• Journal of Korean Physical Therapy Science
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• v.10 no.1
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• pp.170-179
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• 2003

This study was performed that how phonophoresis using ultrasound for piroxicam affects transdermal permeation and anti-inflammative effects. Transdermal permeation study conducted by using hairless mouse had two categories: control group and ultrasound group. Transdermal permeation was observed according to duty cycle and intensity. Anti-inflammatory effects were determined using in Sprague-Dawley rat. The subjects were divided into three groups of six SD rat each 24 hour, 48 hour, 72 hour. The results of this study were as follows: 1. Transdermal permeation of piroxicam was measured according to ultrasound duty cycle. This research demonstrates that ultrasound group retains more transdermal permeation than control group, and that pulsed ultrasound group holds a little more transdermal permeation than continuous ultrasound group. 2. The transdermal permeation of piroxicam is closely related with ultrasound intensity. Effect of each group of transdermal permeation was significant rises in proportion to ultrasound intensity. 3. By observing inflammation of the tissue caused by trauma, phonophoresis group showed more significant of anti-inflammatory effect. The conclusion of phonophoresis was found to improve significantly the transdermal permeation and the anti-inflammatory effect.

• Journal of Pharmaceutical Investigation
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• v.26 no.2
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• pp.99-103
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• 1996

Effects of glycerin and PEG 400 in donor and receptor solutions upon skin permeation of drug were investigated. Deoxycortisone was used as a model compound. In vitro skin permeation study with freshly excised hairless mouse skin was performed and the steady-state skin permeation rates of the drug were determined in different fractions of glycerin or PEG 400 in donor and receptor solutions. Glycerin in donor solution didn't show any effect on the skin permeation rate of deoxycortisone. However glycerin in receptor solution showed significant effect on the skin permeation rate of the drug. In glycerin, there's a critical concentration for balancing hydration and dehydration of skin. At low concentration, less than 20 %, glycerin showed the enhancement of the flux due to the hydration effect of skin. At high concentration, more than 30 %, glycerin retard the permeation rate which might be due to the dehydration effect on the dermis layer. Since dermis has more water content than the stratum corneum, the steady state skin permeation rates were more influenced when glycerin was in receptor solution than that of in donor solution. PEG 400 aqueous solutions doesn't affect the steady state permeation rate of deoxycortisone significantly.

• Journal of Environmental Health Sciences
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• v.26 no.2
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• pp.91-96
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• 2000

We investigated characters of transdermal therapeutic system(TTS) and the skin permeability of that with applying drug delivery system(DDS). Natural gums were selected as material of TTS. The permeation of natural gums ointment containing drug in rat skin using diffusion cell model. Permeation properties of materials were investigated for water soluble drug such as riboflavin in vitro. We used glycerin, PEG 600 and oleic acid as enhancers. Since dermis has more hydration than the stratum corneum, skin permeation rate at steady state was highly influenced when glycerin was used in riboflavin. The permeation rate of content enhancer and drug was found to be faster than that of content riboflavin only. These results showed that skin permeation rate of drug across the composite was mainly dependent on the property of ointment base and drug. All the gum ointment tested showed good safety. Proper selection of the materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.

• 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 Environmental Health Sciences
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• v.43 no.1
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• pp.77-86
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• 2017

Objectives: The purpose of this study was to compare permeation characteristics in three skin types using oil-soluble benzoic acid and water-soluble caffeine after method condition optimization based on OECD guideline 428. Methods: A Franz diffusion cell, a reliable alternative method for skin permeation, was used. One-milliliter samples were taken and immediately replaced with fresh solution in the receptor chamber at regular time intervals (1, 2, 4, 7, 10 and 24 hr). The amount of test substances was measured by LC-MS/MS. Results: The permeation rate increased dose-dependently, and the permeation orders were $KeraSkin^{TM}$ > hairless mouse full skin > human cadaver epidermis for skin types, and benzoic acid solution > caffeine solution > benzoic acid cream > caffeine cream for type of test materials. Conclusion: According to the definitions of Marzulli, benzoic acid and caffeine would be classified as 'fast' and 'moderate' compared with the permeation of other chemical species. The setting conditions and permeation characteristics performed in this study are expected to contribute to future permeation studies.

• 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.

• Biomolecules & Therapeutics
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• v.19 no.1
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• pp.109-117
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• 2011

In this work, we have investigated the effect of polyoxyethylene alkyl ester nonionic surfactants on percutaneous permeation enhancement of a model drug, ketoprofen. We also investigated the mechanism involved in the enhancement using impedance and solubility measurement. Three groups of nonionic surfactants with different ethylene oxide content were studied. The permeation results showed that all surfactants enhanced the percutaneous absorption, irrespective of the molecular weight. The permeation results from PEG-45 monostearate (PEGMS45) were rather unexpected. Impedance and solubility results indicate that the mechanism involved in the enhancement of permeation by PEG-10 monooleate (PEGMO10) and PEGMS45 is rather different. The results from PEGMS45 suggest that it could be a potential candidate as a skin penetration enhancer with high molecular weight, which may poses less skin irritation and systemic side effect than the smaller surfactant molecules. Overall, this work provided some useful information on percutaneous transport enhancement and the mechanistic insights involved in skin permeation for these nonionic surfactants.

• Journal of Pharmaceutical Investigation
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• v.28 no.1
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• pp.1-5
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• 1998

The effect of synthetic polymer membranes on the permeation rate of dideoxynucleoside-type anti-HIV drugs through hairless rat skin was studied using ethylene/vinyl acetate copolymer (EVA) and ethylene/methyl acrylate copolymer (EMA) membranes fabricated by solvent casting method. In vitro skin permeation kinetics study of DDC (2',3'-dideoxythymidine), DDI (2',3'-dideoxyinosine) and AZT (3'-azido-3'-deoxythymidine) across the (membrane/skin) composite was conducted for 24 hours at $37^{\circ}C$ using the Valia-Chien skin permeation system. The results showed that skin permeation rate of each drug across the (skin/membrane) composite was mainly dependent on the property of the membrane. Proper selection of the polymeric membrane which resembles hydrophilicity/lipophilicity of the delivering drug was important in controlling the skin permeation rate.

• Journal of Pharmaceutical Investigation
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• v.25 no.2
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• pp.129-136
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• 1995

In order to reduce the systemic side effects and the gastrointestinal irritation of indomethacin following its oral administration, the drug was formulated as a transdermal gel using poloxamer 407. In vitro diffusion cells fitted with excised rat skins were used to evaluate the effects of formulation variables on skin permeation of indomethacin from poloxamer gels. The formulation variables were the concentrations of indomethacin, poloxamer 407 and ethanol, and the gel pH. The increase of the drug amount in the gel from 0.5% to 2.0% induced a direct but nonlinear increase in the skin permeation rate of indomethacin. The increase of poloxamer concentration from 17.5% to 25% in the gel resulted in a decrease of skin permeation rate of indomethacin, which was due to a reduction in the amount of free drug molecules available for permeation through skin by entrapping more drug molecules within the micelles formed by poloxamer. The increase of ethanol concentration from 10% to 20% in the gel resulted in a linear increase of permeation rate of indomethacin through skin, possibly due to the penetration enhancing effect of ethanol. The skin permeation of indomethacin was substantially influenced by the gel pH, exhibiting a maximum at pH 4.

• Archives of Pharmacal Research
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• v.26 no.5
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• pp.421-425
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• 2003

The aim of the present study was to evaluate the effects of two phospholipid permeation enhancers, lysophosphatidylcholine (LPC) and didecanoylphosphatidylcholine (DDPC), along with a fusidic acid derivative, sodium taurodihydrofusidate (STDHF) and ethanol (EtOH) on the buccal transport of propranolol hydrochloride (PPL) using an ex vivo buccal diffusion model. The permeation rate of [$^3 H$]PPL as measured by steady-state fluxes increased with increasing EtOH concentration. A significant flux enhancement (P＜0.05) was achieved by EtOH at 20 and 30 %v/v concentrations. At a 0.5 %w/v permeation enhancer concentration, the buccal permeation of [$^3 H$]PPL was significantly enhanced by all the enhancers studied (i.e., LPC, DDPC and STDHF) compared to the control (phosphate-buffered saline pH 7.4, PBS). LPC and DDPC displayed a greater degree of permeation enhancement compared with STDHF and EtOH-PBS mixtures with an enhancement ratio of 3.2 and 2.9 for LPC and DDPC, respectively compared with 2.0 and 1.5 for STDHF and EtOH:PBS 30:70 %v/v mixture, respectively. There was no significant difference between LPC and DDPC for the flux values and apparent permeability coefficients of [$^3$H]PPL. These results suggest that phospholipids are suitable as permeation enhancers for the buccal delivery of drugs.