• 문화기술의 융합
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• 제7권4호
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• pp.683-691
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• 2021

본 연구의 목적은 온도조건 별로 밀도요동 초임계 유체를 이용하여 추출한 대마종자 추출물의 수율 측정과 생리활성능을 평가하고, 리포좀 제형으로 난용성 추출물의 용해를 가능하게 하여 경피투과도를 증진시키는 데 있다. 수율 측정 결과, 60℃로 추출한 대마종자가 가장 높게 나타났고, 항산화 실험에서 total polyphenol content assay, DPPH radical scavenging assay, ABTS+ radical scavenging assay 결과, 최고농도에서 45℃ 추출물의 폴리페놀 함량과 radical 소거능이 가장 크게 나타났다. 항균실험 결과, P ropionibacteium acnes 균주에서만 clear zone이 나타났다. 추출물을 3차 정제수에 용해시킨 제형보다 리포좀으로 캡슐화한 제형에서 particle size의 감소와 zeta potential의 절댓값 증가를 확인하여 제형 안정성을 확인하였고, 경피투과도의 증진 또한 확인하였다. 이러한 실험결과를 바탕으로 난용성인 초임계 대마종자 추출물을 화장품의 기능성 천연물 소재로써 활용 가능성을 확인하였다.

• Journal of Pharmaceutical Investigation
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• 제33권3호
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• pp.163-169
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• 2003

In order to develop a film-forming transdermal drug delivery system, polyurethane (PU) based on poly(ethylene glycol) and poly(tetramethylene oxide) was synthesized and characterized. The synthesized PU was blended with Gantrez ES 225 (GT) to improve the adhesion property of film-forming agent to the skin. When film-forming gel formulation containing 3% ketoprofen (KP) was applied, transparent thin film was obtained within 5 minutes and adhered to the skin for 8 hours. In vitro percutaneous absortion studies were performed to determine the rate of ketoprofen absorption through guinea pig skin. A prominent effect of limonene on the skin permeability of ketoprofen was observed among the various skin permeation enhancers investigated. Considering mechanica properties of film and skin permeability of ketoprofen, 2% of limonene was optimal content in the film forming transdermal formulation.

• Journal of Pharmaceutical Investigation
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• 제39권3호
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• pp.177-183
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• 2009

A rapid and sensitive reversed-phase high performance liquid chromatography (HPLC) method was developed for the determination of piroxicam in the rabbit plasma. After a treatment of plasma sample by liquid-liquid extraction, the drug was analyzed on an HPLC system with ultraviolet detection at 330 nm. HPLC was carried out using reversed-phase isocratic elution with a C18 column, a mobile phase of a mixture of acetonitril, doubly deionized water and acetic acid 43.74:56.00:0.26 v/v%) at a flow rate of 1.1 mL/min. The chromatograms showed good resolution and sensitivity and no interference of plasma. The calibration curve for the drug in plasma sample was linear over the concentration range of 0.01-2.0 ${\mu}$g/mL. The intra- and inter-day assay accuracies of this method ranged from 86.82% to 108.33% of normal values and the precision did not exceed 13% of relative standard deviation. The plasma concentration of piroxicam decreased to below the quantifiable limit at 12 hr after the i.v. bolus administration to rabbits following dose of 0.375 mg/kg yielding a apparen t plasma half life of 1.38 hr. The transdermal route prolongs plasma levels of piroxicam. The bioavailability, calculated from the dose-adjusted ratio of the $AUC_{transdermal}$ to the $AUC_{i.v.}$, was 7.44%. The plasma concentration of piroxicam was detected by 48 hr after the transdermal administration of patch at a dose of 32 mg/kg. This method was suitable for cutaneous absorption studies of piroxicam in the rabbit after transdermal administration of different types of dosages of the drug.

• Journal of Pharmaceutical Investigation
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• 제33권1호
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• pp.21-28
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• 2003

Ketorolac tromethamine(KT) is a nonsteroidal agent with potent analgesic and moderate anti-inflammatory activity. The lipid-water partition coefficient of KT was evaluated and KT gel was formulated as a gel containing different pH, different concentrations of polymer (poloxamer 407, carbopol 941), propylene glycol, ethanol and various enhancers. The resulting KT gels were evaluated with respect to their viscosity, in vitro drug permeation rate through hairless mouse skin and stability. In n-octanol and chloroform, the lipid-water partition coefficient of KT was the highest at pH 4 phosphate buffer. The apparent viscosity of KT gel increased with an increase in gel pH, polymer and enhancer concentration. But the apparent viscosity of KT gel decreased with an increase in ethanol concentration. The permeation rate of KT through hairless mouse skin from gels different pH was maximum at pH 4 which is close to KT $pK_{a}$ 3.54. The permeation rate decreased with an increase in polymer, propylene glycol concentration. But the permeation rate increased with an increase in ethanol. The increase of drug concentration from 1 to 3% induced linear increase in permeation rate. The best enhancer was the combination of $Labrasol^{\circledR},\;Transcutol^{\circledR}$, oleic acid and l-menthol. In the accelerated stability test(25, 40 and $50{\circ}C$), pH 5 gel was most stable and pH 4 gel was most unstable for 90 days.

• Journal of Pharmaceutical Investigation
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• 제37권3호
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• pp.149-158
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• 2007

To investigate the permeability of lidocaine, percutaneous absorption studies were performed using excised hairless mouse skin and the penetration of lidocaine via the skin was determined. To increase the skin permeation of lidocine, the effects of $Labrasol^{(R)}$, $Labrafil^{(R)}$, $Labrafac^{(R)}$ and $Transcutol^{(R)}$ were investigated. The skin permeation of lidocaine was increased when $Labrasol^{(R)}$ and $Transcutol^{(R)}$ were used as permeation enhancer. To evaluate the influence of ultrasound, various factors such as application modes (continuous mode and pulsed mode), frequency (1.0 and 3.0 MHz) and intensity (1.0, 1.5 and 2.0 w/$cm^2$) were investigated with lidocaine hydrogel. The pronounced effect of ultrasound on the skin permeation of lidocaine was observed at all ultrasound energy levels. The influence of frequency having an effect on skin permeation rate was higher in the case of using 1 MHz, 2.0 w/$cm^2$ and continuous treatment. As the intensity of ultrasound increased, the permeation of lidocaine was accelerated. The in vivo anesthetic effects were evaluated by two aspects as mechanical threshold and electrical threshold. Six healthy volunteers consented to the randomized, double-blind, and cross-over designed study in each group. In each subject, 3 groups were adapted such as K group (ultrasound with gel base only), L group (lidocaine gel) and B group (ultrasound with lidocaine gel). In conclusion, lidocaine was potent anesthetic which could be block pain threshold effectively. And ultrasound could accelerate the skin penetration of lidocaine. The phonophoretic delivery system could be a good candidate for lidocaine as a local anaesthetic to improve the skin permeation and in vivo anaesthetic effect.

• Journal of Pharmaceutical Investigation
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• 제35권6호
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• pp.403-409
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• 2005

For transdermal delivery of large molecular drugs such as vaccine and protein drugs, novel microneedle treatment device with roll was designed. The roll dimension is 1.43 cm diameter and 2.8 cm perimeter. Total number of microneedle on the roll is 3,360 with $230\;{\mu}m$ height and $740\;{\mu}m$ distance. The pore with $150\;{\mu}m$ depth and $35\;{\mu}m$ diameter on the skin was made by the designed microneedle device. This system could be achieved without pain. The permeation rates of FITC labelled ovalbumin (FITC-OVA, molecular weight: 45,000 g/mol) as a model protein were determined by modified Franz diffusion cells using skins of hairless mice or SD rats which were treated by using microneedle device two or four times. The average penetration fluxes of model protein increased from 674 to $872\;{\mu}g/cm^{2}{\cdot}hr$ as the number of treatment to make pore increased from two to four times. In conclusion, we confirmed the possibility of using the designed microneedle treatment device for transdermal delivery of the large molecular drugs.

• Journal of Pharmaceutical Investigation
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• 제36권2호
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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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• 제29권2호
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• pp.111-115
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• 1999

We have studied the transdermal flux of prostaglandin $E_1$ $(PGE_1)$ from a hydrogel patch through hairless mouse skin, to test the possibility of developing a transdermal delivery system. Karaya gum patch containing $PGE_1$ was prepared by casting method. $PGE_1$ was stable in the patch for 10 weeks. The effect of current application, enhancer (propylene glycol monolaurate : PGML), adhesive and patch thickness on the flux was studied using side-by-side diffusion cell. Passive flux of $PGE_1$ was negligible. Cathodal delivery increased the flux about 20 fold. As the concentrations of PGML increased, flux increased. When 5% PGML was used as the enhancer, maximum flux by cathodal iontophoresis was $55\;{\mu}g/cm^2\;hr$. It increased about 2 folds to $100\;{\mu}g/cm^2\;hr$, when the amount of PGML used was 9%. Large increase in flux and the decrease in time to reach maximum flux were observed when the skin was pretreated with neat PGML (maximum flux obtained was about $200\;{\mu}g/cm^2\;hr$). Use of adhesive decreased the flux significantly. To the contrary of our expectation, increase in current density decreased the flux. These flux data together with the stability data indicate that, though the onset of sufficient delivery occur after 1-2 hours of application, therapeutic amount of $PGE_1$ can be delivered through skin using iontophoresis and penetration enhancer.

• 대한화장품학회지
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• 제42권1호
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• pp.29-35
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• 2016

본 연구에서는 미백제인 RS White를 함유한 O/W 나노에멀젼의 형성 가능성을 유화제 종류별로 실험하였다. 친수성계면활성제로 Tween 80, 60, HCO 60 및 40과 친유성 계면활성제로 Span 80을 사용한 시스템에서는 적정한 농도에서 나노에멀젼이 형성되었으나 Myrj 52, Montanov L 및 Tegocare 450과 Span 80을 사용한 시스템에서는 형성되지 않았다. 형성된 나노에멀젼은 입자의 직경이 100 nm 미만의 반투명 외관을 보였으며 시간 경과에 따른 안정성 평가에서도 안정성을 유지하였다. 이들의 경피흡수 정도를 마크로에멀젼과 비교한 결과 24 h 동안 피부 투과량은 나노에멀젼은 $70.84{\mu}g/cm^2$, O/W 마크로에멀젼은 $28.97{\mu}g/cm^2$으로 나타났다. 따라서, 본 연구는 RS White 미백제를 함유한 안정한 나노에멀젼이 기능성 소재의 효율적인 피부 전달체로서 응용 가능성이 있음을 시사한다.

• KSBB Journal
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• 제28권5호
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• pp.319-326
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• 2013

This study was carried out to investigate the in vitro and in vivo moisturizing properties and percutaneous absorption of PEG-impregnated Aloe vera gel. The PEG-i-Aloe gel was obtained from dewatering and impregnation by soaking (DIS) of Aloe vera leaf slice. The moisturizing property of the obtained sample was evaluated by moisture determination using gravimetric method in desiccator under different RH% and by water sorption-desorption test on human skin. The transdermal penetration characteristics of PEG-i-Aloe gel was investigated by Franz diffusion cell in vitro transdermal absorption method. PEG-i-Aloe gel had high moisture retention ability and could significantly lead the enhancing skin hydration status as well as reducing the skin water loss due to the film formation as a skin barrier. The skin penetration rate of PEGi- Aloe gel at steady state was 9.76 ${\mu}g/(h{\cdot}cm^2)$ and the quantity of the transdermal absorption was 144 ${\mu}g/cm^2$ in 9 hr. The penetration mechanism was well fitted with Higuchi model ($R^2$ = 0.974-0.994). The results show that PEG-i-Aloe gel has the significant moisturizing effect and strong penetration of the animal skin. It could be used as the moisturizing additive in cosmetic skin products.