• Journal of Pharmaceutical Investigation
• /
• v.37 no.3
• /
• pp.149-158
• /
• 2007

To investigate the permeability of lidocaine, percutaneous absorption studies were performed using excised hairless mouse skin and the penetration of lidocaine via the skin was determined. To increase the skin permeation of lidocine, the effects of $Labrasol^{(R)}$, $Labrafil^{(R)}$, $Labrafac^{(R)}$ and $Transcutol^{(R)}$ were investigated. The skin permeation of lidocaine was increased when $Labrasol^{(R)}$ and $Transcutol^{(R)}$ were used as permeation enhancer. To evaluate the influence of ultrasound, various factors such as application modes (continuous mode and pulsed mode), frequency (1.0 and 3.0 MHz) and intensity (1.0, 1.5 and 2.0 w/$cm^2$) were investigated with lidocaine hydrogel. The pronounced effect of ultrasound on the skin permeation of lidocaine was observed at all ultrasound energy levels. The influence of frequency having an effect on skin permeation rate was higher in the case of using 1 MHz, 2.0 w/$cm^2$ and continuous treatment. As the intensity of ultrasound increased, the permeation of lidocaine was accelerated. The in vivo anesthetic effects were evaluated by two aspects as mechanical threshold and electrical threshold. Six healthy volunteers consented to the randomized, double-blind, and cross-over designed study in each group. In each subject, 3 groups were adapted such as K group (ultrasound with gel base only), L group (lidocaine gel) and B group (ultrasound with lidocaine gel). In conclusion, lidocaine was potent anesthetic which could be block pain threshold effectively. And ultrasound could accelerate the skin penetration of lidocaine. The phonophoretic delivery system could be a good candidate for lidocaine as a local anaesthetic to improve the skin permeation and in vivo anaesthetic effect.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.36 no.2
• /
• pp.115-120
• /
• 2010

The formidable barrier property of the stratum cornemum and the high hydrophilicity of active ingredient make it difficult to permeate through the skin and reach to its site of action. The aim of this study was to investigate the effect of chemical penetration enhancers on the skin permeation of a hydrophilic cosmetic active ingredient, such as arbutin. The enhancing effects of N-methyl-2-pyrrolidone (NMP) on the permeation of a hydrophilic cosmetic active ingredient were evaluated by using Franz diffusion cell. The study indicated that NMP has considerable influence on the skin permeability. NMP was not only the most effective enhancer but also increased the skin permeability of arbutin approximately 1.3~1.5 fold compared with control without penetration enhancer. The lag time did not change with NMP, which suggested no effect of NMP on skin lipid fluidity. This suggest that arbutin co-permeated with NMP. The results indicate NMP is effective enhancer of a hydrophilic cosmetic active ingredient in penetration, with potential applications for drug delivery system.

• Journal of Biomedical Engineering Research
• /
• v.43 no.4
• /
• pp.271-279
• /
• 2022

Functional cosmetics containing various ingredients that improve skin health are currently being developed. In addition, technologies that help increase the absorption rate of such cosmetics have recently gained significant attention. Sonophoresis is a method to increase the transdermal absorption of cosmetics using ultrasound. A skin-mimicking phantom was fabricated using polydimethylsiloxane, Strat-M^TM membrane, and thermochromic pigments. Gel-type cosmetics used in skin mask packs and epidermal-growth-factor-based nano-cosmetics were tested for their absorption rates at ultrasound frequencies of 1, 3, and 10 MHz in the single frequency mode, and 1/3 and 3/10 MHz in the dual frequency mode. The gel-type cosmetics and epidermal-grow-factor-based nano-cosmetics showed the highest absorption rate at 3/10MHz dual frequency. The size of the cosmetic particles decreased by 5-9 %. Furthermore, the temperature rise caused by ultrasound could be visually recognized by the thermochromic pigment in the phantom turning white. We presented a skin-mimicking phantom. The device can be customized according to the size of the ultrasound probe and has the advantage of quantitatively evaluating the transdermal permeability of cosmetics at a low cost. The development of the skin-mimicking phantom will be useful for determining the suitable conditions required to increase the absorption rate of cosmetics using ultrasound.

• The Korean Journal of Physiology
• /
• v.10 no.1
• /
• pp.35-40
• /
• 1976

In an attempt to examine the effect of ginseng on sodium transport across the biological membrane, we have studied effects of ginseng alcohol extract on the short-circuit current(SCC) and the $Na^+-K^+$-activated ATPase activity in isolated frog skin preparations. 1. Ginseng alcohol extract applied to the mucosal surface of the frog skin significantly increased SCC at low concentration($1{\sim}10mg%$) but decreased SCC at higher concentration($50{\sim}250mg%$). 2. Similarly, when the drug was added to the serosal bathing medium, the SCC was stimulated at low doses($5{\sim}25mg%$) and inhibibited at high doses($50{\sim}250mg%$). 3. $Na^+-K^+$-activated ATPase activity of the frog skin epidermal homogenate was significantly inhibited by ginseng alcohol extract, the effect being proportional to the concentration of the drug in the incubation mixture. These results may suggest that a low dose of ginseng alcohol extrat enhances the transepithelial sodium transport probably by increasing the permeability of outer membrane of the transporting cell to sodium ion, whereas a high dose of drug reduces the sodium transport primarly by inhibiting $Na^+-K^+$ ATPase mediated active transport step.

• Journal of Pharmaceutical Investigation
• /
• v.32 no.4
• /
• pp.259-265
• /
• 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.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.30 no.2
• /
• pp.263-278
• /
• 2004

Ursolic acid (UA) and Oleanolic acid (ONA), known as urson, micromerol and malol, are pentacyclic triterpenoid compounds which naturally occur in a large number of vegetarian foods, medicinal herbs, and plants. They may occur in their free acid form or as aglycones for triterpenoid saponins, which are comprised of a triterpenoid aglycone, linked to one or more sugar moieties. Therefore UA and ONA are similar in pharmacological activity. Lately scientific research, which led to the identification of UA and ONA, revealed that several pharmacological effects, such as antitumor, hepato-protective, anti-inflammatory, anticarcinogenic, antimicrobial, and anti-hyperlipidemic could be attributed to UA and ONA. Here, we introduced the effect of UA and ONA on acutely barrier disrupted and normal hairless mouse skin. To evaluate the effects of UA and ONA on epidermal permeability barrier recovery, both flanks of 8-12 week-old hairless mice were topically treated with either 0.01-0.1mg/mL UA or 0.1-1mg/mL ONA after tape stripping, and TEWL (transepidermal water loss) was measured. The recovery rate increased in those UA or ONA treated groups (0.1mg/mL UA and 0.5mg/mL ONA) at 6h more than 20% compared to vehicle treated group (p < 0.05). Here, we introduced the effects of UA and ONA on acute barrier disruption and normal epidermal permeability barrier function. For verifying the effects of UA and ONA on normal epidermal barrier, hydration and TEWL were measured for 1 and 3 weeks after UA and ONA applications (2mg/mL per day). We also investigated the features of epidermis and dermis using electron microscopy (EM) and light microscopy (LM). Both samples increased hydration compared to vehicle group from 1 week without TEWL alteration (p < 0.005). EM examination using RuO4 and OsO4 fixation revealed that secretion and numbers of lamellar bodies and complete formation of lipid bilayers were most prominent (ONA=UA > vehicle). LM finding showed that thickness of stratum corneum (SC) was slightly increased and especially epidermal thickening and flattening was observed (UA > ONA > vehicle). We also observed that UA and ONA stimulate epidermal keratinocyte differentiation via PPAR Protein expression of involucrin, loricrin, and filaggrin increased at least 2 and 3 fold in HaCaT cells treated with either ONA (10${\mu}$M) or UA (10${\mu}$M) for 24 h respectively. This result suggested that the UA and ONA can improve epidermal permeability barrier function and induce the epidermal keratinocyte differentiation via PPAR Using Masson-trichrome and elastic fiber staining, we observed collagen thickening and elastic fiber elongation by UA and ONA treatments. In vitro results of collagen and elastin synthesis and elastase inhibitory activity measurements were also confirmed in vivo findings. These data suggested that the effects of UA and ONA related to not only epidermal permeability barrier functions but also dermal collagen and elastic fiber synthesis. Taken together, UA and ONA can be relevant candidates to improve epidermal and dermal functions and pertinent agents for cosmeseutical applications.

• Textile Coloration and Finishing
• /
• v.35 no.3
• /
• pp.179-187
• /
• 2023

In this study, we developed a microfiber-based flexible pressure sensor with high sensitivity and excellent skin breathability. A nonwoven fabric composed of microfibers was prepared by electrospinning, which resulted in excellent moisture permeability of the sensor (143 g∙m^-2∙h^-1). In particular, high-pressure sensitivity (0.36 kPa^-1) was achieved by introducing submicron structures on the microfiber surface by controlling the ambient humidity during electrospinning. The fabrication technology of the microfiber-based flexible pressure sensors reported in this study is expected to contribute to the commercialization of flexible pressure sensors applicable to long-term wearable health monitoring as well as virtual/augmented reality and electronic skin applications.

• YAKHAK HOEJI
• /
• v.36 no.2
• /
• pp.140-149
• /
• 1992

Anti-allergic action of each water extracts of some crude drugs was investigated in mice and rats. The activity of hyaluronidase which was used in the screening test of anti-allergic action was inhibited significantly by Amomi Semen, Asiasari Radix, Cimicifugae Rhizoma, Cinnamomi Ramulus, Glycyrrhizae Radix and Scutellariae Radix. The 48-hour homologous passive cutaneous anaphylaxis(48-hr PCA) in mouse ear was inhibited significantly by intraperitoneal(i.p.) injection of Amomi Semen, Cimicifugae Rhizoma, and ketotifen, a comparative drug of an anti-allergic action. The increase of vascular permeability induced by histamine or serotonin was inhibited significantly by i.p. injection of Amomi Semen, Cimicifugae Rhizoma, Cinnamomi Ramulus and ketotifen. In rat dorsal skin, the increase of vascular permeability which was induced by histamine, serotonin or compound 48/80 was inhibited significantly by i.p. injection of Amomi Semen, Asiasari Radix, Cimicifugae Rhizoma, Scutellariae Radix and ketotifen. Armeniacae Semen and Liriopis Tuber which had not inhibited hyaluronidase activity did not inhibit 48-hr PCA and the increase of histamine, serotonin or compound 48/80-induced vascular permeability in mice and rats. These results suggest that each water extract of Amomi Semen and Cimicifugae Rhizoma has anti-allergic action.

• Journal of the Korean Home Economics Association
• /
• v.37 no.12 s.142
• /
• pp.193-203
• /
• 1999

This study was executed to show influence of material and property of sportswear to physiological responses of body and comfort sensation and to supply basic research data about comfortable sportswear Trainning wear was manufactured with cotton(C) and hygroscopically treated polyester material (FP), and its properties of material were measured. Then rectal temperature, skin temperature, heart rate, weight loss, clothing microclimate and subjective sensation was estimated with study of wearing with these sportswear and examined the influence that it got to physiological responses of body and sensation. Health adult men were selected for subjects and executed at climatic chamber of temperature, $20\pm2^{\circ}C and humidity, $60\pm5%$ R.H. Conclusively sportswear of hygroscopically treated polyester is a favorable functional material. So far factor that affect to physiological comfort sensation has been explained mostly by moisture regain but in our experiment, it turned out that air permeability, water absorption velocity and dynamic oater absorption etc. were affecting factors. So according to this result, air permeability and moisture permeability should be considered with transmittance of temperature moisture for development of comfort material.

• Journal of Ginseng Research
• /
• v.42 no.4
• /
• pp.512-523
• /
• 2018

Background: 20(S)-Protopanaxadiol (20S-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability, thereby enhancing its skin deposition. Thus, we optimized microemulsion (ME)-based hydrogel (MEH) formulations for the topical delivery of 20S-PPD. Methods: MEs and MEHs were formulated and evaluated for their particle size distribution, morphology, drug loading capacity, and stability. Then, the deposition profiles of the selected 20S-PPD-loaded MEH formulation were studied using a hairless mouse skin model and Strat-M membrane as an artificial skin model. Results: A Carbopol-based MEH system of 20S-PPD was successfully prepared with a mean droplet size of 110 nm and narrow size distribution. The formulation was stable for 56 d, and its viscosity was high enough for its topical application. It significantly enhanced the in vitro and in vivo skin deposition of 20S-PPD with no influence on its systemic absorption in hairless mice. Notably, it was found that the Strat-M membrane provided skin deposition data well correlated to those obtained from the in vitro and in vivo mouse skin studies on 20S-PPD (correlation coefficient $r^2=0.929-0.947$). Conclusion: The MEH formulation developed in this study could serve as an effective topical delivery system for poorly soluble ginsenosides and their deglycosylated metabolites, including 20S-PPD.