• Title/Summary/Keyword: Skin permeation

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Hyaluronic Acid Enhances the Dermal Delivery of Anti-wrinkle Peptide via Increase of Stratum Corneum Fluidity (히알루론산의 각질 유동성 향상을 통한 주름 개선 펩타이드 피부 흡수 촉진)

  • Kim, Yun-Sun;Kim, Daehyun;Kim, Yumi;Park, Sun-Gyoo;Lee, Cheon-Koo;Kang, Nae-Gyu
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.44 no.4
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    • pp.447-453
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    • 2018
  • Acetyl hexapeptide 8 (AH8) is a synthetic peptide for anti-wrinkle cosmetics ingredient. It was developed as a mimetic of botox, patternd after N -terminal end of the protein synatosomal-associated protein 25 (SNAP25), a substrate of botulinum toxin. While AH8 has good efficacy and safety profiles, the permeation through the skin is poor. Therefore, we tried to enhance the transdermal delivery of AH8 by using of hyaluonic acid (HA), a linear polysaccharide of N-acetyl glucosamine and glucuronic acid. To investigate the effect of HA on AH8 penetration, we analyzed paraffin sections of $Micropig^{(R)}$ skin. Fluorescence labeled AH8 was applied to micropig skin with or without HA. The absorption of AH8 was limited to the stratum corneum (SC) without HA. On the other hand, AH8 penetrated to the dermis with HA. Especially, low molecular weight HA (5 kDa) was most efficient compared to 500 kDa HA and 2000 kDa HA. Experiments using fourier-transform infrared (FTIR) spectroscopy revealed that lower molecular weight HA had a tendency to increase the fluidity of the SC lipids more, which means enhancing the skin penetration. Therefore, HA could be expected to enhance the anti-wrinkle effect of AH8.

The bioavailability of red ginseng extract fermented by Phellinus linteus

  • Ryu, Jae Sik;Lee, Hyun Jung;Bae, Song Hwan;Kim, Sun Young;Park, Yooheon;Suh, Hyung Joo;Jeong, Yoon Hwa
    • Journal of Ginseng Research
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    • v.37 no.1
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    • pp.108-116
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    • 2013
  • For the improvement of ginsenoside bioavailability, the ginsenosides of fermented red ginseng by Phellinus linteus (FRG) were examined with respect to bioavailability and physiological activity. The polyphenol content of FRG ($19.14{\pm}0.50$ mg/g) was significantly higher (p<0.05) compared with that of non-fermented red ginseng (NFRG, $11.31{\pm}1.15$ mg/g). The antioxidant activities in FRG, such as 2,2'-diphenyl-1-picrylhydrazyl, 2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid, and ferric reducing antioxidant power, were significantly higher (p<0.05) than those in NFRG. The HPLC analysis results showed that the FRG had a high level of ginsenoside metabolites. The total ginsenoside contents in NFRG and FRG were $41.65{\pm}1.53$ mg/g and $50.12{\pm}1.43$ mg/g, respectively. However, FRG had a significantly higher content ($33.90{\pm}0.97$ mg/g) of ginsenoside metabolites (Rg3, Rg5, Rk1, compound K, Rh1, F2, and Rg2) compared with NFRG ($14.75{\pm}0.46$ mg/g). The skin permeability of FRG was higher than that of NFRG using Franz diffusion cell models. In particular, after 3 h, the skin permeability of FRG was significantly higher (p<0.05) than that of NFRG. Using a rat everted intestinal sac model, FRG showed a high transport level compared with NFRG after 1 h. FRG had dramatically improved bioavailability compared with NFRG as indicated by skin permeation and intestinal permeability. The significantly greater bioavailability of FRG may have been due to the transformation of its ginsenosides by fermentation to more easily absorbable forms (ginsenoside metabolites).

Bioavailability of Fermented Korean Red Ginseng

  • Lee, Hyun-Jung;Jung, Eun-Young;Lee, Hyun-Sun;Kim, Bong-Gwan;Kim, Jeong-Hoon;Yoon, Taek-Joon;Oh, Sung-Hoon;Suh, Hyung-Joo
    • Preventive Nutrition and Food Science
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    • v.14 no.3
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    • pp.201-207
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    • 2009
  • In an effort to improve ginsenoside bioavailability, the ginsenosides of fermented red ginseng were examined with respect to bioavailability and physiological activity. The results showed that the fermented red ginseng (FRG) had a high level of ginsenoside metabolites. The total ginsenoside contents in non-fermented red ginseng (NFRG) and FRG were 35715.2 ${\mu}g$/mL and 34822.9 ${\mu}g$/mL, respectively. However, RFG had a higher content (14914.3 ${\mu}g$/mL) of ginsenoside metabolites (Rg3, Rg5, Rk1, CK, Rh1, F2, and Rg2) compared to NFRG (5697.9 ${\mu}g$/mL). The skin permeability of RFG was higher than that of NFRG using Franz diffusion cells. Particularly, after 5 hr, the skin permeability of RFG was significantly (p<0.05) higher than that of NFRG. Using everted instestinal sacs of rats, RFG showed a high transport level (10.3 mg of polyphenols/g sac) compared to NFRG (6.67 of mg of polyphenols/g sac) after 1 hr. After oral administration of NFRG and FRG to rats, serum concentrations were determined by HPLC. Peak concentrations of Rk1, Rh1, Rc, and Rg5 were approximately 1.64, 2.35, 1.13, and 1.25-fold higher, respectively, for FRG than for NFRG. Furthermore, Rk1, Rh1, and Rg5 increased more rapidly in the blood by the oral administration of FRG versus NFRG. FRG had dramatically improved bioavailability compared to NFRG as indicated by skin permeation, intestinal permeability, and ginsenoside levels in the blood. The significantly greater bioavailability of FRG may have been due to the transformation of its ginsenosides by fermentation to more easily absorbable forms (ginsenoside metabolites).

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.

Transdermal Drug Delivery System (경피 흡수와 연구동향)

  • Jin, Hwa Eun;Kim, Jung Hyun;Paik, Il Young
    • Applied Chemistry for Engineering
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    • v.16 no.1
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    • pp.15-20
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    • 2005
  • Many scientists have been interested in drug delivery system (DDS) which improves medical treatment for curing a disease. Transdermal drug delivery (TDD) that is one of the DDS offers several advantages over the traditional methods. For this reason, the study of TDD has been investigated in various field. In this paper, principle of transdermal delivery and penetration enhancers into the skin including in vitro and in vivo data have been studied.

Effect of structure of PVDF membranes on the performance of membrane distillation

  • Chang, Hsu-Hsien;Tsai, Chih-Hao;Wei, Hao-Cheng;Cheng, Liao-Ping
    • Membrane and Water Treatment
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    • v.5 no.1
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    • pp.41-56
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    • 2014
  • A series of microporous PVDF membranes were prepared by isothermal immersionprecipitation of PVDF/TEP casting dopes in both soft and harsh coagulation baths. Morphologies of the membranes' top surfaces were found to depend strongly on the bath strength, which could be controlled by the TEP content in the bath. By changing the bath gradually from pure water to 70% TEP, the top surface evolved from a dense skin-like (asymmetric) to a totally open porous morphology (symmetric). The latter structure could similarly be obtained by precipitation of the same dope in an alcoholic bath, e.g., 1-butanol. Membrane distillation processes to desalt sodium chloride aqueous solutions were conducted using various prepared membranes and two commercial microporous membranes, PTFE (Toyo, Japan, code: J020A330R) and PVDF (GE, USA, code: YMJWSP3001). The permeation fluxes were compared and correlated with the morphologies of the tested membranes.

The flow of $CO_{2}$ and $N_{2}$ gases through Asymmetric polytherimide Membrane

  • Park, You-In;Lee, Kew-Ho
    • Proceedings of the Membrane Society of Korea Conference
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    • 1995.09a
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    • pp.73-85
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    • 1995
  • The asymmetric hollow fiber membranes were prepared by the wet spining of polyetherimide dope solution and the effect of hollow fiber structures on the permeation characteristics of carbon dioxide and nitrogen gases through these membrane were investigated. As the concentration of the $\gamma$-butyrolactone (GBL) in dope solution, acting as a swelling agent was increased, the structure of hollow fiber was changed from the finger to sponge type. The permeabilities of gases (CO$_{2}$, N$_{2}$) through these membrane were measured over the wide range of pressure under different temperature. The effect of water vapor on the permeabilities of gases was also investigated. The measured permeabilities showed the different characteristics depending on the structure of membranes. It was found that the flow through the pores were dominant over the polymers matrix. Blocking effect by water vapor in the pores of skin layer greatly improved the ideal separation factor of carbon dioxide/nitrogen.

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Antihistamine Effects of Triprolidine from the Transdermal Administration of the TPX Matrix in Rats

  • Shin Sang-Chul;Choi Jun-Shik
    • Archives of Pharmacal Research
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    • v.28 no.1
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    • pp.111-114
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    • 2005
  • The antihistamine effects of the triprolidine were studied in rats to determine the feasibility of their enhanced transdermal delivery from the poly (4-methyl-1-pentene) (TPX) matrix system containing penetration enhancer and plasticizer. The antihistamine effects were determined by the Evans blue dye procedure by comparing the changes in vascular permeability increase following the transdermal administration. The vascular permeability increase was significantly reduced by transdermal administration of the triprolidine-TPX system containing triethyl citrate (TEC) and polyoxyethylene-2-oleyl ether (POE). Both the plasticizer and penetration enhancer played an important role in the skin permeation of triprolidine and increased the antihistamine effects. These results showed that the triprolidine-TPX matrix system containing plasticizer and penetration enhancer could be a transdermal delivery system providing the increased antihistamine effects.

Preparation and Permeation Characteristics of Finely Porous Ultrafiltration Membranes by Phase Inversion Method (상전환법에 의한 미세다공성 한외여과막의 제조 및 투과특성)

  • 홍영기;배기서
    • Textile Coloration and Finishing
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    • v.15 no.2
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    • pp.68-75
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    • 2003
  • In this work, ultrafiltration(UF) membranes were prepared using polyethersulfone(PES). The polymer was dissolved in various solvent, such as N, N-dimethyl formamide(DMF), N,-dimethyl acetamide (DMAc), N,N-dimethyl sulfoxide(DMSO) and N-methyl-2- pynolidone(NMP). Each polymer solution was casted on the glass plate, and immersed into non-solvent bath. In this way finely porous UF membranes were prepared by phase inversion method. The cross sectional structure of PES membrane was asymmetric which was consist of sponge-like sublayer, finger-like toplayer, and active skin layer. From the solute rejection experiments, the molecular weight cut off of the prepared membrane in various solvent was evaluated 10,000 for DMF, 30,000 for DMAc, 50,000 for DMSO, and 10,000 for NMP respectively.

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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