• Archives of Pharmacal Research
• /
• 제28권1호
• /
• pp.111-114
• /
• 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.

• 대한의용생체공학회:의공학회지
• /
• 제44권4호
• /
• pp.275-283
• /
• 2023

The demand for skincare has increased due to the end of the COVID-19 pandemic, leading to a focus on skincare devices and technologies designed to improve the delivery of cosmetics. Among these technologies, skincare medical devices that utilize plasma therapy (Plasma) and sonophoresis (Sono) are commonly used in dermatology clinics. However, there is still a lack of quantitative analysis for transdermal absorption effects of Plasma and Sono skincare medical devices. In this study, we quantified enhanced transdermal absorption effects of Plasma and Sono devices through in-silico and ex-vivo studies. The Sono treatment demonstrated an increased transdermal absorption effect, showing a 10~13% difference in penetration compared to the control group in the in-silico experiment, and 159% and 184% increase in the ex-vivo experiment. The Plasma treatment revealed increased transdermal absorption effects, with a 1.0~2.5% penetration difference in the in-silico experiment, and a 124% increase in the ex-vivo experiment compared to the control group. We also observed a synergistic effect from the combined treatment of Plasma and Sono, as indicated by the highest increases of 197% and 242% in penetration. Furthermore, we have determined the optimal device settings and treatment conditions for Plasma-Sono skincare medical devices. Notably, higher on/off durations (Intensity levels) and longer Sono treatments resulted in greater transdermal absorption effects.

• Archives of Pharmacal Research
• /
• 제19권2호
• /
• pp.95-99
• /
• 1996

Four N-adamantyl n-alkanamides were prepared by amide condensation reaction between amantadine and n-alkanoic acid. Their enhancing activity on the penetration of ibuprofen through rabbit skin from petrolatum ointment was evaluated in in-vivo experiment. The experiments showed that the compounds have a strong transdermal penetration-enhancing activity, and their activities were comparable with that of Azone. The measurements of the fluorescence polarization of DP[-i-labelled DPPC liposomes showed that these compounds considerablly decreased the phase transition temperature of the liposomes. The mechanism of the transdermal penetration-enhancing activity of the compounds was ascribed to the reduction of the resistance to drug flux of the stratum corneum lipid layers due to the loose packing of the layers when the bulk head group of the enhancers inserts into the layers.

• KSBB Journal
• /
• 제28권5호
• /
• pp.319-326
• /
• 2013

This study was carried out to investigate the in vitro and in vivo moisturizing properties and percutaneous absorption of PEG-impregnated Aloe vera gel. The PEG-i-Aloe gel was obtained from dewatering and impregnation by soaking (DIS) of Aloe vera leaf slice. The moisturizing property of the obtained sample was evaluated by moisture determination using gravimetric method in desiccator under different RH% and by water sorption-desorption test on human skin. The transdermal penetration characteristics of PEG-i-Aloe gel was investigated by Franz diffusion cell in vitro transdermal absorption method. PEG-i-Aloe gel had high moisture retention ability and could significantly lead the enhancing skin hydration status as well as reducing the skin water loss due to the film formation as a skin barrier. The skin penetration rate of PEGi- Aloe gel at steady state was 9.76 ${\mu}g/(h{\cdot}cm^2)$ and the quantity of the transdermal absorption was 144 ${\mu}g/cm^2$ in 9 hr. The penetration mechanism was well fitted with Higuchi model ($R^2$ = 0.974-0.994). The results show that PEG-i-Aloe gel has the significant moisturizing effect and strong penetration of the animal skin. It could be used as the moisturizing additive in cosmetic skin products.

• KSBB Journal
• /
• 제26권4호
• /
• pp.277-282
• /
• 2011

The penetration of outside material into skin is not easy. It is since the skin, which is a very hard barrier, protects the body against outside chemical and physical stimulation. Microneedle system which can help improve drug penetration into skin is advancing variously in transdermal drug delivery system (TDDS) in the field of skin care. After inserting microneedle into skin by using electrical or artificial forces, it makes microhole and drug penetration easily and induces natural skin rejuvenation. Diffusion and penetration of drug by optical and electrical force of microneedle is better for fast and effective TDDS. This is more developed than the traditional method such as the manual stamp, roller, and meso gun. The drug absorbed into dermal layer by microneedle helps revive and repair damaged skin. In the future, utilization of microneedle for skin care will progress constantly because of its human-friendly biodegradable materials and the development of the no pain microneedle.

• Journal of Pharmaceutical Investigation
• /
• 제30권4호
• /
• pp.247-252
• /
• 2000

The advantages of transdermal administration are avoiding hepatic first pass effect, minimizing inter- and intra-patient variation, maintaining steady-state plasma level to provide long-term therapy from a single dose, and allowing a rapid termination of drug input. Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease. For the development of transdermal systems containing clenbuterol, two limiting factors - long lag time and low flux - must be overcome. In this study, we attempted to select optimal formulation for preparation of clenbuterol patch using hairless mouse skin and flow-through diffusion cell. The flux of clenbuterol increased as the percent of clenbuterol dose dependently in the concentration range of 5-15%. Based on this result, we fixed the concentration of clenbuterol as 15%. The effect of various penetration enhancers on percutaneous absorption of clenbuterol through hairless mouse skin was investigated. Labrafil was the most effective enhancer, which increased the permeability of clenbuterol approximately 4-fold compared with the control without penetration enhancer. Optimal enhancer concentration was 3%. The effect of various adhesives on penetration of clenbuterol was also investigated. Among the adhesives studied, MA-31 was the most effective adhesive. Furthermore, the clenbuterol patch composed of 15% clenbuterol, 3% Labrafil and 82% MA-31, which gave most excellent penetration of drug in in vitro penetration study, maintained therapeutic plasma levels in in vivo study using S.D. rats. These studies demonstrated a good feasibility of clenbuterol administration through the intact skin using a transdermal patch, and show a possibility of the development of clenbuterol patches.

• The Journal of Korean Physical Therapy
• /
• 제23권6호
• /
• pp.77-84
• /
• 2011

Purpose: The objectives of this study were to determine the enhancing effect of iontophoresis method as it transdermally deliver methylene blue (MB) using visual examination, in terms of penetration depth and tissue distribution in the skin, and to determine the effect of application duration on the efficacy of iontophoresis. Methods: Twenty-four male Sprague-Dawley rats were randomly divided into 5-, 10-, 20-, and 40-minute groups. These rats were exposed to either topical or anodic iontophoresis of 1% MB using a direct current of $0.5mA/cm^2$ for 5, 10, 20, and 40 minutes. Using cryosections of rat tissues, the penetration depth of MB was measured using light microscopy. Results: Significant differences in the penetration depth (F=54.20, p<0.001) were detected among the four groups. Post hoc comparisons of the penetration depth of MB data pooled across groups showed no significant difference between all topical application groups and 5-minute iontophoresis group, but did reveal a significant difference in the penetration depth between all topical application groups and 5-minute iontophoresis group versus 10-minute group, between the 10-minute and 20-minute group, and between the 20-minute and 40-minute iontophoresis group (p<0.05). Conclusion: The results demonstrate that iontophoresis enhances transdermal delivery of MB across stratum corneum of skin barrier by visual examination. Furthermore, the penetration depth of iontophoretic transdermal delivery of MB was dependent on the application duration. The duration of iontophoresis is one of the important factor in the efficacy of iontophoresis application.

• Journal of Pharmaceutical Investigation
• /
• 제29권1호
• /
• pp.29-36
• /
• 1999

Aceclofenac is an non-steroidal antiinflammatory drug which has been used in the treatment of rheumatoidal rthritis and osteo-arthritis. In order to decrease the gastric ulcerogenic effects and contol the plasma level of aceclofenac, we have developed the transdermal delivery system of aceclofenac plaster, which were formulated employing matrix polymers of acrylates and penetration-enhancers such as $Lauroglycol^{\circledR}$, $Transcutol^{\circledR}$, oleic acid and linoleic acid. Using Franz diffusion cells mounted with a rat skin, transdermal penetration characteristics of the formulations were evaluated by the HPLC assay of aceclofenac and diclofenac, an active metabolite, in the receptor compartment of pH 7.2 phosphate buffered solution. Skin penetration was increased when the content of aceclofenac increased, showing the flux $(J,\;{\mu}g/cm^2/hr)$ of 0.37 and 2.50 for 2% and 6.75% of the content, respectively. The flux$(J,\;{\mu}g/cm^2/hr)$ from plasters made of $Durotak^{\circledR}$ 87-2074, $Durotak^{\circledR}$ 87-2510 and $Durotak^{\circledR}$ 87-2097 were 2.50, 2.77 and 4.39, respectively. $Durotak^{\circledR}$ 87-2074 showed the lowest penetration due to the carboxylic acid group in the polymer, which might form a strong hydrogen bonding with a secondary amine of aceclofenac. Although both $Durotak^{\circledR}$ 87-2510 and $Durotak^{\circledR}$ 87-2097 are amine-resistant adhesives, $Durotak^{\circledR}$ 872510 showed lower penetration than $Durotak^{\circledR}$ 87-2097 because of the hydroxyl group in $Durotak^{\circledR}$ 87-2510, which might form a weak hydrogen bonding with aceclofenac. These results reveal that the functional group in acrylic polymers would greatly affect the release of aceclofenac from the matrix, which is the rate-limiting step in the penetration of aceclofenac through rat skins. The penetration of aceclofenac from plasters using different penetration-enhancers increased in the following order: Transcutol < linoleic acid < oleic acid. And the flux from the plasters containing oleic acid as a penetrationenhancer was 2.22 times greater than that of creams, which suggest that a newly deveolped aceclofenac plaster could be used in the treatment of rheumatoidal arthritis and osteo-arthritis as an advanced transdermal delivery system.

• Bulletin of the Korean Chemical Society
• /
• 제24권4호
• /
• pp.499-503
• /
• 2003

Encapsulation of L-ascorbic acid (vitamin C) within a bio-compatible layered inorganic material was achieved by coprecipitation reaction, in which the layered inorganic lattice and its intercalate of vitamin C are simultaneously formed. The nano-meter sized powders of vitamin C intercalate thus prepared was again encapsulated with silica nano-sol to form a nanoporous shell structure. This ternary nanohybrid of vitamin Clayered inorganic core-$SiO_2$ shell exhibited an enhanced storage stability and a sustained releasing of vitamin C. Furthermore, the nano-encapsulation of vitamin C with inorganic mineral was very helpful in delivering vitamin C molecules into skin through stratum corneum, facilitating transdermal penetration of vitamin C in topical application.

• 공업화학
• /
• 제16권1호
• /
• pp.15-20
• /
• 2005

최근 약물전달시스템에 관심이 높아지면서 질병 치료를 목적으로 치료용 약물들이 많이 개발되기 시작하였으며, 이 중 경피흡수제제는 여러 가지 이점으로 인하여 지속적으로 연구를 진행하고 있는 흥미로운 분야이다. 본 고에서는 이러한 경피흡수의 원리 및 흡수를 촉진하는 물질들에 대하여 서술하였으며, 이를 발전시키기 위한 in vitro 및 in vivo 연구에 대하여 논하였다.