• Archives of Pharmacal Research
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• v.14 no.1
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• pp.12-18
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• 1991

The effect of urea and urea derivatives on the percutaneous absorption of salicylic acid and sodium salicylate through the skin of rabbit from petrolatum ointment was investigated. It was found that addition of urea or urea derivatives to the ointment base significantly increased the percutaneous absorption of the drugs in proportion to the concentratoin of the additive. The percutaneous absorptoin-enhancing activities of these compounds were that urea derivatives with the more and longer alkyl substituents showed the stronger activities. These activities of urea and urea derivatives were ascribed to the binding of these compounds with the lipids and proteins of the stratum corneum of the skin and the swelling of the tissues, which leads to the reduction of the barrier property of the layer. The preliminary skin irritation test showed that urea and urea derivatives were quite non-irritating to the skin. These results suggest that urea derivatives have a strong possibility to be developed as a percutaneous absorption enhancer.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.27 no.1
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• pp.29-42
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• 2001

We had prepared MLV liposome with Hibiscus Esculentus Ext.(HEE) which have fluorescent light in order to evaluate its percutaneous absorption about hairless rat skin. Then we investigated particle size of MLV using confocal laser scanning microscope(CLSM) and transmission electron microscope(TEM), respectively. Stability of MLV liposome and penetration of MLV liposome to hairless rat skin was measured by CLSM. As a result of experiments, MLV was globular shape and the rage of particle size was 0.3-0.5$\mu\textrm{m}$ mostly. Cream-type MLV had high stability comparatively. When we treated with MLV to rat skin, skin penetration was enhanced, especially, the optimum concentration of MLV on penetration to rat skin was 10%. Optimum penetration time was 6hr-12hr. And MLV-type HEE was more effective on percutaneous absorption than HEE-cream or liposome-type HEE.

• Journal of Pharmaceutical Investigation
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• v.34 no.2
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• pp.107-114
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• 2004

External lyogels containing prostaglandin $E_1$ ethyl ester $(PGE_1-EE)$, a prodrug of prostaglandin $E_1\;(PGE_1)$ as a therapeutic agent for erectile dysfunction, were formulated to overcome the aqueous instability and enhance the percutaneous absorption. Lyogels of $PGE_1-EE$ were prepared with ethanol (EtOH)/proplyene glycol (PG) cosolvent system as a vehicle, cineol as an enhancer, and hydroxypropylcellusose as a gelling agent. In vitro percutaneous absorption studies were performed to determine the rate of $PGE_1$ absorption through rat or hairless mouse skin. The permeability of $PGE_1-EE$ lyogel with enhancer was 16-fold greater than that of lyogel without enhancer. Cosolvent produced 9-fold increase in percutaneous absorption. Pharmacodynamic effects of lyogels were evaluated in mature male cats in terms of intracavernosal pressure (ICP). Lyogels containing 0.1 % of $PGE_1-EE$ showed higher ICP compared to intraurethral preparation of $PGE_1$ (1 %) and enhancer-free control lyogel. The shelf-life $(t_{10%})$ of lyogel at refrigerated condition $(4^{\circ}C)$ was calculated as 928 days, which is 4.2 times longer than that of control hydrogel. As a result, $PGE_1-EE$ was formulated successfully to a lyogel system with a selective enhancer and cosolvent system for the topical delivery of $PGE_1$.

• Archives of Pharmacal Research
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• v.21 no.5
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• pp.503-507
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• 1998

Percutaneous absorption and model membrane variations of melationin (MT) in aqueous-based propylene glycol and $2-hydroxypropyl-{\beta}-cyclodextrin $vehicles were investigatted. the excised hairless mouse skin (HMS) and two synthetic ethylene vinyl acetate (EVA) and microporous polyethylene (MPE) were selected as a model membrane. the solubility of MT was determined by phase equilibrium study. the vertical $Franz{\circledR}$ type cell was used for diffusion study. The concentration of MT was determined using reverse phse HPLC system. The MT solubility was the highest in a mixture of PG and $2-HP{\beta}CD$. The percutaneous absorption of MT through excised HMS increased as the solubility increased. However, the permeability coefficient decreased and then slightly increased in mixture of PG and $2-HP{\beta}CD$. On the other hand, both flux and permeability coefficient through EVA membrane decreased as the solubility increased. No MT was detected over 12 h after starting diffusion through MPE membrane. The flux of MT was dependent on the type of membrane selected. Flux of MT was greatest in excised HMS followed by EBA and MPE membrane. Flux of MT through EVA membrane was 5-20 times lower when compared to excised HMS. Interestingly, volumes of donor phase when MPE membrane was used, significantly increased during the study period. the HMS might be applicable to expect plasma concentration of MT in human subjects based on flux and pharmacokinetic parameters as studied previously. the current studies may be applied to deliver MT transdermally using aqueous-based vehicles and to fabricate MT dosage forms.

• Journal of the Korean Applied Science and Technology
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• v.25 no.2
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• pp.137-143
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• 2008

Chemicals for cosmetics, including skin, the skin absorbs some of the research in the field of science or pharmacy recently, about the environment and the health of the heightened interest in skin absorption, and many other human attributes and absorption evaluation studies are underway in various areas. In this study, The effects of commercial permanent wave products to skin which are composed with cysteine and bases using rat. Results are as follows; the content of penetration 4 hours later with steady state and no significant changeable after 20 hours later. In cysteine groups lag time and permeability coefficient of young skin is 3.32hr and $0.102{\mu}g/cm^2{\cdot}hr$, lag time and permeability coefficient of old skin is 4.04hr and $0.106{\mu}g/cm^2{\cdot}hr$. In conclusion of study lag time and permeability coefficient in old skin and wounded skin are faster than healthy skin. We notified that fine rinkle and rash of skin were changeable in the case of treating with permanent wave drugs than normal skin.

• Journal of Pharmaceutical Investigation
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• v.37 no.3
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• pp.173-177
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• 2007

The purpose of this study was to investigate the effect of salt formation on the percutaneous absorption of meloxicam through hairless mouse skin from a pressure sensitive adhesive (PSA) matrix. In addition, the influences of enhancers on the permeation of meloxicam or meloxicam-ethanolamine (MX-EA) salts across the hairless mouse skin were evaluated using a flow-through diffusion cell system. The salt formation of meloxicam resulted in lower permeation rate than the parent drug. $Span^{(R)}$ 80 provided the highest enhancing effect for meloxicam and meloxicam monoethanolamine salt. The maximum amount of the drug that can be loaded without retarding permeation rate was different depending on the compound. No relationship was found between the fluxes of meloxicam or MX-EA salts from saturated solutions and those from PSA matrices containing the same enhancer.

• Journal of Pharmaceutical Investigation
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• v.33 no.2
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• pp.79-84
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• 2003

The effects of various pressure sensitive adhesives (PSA) and enhancers on the percutaneous absorption of tulobuterol were investigated. The permeation rate of tulobuterol through hairless mouse skin from various adhesives was evaluated using a flow-through diffusion cell system at $37^{\circ}C$. The permeability of tulobuterol was variable depending on the physicochemical property of the PSA. The permeation rate of tulobuterol from polyethylene oxide grafted acrylic adhesive matrix was higher than that from other PSA matrices. The flux of tulobuterol was $4.37{\pm}0.34\;{\mu}g/hr/cm^2$ from polyethylene oxide grafted acrylic adhesive matrix. When the effects of various enhancers on the percutaneous absorption of tulobuterol from grafted acrylic adhesive were evaluated, Plurol $oleique^{\circledR}$ showed higher flux than all other enhancers tested.

• Archives of Pharmacal Research
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• v.27 no.3
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• pp.351-356
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• 2004

A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol: ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.129-129
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• 1995

ASPS against TGF-${\beta}$ is developing as scar formation inhibitor. The scar was caused by undesired collagen deposition due to overexpression of TGF-${\beta}$ in wounded tissue. The in vitro percutaneous absorption of ASPS(25mer)was investigated by using Furanz Diffusion Cell. The flux of ASPS cannot be found through normal skin due to high molecular weight (MW 10,000) and polyanionic charge. However, the skin permeation of ASPS through tape-stripped damaged skin was markedly increased. The skin fluxs of ASPS were decreased in the following order; hairless mouse> rat >human cadaver skin.

• Journal of Pharmaceutical Investigation
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• v.33 no.2
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• pp.129-133
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• 2003

In order to evaluate the effects of vehicles and penetration enhancers on skin permeation of apomorphine, the skin permeation rates of apomorphine from vehicles of different composition were determined using Franz diffusion cells fitted with excised rat skins. Solubility of apomorphine in various solvents was investigated to select a vehicle suitable for the percutaneous absorption of apomorphine. The solvents used were propylene glycol (PG), $Transcutol^{\circledR},\;Labrasol^{\circledR},\;Labrafac hydro WL^{\circledR},\;Labrafil WL 2609 BS^{\circledR}$ and isopropyl alcohol. Even though permeation rates of apomorphine from each vehicle were low $(0.008-0.36\;{\mu}g/cm^2/hr)$, the combination of PG and $Labrafac^{\circledR}$ increased it significantly. The permeation rates of apomorphine from $PG/Labrafac^{\circledR}$ mixtures increased as the volume fraction of PG in the mixture increased. The maximum permeation rate of $18\;{\mu}g/cm^2/hr$ was achieved at 30% of PG, which decreased with further increase of PG fraction. A series of fatty acids, alcohols and monoterpenes were employed as penetration enhancers. Incorporation of each enhancer in the $PG/Labrafac^{\circledR}$ (30:70) mixture at the level of 10% improved the skin permeation significantly. The highest permeation rate, $117\;{\mu}g/cm^2/hr$, was attained with myristic acid.