• 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 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.3
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• pp.53-59
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• 1995

Ethinylestradiol (EE)-containing matrix was fabricated with ethylene-vinyl acetate(EVA) copolymer to control the release of the drug, Effect of addition of PEG 400 as receptor solution, the stripping of skin and Azone pretreatment on skin on the permeation of EE through the excised mouse skin was also studied. The permeation rate of EE through the excised mouse skin was affected by the PEG 400 volume fraction. The Azone pretreatment on skin didn't affect on the steady state flux, however, the lag time was shortened. The permeation rate of EE through the stripped skin was much larger than that through the whole skin. It showed that the stratum corneum acts as a barrier of skin permeation. The fact that there is little difference in EE permeation between the intact skin and the stripped skin with EVA membrane shows the permeation of EE through the mouse skin is mainly controlled by the membrane.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.23 no.3
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• pp.108-114
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• 1997

The skin permeation study has two meanings in cosmetics. One is how to promote the skin permeation of active meterials for improving their bioavailabilities and the other is how to decrease it of irritants for reducing their skin side effects. In this study, we selected methyl paraben, one of the preservatives, as a model irritant and tried to reduce the skin irritation by the decrease of skin permeation. Furthermore, the relationship between skin permeation and skin primary irritation was discussed. For in vitro skin permeation experiments, Franz type diffusion cells and the excised skin of female hairless mouse from 8 weeks old were used. The donor compartment was charged with oil only or O/W emulsion containing 0.3% MP. We selected 19 oils, including esters, triglycerides, plant oils, hydrocarbons, and alchols, which are broadly used in cosmetics. We evaluated with female guinea pig. The skin permeahility of MP from the oils showed following order: ester oils > triglycerides > plant oils > hydrocarbons > alcohols. We considered that this result was based on the different effect of each oil on the barrier function of stratum corneum. In O/W emulsion containing each oil, the skin permeability of MP decreased as the oil/water partition coefficient of MP increased. The skin primary irritation increased as the skin permeability of MP increased. In conclusion, we suggest that the skin irritation could be reduced by the decrease of skin permeability of MP, which may be obtained by the good selection of oils in cosmetic preparations.

• The Journal of Korean Physical Therapy
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• v.14 no.4
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• pp.147-162
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• 2002

Transdermal permeation enhancer has been used to increased skin absorption. External control of drug release and skin absorption can also be achieved by iontophoresis or phonophoresis. However, because several problems with iontophoresis are that it has a risk to skin damage because of the change of pH and the increase of current density in applying it and that it can be applied only in the form of water solution, This study is to enhance drug permeation via skin following application of ultrasound. For this goal, in gel containing piroxicam, the degree of skin permeation in vitro and anti-inflammatory effect in in vivo were investigated. Permeation study using hairless mouse skin was performed at 37 $^{\circ}C$ using buffer saline as the receptor solution. The amount of piroxicam were quantified using a HPLC system consisting of solvent delivery system. Following adoption of ultrasound 1 MHZ, it showed relatively high permeation rate where it was compared with non treated by ultrasound. The influence of duty cycle having an effect on skin permeation rate was slight higher in the case of using pulsed mode. Skin permeation increase attended by intensity of ultrasound, the permeation of trice was accelerated at 2.0 W/$cm^{2}$ than 1.0 W/$cm^{2}$. The skin permeation of piroxicam was substantially influenced by ultrasound. Anti-inflammatory effects were determined using carrageenan-induced paw swelling method in SD rat. Paw swelling tests showed that pulsed phonophoresis group was more effective than control group and only gel application group. The conclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory effect in vivo.

• 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 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.

• 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.

• Journal of Pharmaceutical Investigation
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• v.31 no.2
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• pp.95-100
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• 2001

Various alkyl ester prodrugs of diclofenac were synthesized in order to investigate the relationship between their skin permeation characteristics and physicochemical properties. Solubility in various vehicles was measured at room temperature. 1-Octanol/water partition coefficients (Log P) and capacity factors (k') were measured to determine the lipophilicity of the prodrugs. Stability of prodrugs in the skin extract and homogenate was also investigated before conducting the skin permeation studies. Increases in the Log P and capacity factor values were observed when alkyl esters of diclofenac were prepared. Since the aqueous solubility of the prodrugs was not high enough, they were saturated in propylene glycol (PG) for skin permeation studies. Prodrugs were rapidly metabolized to diclofenac, both in skin homogenate and in dermal extract of skin. The skin permeation rate of alkyl ester prodrugs was significantly higher than diclofenac with shorter lag time. Moreover, a parabolic relationship was observed between the permeation rate and the log P values of prodrugs, and the maximum flux was achieved at a log P value of around 4.0.

• Journal of Pharmaceutical Investigation
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• v.24 no.3
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• pp.27-32
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• 1994

In order to reduce systemic side effects following oral administration, flurbiprofen was formulated as transdermal gels consisting of the drug, poloxamer 407 and ethanol in buffer solutions. The effect of formulation variables in the preparation of flurbiprofen gels on skin permeation of the drug was evaluated using Keshary-Chien diffusion cells fitted with excised rat skins. The permeation rate of flurbiprofen through rat skin was directly proportional to initial drug concentration (between 0.1% and 1.0%) in the gel while it was inversely proportional to poloxamer 407 concentration (between 17.5% and 25%). The skin permeation of flurbiprofen was substantially influenced by the gel pH between 3 and 7, exhibiting a maximum at pH 4. The concentration effect of ethanol on the permeation of the drug was negligible in the concentration range of $10{\sim}20%$.