• Journal of Pharmaceutical Investigation
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• v.36 no.2
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• pp.97-102
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• 2006

The aim of this study was to investigate the feasibility and optimize permeability of slim patch type as a transdermal delivery system of caffein. Slim patch type was formulated and tested in modified Franz diffusion cell across cellulose membrane and hairless mouse skin in pH 5.8 phosphate buffer solution (PBS). The effect of $Pharmsolv^{\circledR}$ and drug concentration on permeation at four model, 1,2% $Pharmsolv^{\circledR}$ with $0.12\;mg/cm^2$ caffein and 0.12, $1.2\;mg/cm^2$ caffein with 2% $Pharmsolv^{\circledR}$ through hairless mouse skin was studied in vitro. The release of caffein from slim patch with various loading was fitted by the Higuchi's diffusion equation. The result showed that chemical $Pharmsolv^{\circledR}$ produced a large and significant increase of permeation. The effect of 2% $Pharmsolv^{\circledR}$ on permeation of caffein was greater about 10-fold greater than 1% $Pharmsolv^{\circledR}$ in first 60 minutes. The effect of drug concentration, however, was lower than that produced by chemical $Pharmsolv^{\circledR}$. Within the tested system, the most efficient combination for caffein slim patch type was $0.12\;mg/cm^2$ caffein with 2% $Pharmsolv^{\circledR},$ although $1.2\;mg/cm^2$ caffein with 2% $Pharmsolv^{\circledR}$ showed highest amounts permeation, because permeated percentages were significantly lower about $1/4{\sim}1/5$ times.

• Journal of Pharmaceutical Investigation
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• v.35 no.3
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• pp.173-177
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• 2005

Addition of 30% propylene glycol was required to maintain sink condition in the evaluation of percutaneous absorption of estradiol and norethindrone acetate. The permeability of estradiol was higher in silicone and SIS adhesives. However, estradiol was crystallized in silicone, SIS, and SBS adhesive matrix. The permeability ratio of estradiol or norethindrone acetate from acrylic pressure sensitive adhesives varied widely depending on the functional group of the acrylic adhesives. PEO grafting to acrylic adhesive seemed to change physicochemical property of acrylic adhesive and increased the permeability of estradiol and norethindrone acetate significantly. On the contrary, highly cross-linked enhancer compatible acrylic adhesive decreased the permeability of both estradiol and norethindrone acetate. $Span^{\circledR}$ 20 provided the highest enhancing effect on the permeability of both estradiol and norethindrone acetate followed by oleic acid and $Crovol^{\circledR}$ EP40. The permeability of the drugs from the developed system was comparable to that from commercial $Combitran^{\circledR}$, although significantly lower amount of estradiol and norethindrone acetate were loaded in the developed system.

• 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.41 no.1
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• pp.1-7
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• 2011

The effects of different formulation variables including pressure sensitive adhesive (PSA), permeation enhancer, thickness of the matrix and loading amount of drug on the transdermal absorption of galantamine were investigated across the hairless mouse skin. The permeation profile of galantamine was different depending on the types of PSA, loading amount of drug, thickness of the matrix and type of enhancer used. Highest flux of galantamine was obtained from acrylic PSA but crystals were formed in the patch within 72 h. Among the PSAs screened, crystal formation was not observed only in the patches formulated in Styrene Butadiene Styrene (SBS) matrix. Permeation rate increased linearly as the concentration of galantamine in SBS matrix increased from 2.5 to 15% w/w. Among the enhancers screened, Brij$^{(R)}$ 30 provided highest flux of galantamine. Matrix thickness of 80 ${\mu}m$ was optimum for maintaining adhesiveness as well as consistently delivering galantamine for longer period of time.

• Journal of Pharmaceutical Investigation
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• v.39 no.1
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• pp.19-21
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• 2009

This study was performed to examine the possibility of increasing the level of furosemide permeation from the ethylene-vinyl acetate (EVA) matrix through the skin by incorporating various enhancers in the EVA matrix. The effects of the enhancers on the level of furosemide permeation through the skin were evaluated using Franz diffusion cells with intact excised rat skins. The enhancers examined were the fatty acids (saturated, unsaturated), the pyrrolidones, the propylene glycol derivatives, the glycerides and the non-ionic surfactants. Among the enhancers used, polyoxyethylene-2-oleyl ether (a non-ionic surfactant) showed the best enhancement. The polyoxyethylene 2-oleyl ether as a permeation enhancer could be used for development of furosemide-EVA transdermal matrix system.

• Journal of Pharmaceutical Investigation
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• v.28 no.1
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• pp.43-50
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• 1998

Niosomes are vesicles formed from synthetic non-ionic surfactants, offering an alternative to chemically unstable and expensive liposomes as a drug carrier. Non-ionic surfactant and cholesterol mixture film leads to the formation of vesicular system by hydration with sonication method. The formation of niosome was ascertained by negative staining of TEM. The entrapment efficiency of niosomal suspension was gradually increased with increasing the ratio of cholesterol to surfactant. It was found that the niosome with 6 : 4 (polyoxyethylene 2-cetyl ether: cholesterol) ratio was more stable than those with other ratios. The topical application of acyclovir(ACV) in the treatment of herpes simplex virus type 1(HSV-1) skin disease has a long history. There are an increasing number of reports, however, in which topical ACV therapy is not as effective as oral administration. Lack of efficacy with topical ACV has been hypothesized to reflect the inadequate delivery of drug to the skin. We investigated the permeation of niosome containing $[^{3}H]ACV$ in hairless mouse skin using Franz diffusion cell model. Permeation coefficient(P) of aqueous ACV was $6.7{\times}10^{-4}\;(cm/hr)$ and that of ACV in niosome was $23.4{\times}10^{-4}\;(cm/hr)$, suggesting about 3.5 times increase in the transdermal permeation.

• Journal of Pharmaceutical Investigation
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• v.30 no.4
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• pp.283-288
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• 2000

The purpose of the present study was to investigate the topical bioavailability of retinol (vitamin A) after its transdermal administration. For this purpose, we developed the convenient HPLC method to measure the retinol concentration in the biological fluids such as plasma and skin tissues. The low detection limit was $0.1\;{\mu}g/ml$ using a gradient HPLC system of UV detection. The initial plasma concentration of retinol was about $20\;{\mu}g/ml$ after its i.v. bolus administration (4.32 mg/kg). The half life $(t_{1/2{\alpha}})$ in the distributive phase was 1.3 min, while retinol was slowly disappeared in the post-distributive phase. On the other hand, the maximum plasma concentration $(C_{max})$ was about 776 ng/ml after appling to rat skin at a dose of 43.2 mg/kg. Furthermore, the concentration of retinol in the skin tissues was about 600 ng/g tissue at 12 hr after its transdermal administration. In conclusion, the initial plasma concentration of retinol was comparable with the skin concentration after its cutaneous absorption, followed by being decreased with the passage of the time.

• Polymer(Korea)
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• v.33 no.3
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• pp.237-242
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• 2009

This study examined the transdermal delivery of alendronate across hairless mouse skin. The effects of iontophoresis, perforation with a microneedle, and a combination of a microneedle pretreatment and iontophoresis were evaluated in vitro test. Hydrogel patches were polymerized by UN polymerization to supply a hydrogel patch to the iontophoretic transdermal drug delivery system. The alendronate content in the iontophoretic delivery patch was $5.0\;mg/cm^3$. The amounts of alendronate that permeated across the hairless mouse skin when current densities of 0.25 and $0.50\;mA/cm^2$ were supplied to the iontophoretic alendronate patch were $0.80{\pm}0.03$ and $2.00{\pm}0.02{\mu}g$, respectively. After pretreatment with a microneedle, the amounts of alendronate that permeated across the hairless mouse skin increased to $70.65{\pm}0.37$ and $162.23{\pm}0.40{\mu}g$, respectively. The biocompatibility of the iontophoretic alendronate patch was examined according to the international standardization organization 10993.

• Journal of Pharmaceutical Investigation
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• v.34 no.6
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• pp.491-497
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• 2004

We investigated some important factors which affect the transdermal flux of ketoprofen, a nonsteroidal anti-inflammatory agent, as a first step to provide some basic knowledge for the development of a iontophoretic transdermal patch system. Factors such as current density, polarity, buffer (HEPES) and electrolyte concentration and pH were studied using hairless mouse skin. The effect of poly(L-lysin), which is known to affect the electro-osmotic flow through skin, on flux was also studied. Passive flux was about $20\;{\mu}g/cm^2hr$ at pH 4.0, but was negligible at pH 7.4 where all ketoprofen molecules dissolved are ionized (ketoprofen pKa=5.94). At pH 4.0, application of anodal current increased the flux further above the passive level, however anodal flux at pH 7.4 was much smaller than passive flux at pH 4.0. The application of cathodal current at pH 4.0 increased the average flux to $30-40\;{\mu}g/cm^2hr$, depending on the current density applied. At pH 7.4, cathodal flux was only about $5\;{\mu}g/cm^2hr$. Decrease in buffer and electrolyte concentration increased this cathodal flux about 10 fold. However decrease in HEPES buffer concentration 100 fold did not affect the flux. Anodal flux of acetaminophen was much larger than cathodal flux, indicating that electroosmotic flow can be playing an important role in the flux. Poly(L-lysin) increased the cathodal flux at pH 7.4. These results provide some important insights into the mechanism of transdermal flux of ketoprofen and the role of electroosmotic flow.

• Proceedings of the PSK Conference
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• 2000.10a
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• pp.261.1-261.1
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• 2000