• Journal of Pharmaceutical Investigation
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• v.28 no.1
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• pp.15-23
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• 1998

Extract of Centella asiatica(ECA), which is poorly water-soluble extract from the Centella asiatica is known to express excellent wound healing properties. $ECA-{\beta}-cyclodextrin$ $(asiaticoside-{\beta}-cyclodextrin\;and\;genin-{\beta}-cyc1odextrin)$ solid dispersion system, which was prepared by freezedrying method, was formulated as gels containing poloxamer 407 and propylene glycol, and evaluated with respect to their viscosity, stability, skin permeation and drug amount in the skin of hairless mouse. The average molar ratio $asiaticoside-{\beta}-CD$ and $genin-{\beta}-CD$ was 1:1.7 and 1:22, respectively. When the molar ratio of genin and ${\beta}-CD$ was 1:5, madecassic acid made 100% solid dispersion system and asiatic acid about 65%. In dissolution study, >99% of asiaticoside from $asiaticoside-{\beta}-CD$ was dissolved in 5 minutes, and >99% madecassic acid and >64% asiatic acid from $genin-{\beta}-CD$. The apparent viscosity of poloxamer 407 gels with $ECA-{\beta}-CD$ solid dispersion system increased in proportion to poloxamer 407 and propylene glycol concentration. In the accelerated stability test, all $ECA-{\beta}-CD$ poloxamer 407 gels showed that asiaticoside was most stable and madecassic acid stable and asiatic acid similar to stability of gel with free ECA. The permeation amount of asiaticoside in poloxamer gels through hairless mouse skin decreased as the concentration of poloxamer 407 increased. When propylene glycol was added at the level of 10%, the permeation amount of asiaticoside at poloxamer gels through hairless mouse skin increased but from 15% it decreased. The permeation of asiaticoside into the skin of hairless mouse was estimated to be about $0.10\;{\mu}g/cm^2$.

• Journal of the Korean Academy of Clinical Electrophysiology
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• v.4 no.1
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• pp.49-61
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• 2006

This study conducted the following experiment to examine and compare transdermal permeation effects according to parameters of ultrasound and physiochemical characteristics of meloxicam. Permeation by ultrasound among these experimental drugs was relatively higher and it was involved in COX-2 inhibition unlike other drugs. Recently use of oral agents has been rapidly increased, but it was not generalized to transdermal agent and this study selected meloxicam that transdermal permeation research using ultrasound was not performed and conducted transdermal permeation experiment with skin of hairless mouse and analyzed permeation with HPLC. It made gel first and analyzed permeation depending on frequency and intensity of ultrasound of meloxicam with the same experimental procedures as the above experiment. The results of this study can be summarized as follows. Transdermal permeation by ultrasound frequency was higher in 1.0 MHz and it was higher as intensity increased. In comparison by parameters of ultrasound, there was similar permeation in $1.0\;W/cm^2$ of continuous mode and $3.0\;W/cm^2$ of pulsed mode and it was effective to high intensity for using pulsed mode. It was found that duty cycle of ultrasound affected transdermal permeation in meloxicam gel used in this experiment and transdermal permeation was higher in used ultrasound as phonophoresis than non-ultrasound for anti-inflammatory effects.

• Bulletin of the Korean Chemical Society
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• v.28 no.1
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• pp.99-102
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• 2007

To prepare freeze-dried ascorbyl palmitate (AsP)-containing liposome which can protect the drug from moisture attack and be used instantly by mixing with water for anti-aging and skin whitening therapy, AsP was encapsulated into liposomes and freeze-dried with trehalose. The freeze-dried liposome formulations were characterized by measuring water contents, particle size, time required for complete reconstitution. With the freeze-dried liposomes, we performed the stability test under accelerated conditions, skin permeation and localization test. The measurement of the time to perfect reconstitution showed that the freeze-dried liposomes can be changed to their initial state rapidly and short term stability test of AsP in reconstituted liposomes under accelerated conditions confirmed that the stability of AsP was considerably enhanced as compared to freshly prepared liposomes. The skin permeation and localization properties of AsP in reconstituted liposomes were not significantly different, indicating that the liposomal structures were maintained before and after freezedrying. In conclusion, the freeze-drying method provided a possible way to overcome the instability issue of AsP induced by the moisture and reproduced similar skin permeation and localization properties as shown by freshly prepared liposomes.

• Archives of Pharmacal Research
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• v.27 no.7
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• pp.763-768
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• 2004

To investigate the feasibility of developing a new quercetin transdermal system, a preformulation study was carried out. Therefore, the effects of vehicles and pressure-sensitive adhesives (PSA) on the in vitro permeation of quercetin across dorsal hairless mouse skin were studied. Among vehicles used, propylene glycol monocaprylate (PGMC) and propylene glycol mono-laurate were found to have relatively high permeation flux from solution formulation (i.e., the permeation fluxes were 17.25$\pm$1.96 and 9.60$\pm$3.87 $\mu\textrm{g}$/$\textrm{cm}^2$/h, respectively). The release rate from PSA formulations followed a matrix-controlled diffusion model and was mainly affected by the amount of PSA and drug loaded. The overall permeation fluxes from PSA formulations were less than 0.30 $\mu\textrm{g}$/$\textrm{cm}^2$/h, which were significantly lower compared to those obtained from solution formulations. The lower permeation fluxes may be due to the decrease of solubility and diffusivity of quercetin in the PSA layer, considering the fact that the highest flux of 0.26 $\mu\textrm{g}$/$\textrm{cm}^2$/h was obtained with the addition of 0.2％ butylated hydroxyanisole in PGMC-diethyl-ene glycol monoethyl ether co-solvents (80-85 ： 15-20, v/v). Taken together, these observations indicate that improvement in the solubility and diffusivity of quercetin is necessary to realize fully the clinically applicable transdermal delivery system for the drug.

• Journal of Environmental Health Sciences
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• v.30 no.2
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• pp.65-70
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• 2004

Hair is based upon the skin which enroll the body of high living animals and have multiple membrane structure. This study were used rats and carried out to find out the effects of commercial permanent wave products to skin which are composed of thioglycolic acid and bases. Results were as follows. Permanent wave penetrated to 3 hours later with steady state in skins and was not significant changeable after 20hr later. In case of neutralizer with thioglycolic acid lag time and permeability coefficient in healthy skin were 3.38hr and 0.96$\mu\textrm{g}$/$\textrm{cm}^2$/hr, in old skin were 3.14hr and 0.l28$\mu\textrm{g}$/$\textrm{cm}^2$/hr, and in wounded skin were 3.08hr and 0.157$\mu\textrm{g}$/$\textrm{cm}^2$/hr. In conclusion, lag time and permeability coefficient in old skin and wounded skin were faster than healthy skin. In vivo which was studied by general time and method of permanent wave. We found out that fine rinkle and rash of skin were changeable in the case of treating with permanent wave drugs than normal skin. Also, permanent wave drugs could induced rash and eruption at the skin by the naked eye.

• Journal of Pharmaceutical Investigation
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• v.35 no.5
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• pp.329-332
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• 2005

HPMC-based novel gel formulations for the transdermal delivery of testosterone (TS) were developed, and the effect of various skin permeation enhancers was studied in vitro and in vivo. In vitro hairless mouse skin permeation of TS from the gel was investigated using Keshary-Chien diffusion cells for 8 hours at $37^{\circ}C$. In vivo plasma concentration profiles of TS after applying the gel on the abdominal skin of rat were determined using a commercial radioimmunoassay kit. Hairless mouse skin permeation of TS increased with the addition of permeation enhancers both in vitro and in vivo. Combination of diethanolamine (2%) and N-methylpyrrolidone (NMP, 6%) was the most effective among tested. Plasma concentration of TS significantly increased for at least 24 hours with the addition of diethanolamine and NMP. These results suggest the feasibility of the development of a HPMC-based gel formulation for the transdermal delivery of TS.

• Translational and Clinical Pharmacology
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• v.25 no.1
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• pp.15-20
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• 2017

This study was performed to evaluate the use of vibrating microneedles for the transdermal delivery of vitamin C. The microneedles were designed to vibrate at three levels of intensity. In vitro permeation by vitamin C was evaluated according to the specific conditions such as vibration intensity (levels 1, 2 and 3), application time (1, 3, 5, 7 and 10 min), and application power (500, 700 and 1,000 g). The highest permeation of vitamin C was observed at level 3 of vibration intensity, 5 min of application, and 1,000 g of application power. Vitamin C gel showed no cytotoxic effect against Pam212 cells or skin irritation effects. A pharmacokinetic study of the gel in rats was conducted under optimized conditions. The $AUC_{0-{\infty}}$ and $C_{max}$ increased 1.35-fold and 1.44-fold, respectively, compared with those after vitamin C gel without application with vibrating microneedles. The present study suggests that vibrating microneedles can be used to facilitate the skin permeability of vitamin C under optimal conditions.

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.203.1-203.1
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• 2000

• KSBB Journal
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• v.16 no.3
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• pp.253-258
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• 2001

Recently, there were many studies not only to enhance drug delivery effect but to reduce side effect. Drug delivery system(DDS) is able to improve efficiency with decreasing side effect of drug dosage. Among these application fields, DDS is often used as the method of drug dosage into the epidermic skin. We investigated characters of transdermal therapeutic system(TTS) and the skin permeability of that with applying DDS. We investigated the permeation of xanthan gum containing drug in rat skin using borizontal membrane cell model. Permeation properties of materials were investigated for water-soluble drug with oxiniacic acid and also for lipophilic drug with clofibrate. The permeation rate of lipophilic drug was found to be faster than that of water-soluble drug in vitro. The rate differences of both water-soluble drug and lipophilic drug according to drug content were negligible. We used glycerin, PEG 600 and oleic acid as enhancers. These results showed that skin permeation rate of each drug across the composite was mainly dependent on the property of base and chemical property of drug etc.. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate. This result suggests a possible use of natural polymer base as a transdermal delivery system of antihyperlipoproteinemic agent.

• Journal of Environmental Health Sciences
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• v.39 no.4
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• pp.360-368
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• 2013

Objectives: Phthalates are used in a large variety of products including as coatings of pharmaceutical tablets, film formers, stabilizers, dispersants, emulsifying agents, and suspending agents. They have been the subject of great public concern in recent years. The extensive uses of this material have attracted attention and issues regarding its safety have been raised. Methods: In this study, three types of phthalate skin permeation were studied using matrixes such as ointments, creams and lotions in vitro. The absorption of phthalate diesters [Dimethyl phthalate (DMP), Di-n-propyl phthalate (DPP) and Di-n-pentyl phthalate (DNPP)] using film former has been measured in vitro through rat skin. Epidermal membranes were set up in Franz diffusion cells and their permeability to PBS measured in order to establish the integrity of the skin before the phthalates were applied to the epidermal surface. Results: Absorption rates for each phthalate ester were determined and permeability assessment made to quantify any irreversible alterations in barrier function due to contact with the esters. Types of phthalate in vitro experimental results quickly appeared in the following order DMP > DPP ${\geq}$ DNPP. Conclusions: In the experimental results, lotion> cream> ointment, and the permeation rate of lotion with a great amount of moisture was the fastest. Skin permeation rate is generally influenced by the chemical characteristics of a given chemical, such as molecular weight and lipophilicity. As the esters became more lipophilic and less hydrophilic, the rate of absorption decreased.