• 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.

• Membrane Journal
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• v.9 no.1
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• pp.43-50
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• 1999

The effects of water vapor on the permeation rates of oxygen and nitrogen through poly sulfone hollow-fiber membrane were investigated. The permeation rates of both 02 and $O_2$ were decreased significantly owing to the presence of water vapor. The permeation rate of oxygen with 100% relative humidity was reduced by as much as 20%, while the permeation rate of nitrogen decreased by 14% at 30 "C and 3kgf/$cm^2$ of upstream pressure. The permeation rates of $O_2$ were declined monotonously with running time and arrived at steady state values by the presence of water vapor. However, those of $N_2$ increased tentatively and then decreased to the steady state.tate.

• 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.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 Korean Applied Science and Technology
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• v.17 no.1
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• pp.43-48
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• 2000

Drug delivery system(DDS) applied to various fields, such as medicine, cosmetics, agriculture and necessities of life. 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. Chitosan was selected as material of TTS. We investigated the permeation of chitosan ointment containing drug in rat skin using horizontal membrane 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 content water(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when glycerin was used in water-soluble drug. The permeation rate of content enhancer and drug was found to be faster than that of content water-soluble drug only. These results showed that skin permeation rate of drug across the composite was manly dependent on the property of ointment base and drug. 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.

• Archives of Pharmacal Research
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• v.27 no.11
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• pp.1177-1182
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• 2004

The effect of poly[2-methacryloyloxyethyl phosphorylcholine] (pMPC) on the skin permeation property was investigated by performing in vitro skin permeation study of a model drug, nicotinic acid (NA). Effect of pMPC polymer in donor solution on skin permeation rates was evaluated using side-by-side diffusion cells. Also, the structural alterations in the stratum corneum (SC), inter-lamellar bilayer (ILB) and dermis layers in pMPC-treated and -untreated skin sections were investigated with transmission electron microscopy (TEM). The permeation profile of NA without pMPC in donor solution showed biphasic mode: initial $1^{st} phase and 2^{nd}$ hydration phase. The sudden, more than 10-fold increase in flux from the initial steady state (43.5 $\mu g/cm^2$/hr) to the $2^{nd}$ hydration phase (457.3 $\mu g/cm^2$/hr) suggests the disruption of skin barrier function due to extensive hydration. The permeation profile of NA with 3% pMPC in the donor solution showed monophasic pattern: the steady state flux (10.9 $\mu g/cm^2$/hr) without abrupt increase of the flux. The degree of NA permeation rate decreased in a concentration-dependent manner of pMPC. TEM of skin equilibrated with water or 2% pMPC for 12 h showed that corneocytes are still cohesive and epidermis is tightly bound to dermis in 2% pMPC-treated skin, while wider separation between corneocytes and focal dilations in inter-cellular spaces were observed in water-treated skin. This result suggests that pMPC could protect the barrier property of the stratum corneum by preventing the disruption of ILB structure caused by extensive skin hydration during skin permeation study.

• 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.

• Journal of Pharmaceutical Investigation
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• v.35 no.4
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• pp.273-278
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• 2005

Nicotine transdermal therapeutic systems $(TTS_S)$ have been regarded as an effective mean to aid smoking cessation. However, most of nicotine $TTS_S$ in the market have some problems such as unpleasant side effects and skin irritation due to the excess amount of the drug permeated and the properties of the additives employed. In order to solve these problems, new nicotine $TTS_S$ were formulated using biocompatible additives. The optimized formula of the drug layer consisted of nicotine, propylene glycol and poloxamer 188 at the ratio of 1.2: 17.0: 2.0. The drug layer had the sickness of $1,250\;{\mu}m$, the pH of 8.12. The skin permeation rate of nicotine from optimized nicotine patch (NP) was $21.5\;{\mu}g/cm^2/h$. Transdermal administration of nicotine patch has been carried out for the determination of pharmacokinetic parameters in rats. Steady-state plasma concentration of nicotine following transdermal application of NP (area of patch = $15\;cm^2$) on the dorsal skin of rats was 143.2 ng/ml and AUC for 24 hrs was 3,022 ng h/ml. In case of $EXODUS^{\circledR}$ and Nicotinell $TTS^{\circledR}$, the steady-state plasma concentration of nicotine and ACU for 24 hrs were 428.9 ng/ml, $9,121\;ng{\cdot}hr/ml$ and 155.3 ng/ml, $3,152\;ng{\cdot}h/ml$, respectively. NP showed the experimental plasma nicotine concentration profile was very similar to the simulated one and had an appropriate skin permeation rate and a steady-state concentration of nicotine, which can show therapeutic blood levels of the drug for 24 hrs without severe side effects.

• Journal of the Korean Applied Science and Technology
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• v.28 no.2
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• pp.170-177
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• 2011

Transdermal drug delivery(TDS) offers many important advantages. For instance, it is easy and painless, it protects the active compound from gastric enzymes, and it avoids the hepatic first-pass effect. Also, it is simple to terminate the therapy if any adverse or undesired effect occurs. But skin is a natural barrier, and only a few drugs can penetrate the skin easily and in sufficient quantities to be effective. Therefore, in recent years, numerous studies have been conducted in the area of penetration enhancement. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharide, such as xanthan gum and algin were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers and drug contents. Among these polysaccharide, the permeation rate of Paroxetine such as lipophilic drug was the fastest in xanthan gum matrix in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. 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.

• Journal of the Korean Applied Science and Technology
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• v.27 no.4
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• pp.407-414
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• 2010

New biological treatments were being developed at a record place, but their potential could be compromised by a significant obstacle: the delivery of these drugs into a body. Pharmaceutical delivery is now nearly as important as product. New systems are being developed, and Drug Delivery Markets Series cover these new systems. Transdermal Delivery System(TDS) is often used as a method of drug dosage into the epidermic skin. An approach used to delivery drugs through the skin for therapeutic use as an alternative to oral, intravascular, subcutaneous and transmucosal routes. Various transdermal drug delivery technologies are described including the use of suitable formulations, carriers and penetration enhancers. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other methods of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharides, such as karaya gum and glucomannan, were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, drug contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in fibric acid(ciprofibrate) such as lipophilic drug in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. 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. Especially, this result suggests a possible use of polysaccharide gel ointment matrix as a transdermal delivery system of anti-hyperlipoproteinemic agent.