8
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    • 2024
  • The safety of cosmetic ingredients is considered paramount. In order to enhance safety, a novel preservative, PE-gal, was bio-synthesized by utilizing the Escherichia coli enzyme 𝛽-galactosidase on the conventional preservative 2-phenoxyethanold (PE). The skin absorption of the bio-synthesized product, PE-gal, intended for use in cosmetics, was evaluated for permeability using the Franz Diffusion Cell Assay system, comparing it with the conventinal preservative PE. When using samples of the same mass concentration, the Flux and Kp values of PE increased over time, indicating a gradual increase in permeability. However, PE-gal did not exhibit sufficient permeability to measure. This suggests that the skin permeability of PE is higher than that of the PE-gal saccharide. According to Marzulli et al., when confirming the degree of permeation using Kp values, the permeation rate of PE was measured as "slow" at a concentration of 1mg/mL. Thus, the transdermal permeability of the divedened form of PE-gal was significantly lower compared to PE.