• Translational and Clinical Pharmacology
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• 제25권1호
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• pp.15-20
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• 2017

This study was performed to evaluate the use of vibrating microneedles for the transdermal delivery of vitamin C. The microneedles were designed to vibrate at three levels of intensity. In vitro permeation by vitamin C was evaluated according to the specific conditions such as vibration intensity (levels 1, 2 and 3), application time (1, 3, 5, 7 and 10 min), and application power (500, 700 and 1,000 g). The highest permeation of vitamin C was observed at level 3 of vibration intensity, 5 min of application, and 1,000 g of application power. Vitamin C gel showed no cytotoxic effect against Pam212 cells or skin irritation effects. A pharmacokinetic study of the gel in rats was conducted under optimized conditions. The $AUC_{0-{\infty}}$ and $C_{max}$ increased 1.35-fold and 1.44-fold, respectively, compared with those after vitamin C gel without application with vibrating microneedles. The present study suggests that vibrating microneedles can be used to facilitate the skin permeability of vitamin C under optimal conditions.

• Biomolecules & Therapeutics
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• 제22권1호
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• pp.73-77
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• 2014

The purpose of this study was to examine the effect of stabilization of retinyl palmitate (RP) on its skin permeation and distribution profiles. Skin permeation and distribution study were performed using Franz diffusion cells along with rat dorsal skin, and the effect of drug concentration and the addition of pectin on skin deposition profiles of RP was observed. The skin distribution of RP increased in a concentration dependent manner and the formulations containing 0.5 and 1 mg of pectin demonstrated significantly increased RP distributions in the epidermis. Furthermore, it was found that skin distribution of RP could be further improved by combined use of pectin and ascorbyl palmitate (AP), due largely to their anti-oxidative effect. These results clearly demonstrate that the skin deposition properties of RP can be improved by stabilizing RP with pectin. Therefore, it is strongly suggested that pectin could be used in the pharmaceutical and cosmetic formulations as an efficient stabilizing agent and as skin penetration modulator.

• 한국미생물·생명공학회지
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• 제41권3호
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• pp.320-326
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• 2013

이전 연구에서 저자들은 담쟁이덩굴 줄기 추출물의 항산화 및 세포 보호 효과를 연구하였다. 본 연구에서는 우수한 활성을 갖는 담쟁이덩굴 줄기 추출물의 피부흡수를 증진시키고자 이를 함유한 나노에멀젼을 제조하고 물리적 특성 및 피부흡수능을 평가하였다. 고압유화기(microfluidizer)를 이용하여 제조한 나노에멀젼은 평균 입자 크기가 302 nm를 나타내었으며 포집 효율은 86% 이상으로 나타났다. 나노에멀젼은 단분산의 입도 분포를 나타내었고 고압유화과정을 거치지 않은 일반 에멀젼보다 2주간 높은 안정성을 나타내었다. Franz diffusion cell을 이용하여 제조된 담쟁이덩굴 추출물 함유 나노에멀젼의 피부흡수능을 평가하였다. 그 결과 대조군으로 사용된 1,3-butylene glycol 용액이 32.59%의 피부흡수율을 나타내었고, 나노에멀젼은 42.47%의 피부 흡수능을 나타내었다. 또한 담쟁이덩굴 줄기 추출물의 화장품에 있어 천연 항균제로써의 응용 가능성을 연구하고자 에틸아세테이트 분획의 피부 상재균에 대한 항균작용을 측정하였다. 항균활성 측정결과 담쟁이덩굴 줄기 추출물은 Staphylococcus aureus, Bacillus subtilis에 대해 항균활성을 나타내었으며, 화장품에 주로 사용되는 항균제인 methyl paraben 보다 높은 항균활성을 가지고 있음을 확인하였다. 이상의 결과들은 담쟁이덩굴 줄기 추출물을 함유한 나노에멀젼이 피부흡수능 증진을 통해 향후 화장품 제형으로서 이용가능성이 큼을 시사한다. 또한 담쟁이덩굴 줄기 에틸아세테이트 분획의 Gram (+) 세균에 대한 항균활성을 바탕으로 이전 연구에서 밝혀진 항산화 활성 및 세포보호효과와 더불어 기능성원료로서 응용 가능성이 큼을 시사한다.

• Macromolecular Research
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• 제17권12호
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• pp.969-975
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• 2009

This article describes the topical delivery and localization of budesonide through the hairless mouse skin. Two poly(ethylene oxide)-block-poly($\varepsilon$-caprolactone)-block-poly(ethylene oxide) (PEO-PCL-PEO) triblock copolymers (T 222 and T 252) having different CL:EO ratios were added in the preparation of budesonide particles stabilized with poly(vinyl alcohol) (PVA) and Tween 80 under ultrasonication. For comparison, a commercial PEO-PPO-PEO triblock copolymer (F68) was studied under the same condition. To demonstrate the effects of the triblock copolymer, the particle size of budesonide emulsion, entrapment efficiency, and in vitro release were measured and compared. The budesonide particles stabilized by the triblock copolymers had a diameter of ca. 350 nm with entrapment efficiencies of 66-76%. The In vitro release profiles of all samples showed an initial burst followed by sustained release. The skin penetration and permeation of budesonide were analyzed by using a Frantz diffusion cell. T 222 and T 252 exhibited higher total permeation amounts, but lower budesonide penetration amounts, than F68. The results suggest that the partitioning of budesonide in each skin layer can be adjusted in order to avoid skin thinning and negative immune response arising from the penetration of budesonide in blood vessels.

• 한국환경보건학회지
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• 제42권1호
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• pp.61-70
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• 2016

Objectives: The purpose of this study is to determine the exposure risk to tattoo components by analyzing skin absorption using the in vitro method. Tattoos are commonly used for cosmetic purposes, and the skin of not only the operator but of the people who are undergoing the cosmetic procedure is continuously exposed to hazardous chemicals. Methods: Skin permeation risk determination was conducted by the in vitro Franz diffusion cell method according to the ingredient types of tattoo dyes, such as volatile organic compounds (VOCs), non-volatile organic compounds and heavy metals, using hairless mouse full skin and human cadaver epidermis. Results: The major components with good skin penetration for each type of tattoo dye ingredient were clarified. Among the tatto dye ingredients, 1,2-Dichlorobenzene, Zn, Al, Pb and Ti showed good skin penetration. Most of the skin transmission rates were higher in hairless mouse full skin than in human cadaver epidermis. Conclusion: A possible exposure risk to hazardous substances in tattoo dyes was confirmed from this study. These results are expected to provide a positive contribution to the establishment of management regulations for tattoo dyes.

• Journal of Pharmaceutical Investigation
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• 제37권6호
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• pp.365-368
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• 2007

The primary aim of this study was to investigate the enhancement effect of low-frequency ultrasound on skin permeation. In vitro permeation experiments were performed using Franz modified diffusion cells with ketoprofen as model drug. The effect of various ultrasound factors-ultrasound application mode (continuous mode and discontinuous mode), ultrasound intensity (0.26 $W/cm^2$, and 0.29 $W/cm^2$) and duty cycle (3%, 16%, 50%, and 83%) were studied. The highest permeation was observed at 0.29 $W/cm^2$ intensity, 50% duty cycle, and discontinuous mode. The result suggested the feasibility of low frequency ultrasound application for the phonophoretic transdermal drug delivery system.

• 대한화장품학회지
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• 제41권4호
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• pp.315-324
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• 2015

본 논문에서는 양친매성물질인 $C_{12-20}$ 알킬글루코사이드, $C_{14-22}$ 알코올 및 베헤닐알코올로 구성된 액정 에멀젼을 제조하고 그 특성 및 in vitro 피부 투과 연구를 수행하였다. 액정 에멀젼의 배합비 실험 결과, $C_{12-20}$ 알킬글루코사이드 0.8%, $C_{14-22}$ 알코올 3.2% 및 베헤닐알코올 4%에서 선명한 액정 구조가 관찰되었다. 액정 에멀젼과 비교군으로 O/W 에멀젼의 물리적 특성을 비교한 결과, 액정 에멀젼과 O/W 에멀젼의 점성은 각각 $1871.26{\sim}1.15Pa{\cdot}s$ 및 $1768.69{\sim}1.14Pa{\cdot}s$이었으며, 전단응력은 액정 에멀젼은 190.45 ~ 919.38 Pa, O/W 에멀젼은 178.68 ~ 909.18 Pa로 측정되었다. 저장 탄성률은 액정 에멀젼은 4487.82 ~ 8195.59 Pa, O/W 에멀젼은 3428.53 ~ 9157.45 Pa, 탄성에 대한 점성의 비인 tan (delta) 값은, 액정 에멀젼은 0.23 ~ 0.25, O/W 에멀젼은 0.43 ~ 0.19로 나타났다. 경피 수분 함량 측정 결과, 액정 에멀젼은 O/W 에멀젼에 비하여 사용 후 1 h부터 6 h까지 유의적으로 더 높은 피부 수분 함량을 나타냈으며, 경피 수분 손실에서는 30 min부터 4 h까지 유의적으로 수분 손실 억제 효과를 나타내었다. 글리시리직애씨드를 이용한 피부 투과 실험 결과, 24 h 동안 피부 투과량은 액정 에멀젼($64.58{\mu}g/cm^2$), O/W 에멀젼($37.07{\mu}g/cm^2$), 부틸렌글라이콜 용액($41.05{\mu}g/cm^2$) 순으로 나타났고, 시간별 투과능 관찰 결과는 8 h 이후부터 액정 제형에서 피부 투과능이 증가하는 것으로 나타났다. 결론적으로 액정 에멀젼은 피부의 보습 효과를 증진시킬 뿐만 아니라 기능성 소재의 효율적인 피부 전달체로서 응용 가능성이 있음을 시사한다.

• Journal of Pharmaceutical Investigation
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• 제29권4호
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• pp.343-348
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• 1999

The purpose of this study is to prepare the controlled release adhesive patch containing naproxen. Pressuresensitive adhesive (PSA)-type patch was fabricated by casting of polyisobutylene (PIE.) and mineral oil in toluene. Membrane-controlled release (MCR)-type patch was prepared by the attachment of the controlled release membrane on the PSAtype patch. The membrane was mainly composed of Eudragit, polyethylene glycol(PEG) and glycerin. The drug release profile and skin permeation test with various patches were evaluated in vitro. The release of naproxen from PIE-based PSAtype patch with various loading doses fitted Higuchi's diffusion equation. However, the permeation of naproxen through hairless mouse skin from PSA-type patch followed zero-order kinetics. In MCR-type patch, thickness of controlled release membrane affected on the drug release rate highly. In the composition of membrane, the release rate was decreased as the ratio of Eudragit increased. The drug release from the MCR-type patch followed zero order kinetics. The permeation of naproxen through hairless mouse skin from MCR-type patch showed lag time for the intial release period and didn't fit the zero-order kinetics

• 약학회지
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• 제56권3호
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• pp.152-157
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• 2012

Angelica gigas is one of the most widely used herbal medicines in Asia. Root extract of Angelica gigas is known to have anti-oxidant activity and skin whitening effect. The aim of this study was to prepare microemulsion system of root extracts of Angelica gigas for topical delivery. Microemulsion was successfully prepared by using MCT (medium chain triglyceride) as an oil phase, Labrasol as a surfactant, and the mixture of propyleneglycol and phosphatidylcholine (4 : 1) as a cosurfactant. In vitro and in vivo skin permeation and deposition of decursin, as a marker, was determined using hairless mouse. Microemulsion significantly increased the in vitro skin permeation of decursin for up to 12 hours and was significantly higher than the control (water). Moreover, microemulsion formulation showed significantly higher skin deposition of decursin compared to the control in both in vitro and in vivo studies. Thus, microemulsion could be a useful vehicle for topical application of root extracts of Angelica gigas.

• Archives of Pharmacal Research
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• 제24권6호
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• pp.572-577
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• 2001

The feasibility of skin penetration was studied for aspalatone (AM, acetylsalicylic acid maltol ester), a novel antithrombotic agent. In this studys hairless mouse dorsal skins were used as a model to select composition of vehicle and AM. Based on measurements of solubility and partition coefficient, the concentration of PC that showed the highest flux for AM across the hairless mouse skin was found to be 40%. The cumulative amount permeated at 48 h, however, appear inadequate, even when the PC concentration was employed. To identify a suitable absorption enhancer and its optimal concentration for AM, a number of absorption enhancers and a variety of concentration were screened for the increase in transdermal flux of AM. Amongst these, linoleic acid (LOA) at the concentration of 5% was found to have the largest enhancement factor (i.e., 132). However, a further increase in AM flux was not found in the fatty acid concentration greater than 5%, indicating the enhancement effect is in a bell-shaped currie. In a study of the effect of AM concentration on the permeation, there was no difference in the permeation rate between 0.5 and 1% for AM, below its saturated concentration. At the donor concentration of 2%, over the saturated condition, the flux of AM was markedly increased. A considerable degradation of AM was found during permeation studies, and the extent was correlated with protein concentrations in the epidermal and serosal extracts, and skin homogenates. In rat dorsal skins, the protein concentration decreased in the rank order of skin homogenate > serosal extract > epidermal extract. Estimated first order degradation rate constants were $6.15{\pm}0.14,{\;}0.57{\pm}0.02{\;}and{\;}0.011{\pm}{\;}0.004{\;}h^{-1}$ for skin homogenate, serosal extract and epidermal extract, respectively. Therefore, it appeared that AM was hydrolyzed to some extent into salicylmaltol by esterases in the dermal and subcutaneous tissues of skin. taken together, our data indicated that transdermal delivery of AM is feasible when the combination of PC and LOA is used as a vehicle. However, since AM is not metabolically stable, acceptable degradation inhibitors may be nervessary to fully realize the transdermal delivery of the drug.