• YAKHAK HOEJI
• /
• v.60 no.1
• /
• pp.36-45
• /
• 2016

This study was aimed to enhance the percutaneous absorption of tizanidine hydrochloride (TZ) across Strat-M$^{TM}$ artificial membrane and excised hairless mouse skin using various vehicles and chemical permeation enhancers. Solubility studies were performed using hydrophilic and lipophilic vehicles. To initially evaluate vehicle effects on skin permeation, Strat-M$^{TM}$ membrane was adopted using Franz-type diffusion cells loaded with 0.4 mg donor dose. Effects of fatty acids on the permeation of TZ from PG and PGMC were compared, and the effects of various hydrophilic vehicles in the presence of linoleic acid were studied using excised hairless mouse skin specimens. The mean solubility (mg/ml) of TZ in hydrophilic vehicles was higher: water > PG > DMSO > ethanol > PEG 200 > NMP > PEG 300 > PEG 400 > DGME, and solubilities in lipophilic vehicles such as PGMC, PGMC, IPM, Captex 200 and Captex 300 were much less than 1.0 mg/ml. Permeation rates through StratTM membrane from pure vehicles were in the rank order: PGMC ${\geq}$ LBF > DMSO ${\geq}$ NMP ${\geq}$ PGML ${\geq}$ PG ${\geq}$ PEG 200 ${\geq}$ DGME ${\geq}$ EtOH. However, permeation rates of TZ through hairless mouse skin from pure vehicles were very low, although PG showed the highest flux ($1.66{\pm}0.28{\mu}g/cm^2{\cdot}hr$). Therefore, PG was selected in further studies. Addition of enhancers (3 v/v%) into PG markedly increased the flux (${\mu}g/cm^2{\cdot}hr$): oleyl alcohol ($14.9{\pm}3.1$) ${\geq}$ oleic acid ($14.5{\pm}1.6$) ${\geq}$ linoleic acid ($13.7{\pm}1.3$) > capric acid ($4.4{\pm}0.6$) > caprylic acid ($2.1{\pm}0.4$). Among hydrophilic vehicles with linoleic acid, PG and DMSO revealed relatively higher permeation for TZ. Increase of donor dose in PG resulted in dose-dependent permeation fluxes. These results suggest that permeation properties of TZ from nonaqueous solutions are markedly different between Strat-$M^{TM}$ membrane and excised hairless mouse skin, and transdermal delivery of TZ would be feasible with a combination of PG and enhancers.

• 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.

• Korean Journal of Animal Reproduction
• /
• v.22 no.3
• /
• pp.265-276
• /
• 1998

In an attempt to evaluate the function of MAP kinase of porcine oocytes and to develop a method of assessment for kinase activity, we used MBP as a substrate to detect the MAP kinase activity of porcine oocytes matured in in vitro. The MAP kinase which had lower activity during the first 20 hours of culture started to show an increased amount of activity at 25 hours at which a collapse in nuclear membrane was induced. Significant (P<0.05) a, pp.ared at 30 hours of being cultured. The gel phosphorylation method, MBP which has been known to be a substrate for kinase such as cdc2 kinase, was phosphorylated at two positions corresponding to ERK 1 (44kDa) and ERK2 (42 kDa) which are known as mammalian MAP kinase. The existence of MARKK and MAP kinase were identified with western blotting at 0 hour culture of immature GV oocytes. The amount of those proteins did not increase during 40 hours of culture, which suggest that the increase of MAP kinase activity was caused by phosphorylaton rather than due to change in protein amount. MAPKK and MAP kinase were shown to be dephosporylated with deactivated at M 1 stage by inhibition of protein synthesis with cycloheximide added at the strat following the cultrue. We have reulsts that indicate the existedence of MAP kinase cascade which was activated simultaneously with start of porcine oocyte maturation (GVBD).

• Journal of Life Science
• /
• v.31 no.11
• /
• pp.1004-1009
• /
• 2021

Angelica gigas Nakai (AGN) has been used in Korean herbal medicine for various pharmacological activities, such as to create antioxidant and skin whitening effects. Decursin and decursinol angelate of AGN extracts can be used as potential active drugs and cosmetic ingredients. This study investigated the possibility of topical delivery of AGN extracts using a manufactured emulsion system. Lotion was formulated by using Tefose^® and paraffin for the oil phase, Kolliphor RH 40 for the surfactant and solubilizing agent-which showed high solubility in water (0.82 mg/ml)-and a water phase with a carbomer. In vitro skin permeation of decursin and decursinol angelate was determined using a Strat-M^® membrane in Franz diffusion cells. Lotion samples as the experimental group (248.08±19.72 ug/cm²) significantly increased the permeation of decursin and decursinol angelate for up to 24 hr compared to the control group (119.18±19.23 ug/cm²). The permeability was also characterized by the flux (penetration rates) and Kp (permeability coefficient) values. The experimental group (17.20±1.23 ug/h/cm² and 5.73±1.39 cm/h^*10^-3) had higher flux and Kp than the control group (8.22±1.24 ug/h/cm² and 2.74±0.51 cm/h^*10^-3). Lotion with decursin and decursinol angelate of AGN extracts could be used for the topical application of drug and cosmetic products.

• 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.