• The Journal of Korean Physical Therapy
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• v.18 no.1
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• pp.75-82
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• 2006

Purpose: This study conducted the following experiment to examine transdermal permeation effects or 500 KHz ultrasound with lidocaine HCl. Methods; First, to experiment skin permeation enhancement effects of 500 KHz ultrasound frequency, it produced apparatus and transducer of 500 KHz ultrasound and Franz diffusion cell for skim permenation experiment suitable to purposes of the experiment. Transdermal permeation experiment applied Lidocaine HCL gel to skin of hairless mouse depending on ultrasound frequency and duty cycle and analyzed permeation ratio with HPLC. Results: As a result of fixing lidocaine HCl gel at the same intensity with pulsed mode and continuous mode and comparing transdermal permeation ratio by frequency, transdermal permeation ratio was increased at 500 KHz ultrasound and remarkably increased at continuous ultrasound. It was found that 1 MHz and 500 KHz ultrasound in transdermal permeation experiment enhanced transdermal permeation of lidocaine HCl. In particular, transdermal permeation of 500 KHz using lidocaine HCl gel was highest. Conclusion: However, researches considering various frequencies, intensities and application hours in low frequency areas including 500 KHz ultrasound are needed to increase deep permeation or drugs.

• Journal of Pharmaceutical Investigation
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• v.24 no.1
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• pp.17-24
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• 1994

The antiinflammatory and antirheumatic activities of a 3% ketoprofen gel (ID-GEL) were evaluated using carrageenan-induced paw edema method and adjuvant-induced arthritis method, respectively, after its transdermal administration of 50 mg on rat paws in reference to existing transdermal preparations containing 3% ketoprofen and other nonsteroidal antiinflammatory drugs (NSAIDs). The % inhibition of carrageenan-induced edema by ID-GEL was 56.2-65.0%, close to the maximum inhibition obtainable with this model, while the % inhibition by existing 3% ketoprofen gels and other NSAID transdermal preparations were 33.8-47.7% and 18.7-29.2%, respectively. ID-GEL had a pronounced antirheumatic activity in both preventive and curative studies with adjuvant-induced arthritis in rats in respect with the inhibition of edema, arthritis score and weight gain, in reference to existing 3% ketoprofen gel.

• 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.

• Journal of the Korean Academy of Clinical Electrophysiology
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• v.1 no.2
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• pp.11-19
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• 2003

The purpose of this study investigated the anesthetic effects of lidocaine gel by phonophoretic transdermal delivery. The anesthetic effects were evaluated by two aspects as quantitative sensory testing and sensory nerve conduction study. Twelve healthy males(aged $23.25{\pm}2.09$ years) were studied. Exclusion criteria were ; pain, history of sensory disturbances and skin conditions in the areas to be examined. The subjects were divided into two groups; group I(lidocaine gel without ultrasound) and group II(lidocaine gel with ultrasound). The following results were obtained; 1. In changes of tactile threshold and electrical pain threshold, all groups were significantly increased(p<0.05). 2. In changes of electrical pain threshold, it was significantly differenced between the groups(p<0.05). We conclude that the transdermal delivery of lidocaine gel by phonophoresis has a possibility to use for surface anesthesia and the pain control of the superficial tissue.

• Biomolecules & Therapeutics
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• v.16 no.3
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• pp.210-214
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• 2008

The pharmacokinetic parameters and bioavailability of pranoprofen from the gel were measured to determine the enhancing effect of octanoic acid on the transdermal absorption of pranoprofen in rats. 8 mg/kg of pranoprofen was administered from gel with octanoic acid (the enhancer group) or that without octanoic acid (the control group) via the transdermal route, and the results were compared with those obtained from the intravenously (0.5 mg/kg, IV group) or orally administered group (4 mg/kg, oral group). The AUC of the control, the enhancer, the IV, and the oral groups were $20.2{\pm}5.1$, $50.7{\pm}12.7$, $19.9{\pm}2.5$, and $70.5{\pm}17.6\;ug/ml{\cdot}h$ respectively. The average $C_{max}$ of the control and the enhancer group were $0.93{\pm}0.23$ and $2.82{\pm}0.71\;ug/ml$, respectively, and the mean $T_{max}$ of the control and the enhancer group was 7.00 h. The relative bioavailability of the transdermally administered pranoprofen gel containing octanoic acid was approximately 2.50 times higher than the control group, showing a relatively constant, sustained blood concentration with minimal fluctuation. This suggests that it might be feasible to develop a pranoprofen gel preparation containing an enhancer for the transdermal administration, which is more convenient dosage form than the oral dosage forms.

• KSBB Journal
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• v.28 no.5
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• pp.319-326
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• 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.

• Journal of Pharmaceutical Investigation
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• v.24 no.2
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• pp.105-108
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• 1994

The ulcerogenic activity of a 3% ketoprofen gel (ID-GEL) after its transdermal application in rats was determined with the Litchfield and Wilcoxon method in reference to the oral administration of ketoprofen in a suspension. The $UD_{50}$ (dose producing ulcers in 50%, of the rats tested) of ID-GEL after its transdermal application was approximately 4 times greater than that after the oral administration of the drug, indicating that the ulcerogenic activity of ketoprofen was much lowered with its transdermal application.

• 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.

• Journal of Pharmaceutical Investigation
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• v.24 no.1
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• pp.11-16
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• 1994

In order to reduce the systemic side effects and gastrointestinal irritation of ketoprofen after its oral administration, it was formulated as a 3% ketoprofen gel (ID-GEL) with Pluronic F-127. The pharmacokinetic characteristics of ID-GEL was evaluated following its transdermal application on the dorsal skin of rats at the dose of 9 mg/kg in reference to those of existing 3% ketoprofen gels. Even though the maximum concentration of 810 ng/ml was reached at 6 hrs postdose, the plasma concentration was kept almost constant until 24 hrs postdose, which suggested that ketoprofen was released continuously from the gel during this period. The bioavailability of ID-GEL was two times higher than those of existing 3% ketoprofen gels, based on the calculated area under the plasma concentration-time curves after the percutaneous administration.

• Journal of Pharmaceutical Investigation
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• v.39 no.6
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• pp.437-443
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• 2009

To develop a topical bioadhesive formulation of clotrimazole for enhanced transdermal delivery, hydroxypropyl methylcellulose gel containing permeation enhancer was formulated and permeation studies were carried out. The release characteristics of the drug from the gel formulation were examined according to the receptor medium, drug concentration, and temperature. The rate of drug release from the gel increased with increasing drug concentration and temperature. The activation energy (Ea) of drug permeation, which was calculated from the slope of log P versus 1/T plots, was 14.41kcal/mol for a 1%(w/w) loading dose. The enhancer, such as saturated, unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants, were incorporated onto the gels to increase the amount of drug permeation into the skin. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest level of enhancement. These results show that clotrimazole gels containing polyoxyethylene 2-oleyl ether could be used for the enhanced transdermal delivery of clotrimazole.