• Biomolecules & Therapeutics
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• 제19권3호
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• pp.357-363
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• 2011

In relieving local pains, ropivacaine has been widely used. In case of their application such as ointments and creams, it is difficult to expect their effects for a significant period of time, because they are easily removed by wetting, movement and contacting. Therefore, the new formulations that have suitable bioadhesion were needed to enhance local anesthetic effects. The effect of drug concentration and temperature on drug release was studied from the prepared 1.5% Carboxymethyl cellulose (CMC) (150MC) gels using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. As the drug concentration and temperature increased, the drug release increased. A linear relationship was observed between the logarithm of the permeability coefficient and the reciprocal temperature. The activation energy of drug permeation was 3.16 kcal/mol for a 1.5% loading dose. To increase the skin permeation of ropivacaine from CMC gel, enhancers such as saturated and unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants were incorporated into the ropivacaine-CMC gels. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest enhancing effects. For the efficacy study, the anesthetic action of the formulated ropivacaine gel containing an enhancer and vasoconstrictor was evaluated with the tail-flick analgesimeter. According to the rat tail-flick test, 1.5% drug gels containing polyoxyethylene 2-oleyl ether and tetrahydrozoline showed the best prolonged local analgesic effects. In conclusion, the enhanced local anesthetic gels containing penetration enhancer and vasoconstrictor could be developed using the bioadhesive polymer.

• Toxicological Research
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• 제27권3호
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• pp.153-160
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• 2011

To evaluate the whitening effect of black tea water extract (BT), BT was topically applied to artificially hyperpigmented spots on the back skins of brown guinea-pigs (weight: 450~500 g) induced by 1,500 mJ/$cm^2$ of ultraviolet B (UVB) irradiation. The test compounds of 30 ${\mu}l$ were applied twice a day, six days a week, for four weeks. The artificially hyperpigmented spots were divided into 5 groups: control (UVB + saline, C), vehicle control [UVB + propylene glycol: ethanol: water (5 : 3 : 2), VC], positive control (UVB + 2% hydroquinone, PC), experimental 1 (UVB + 1% BT), experimental 2 (UVB + 2% BT). After 4-week application, the spots were removed by biopsy punch under anesthetic condition and used as specimens for the histological examination. The total polyphenol and flavonoid contents of BT were 104 and 91 mg/g, respectively. The electron-donating ability of BT revealed a dose-dependent response, showing the excellent capacities of 86% at 800 ${\mu}g$/ml. The artificially hyperpigmented spots treated with the PC and BT were obviously lightened compared to the C and VC groups. At the fourth week, the melanin indices for the PC and BT groups were significantly lower (p < 0.001) than those of the C and VC groups. In histological examination, PC and BT groups were significantly reduced in the melanin pigmentation, the proliferation of melanocytes and the synthesis of melanosomes compared to the C and VC groups. It is found that BT inhibits the proliferation of melanocytes and synthesis of melanosomes in vivo using brown guinea pigs, thereby showing a definite skin whitening effect.

• Archives of Plastic Surgery
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• 제35권5호
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• pp.507-513
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• 2008

Purpose: Interest in the augmentation of hair growth for functional and aesthetic purpose has increased dramatically in recent years. Many hair growth products have been released, but most of these have not been proven scientifically. This study aims to measure the hair growth effect of azelaic acid and vitamin $B_6$, which have been known as hair growth materials, in animal models. Methods: Six weeks old C57BL/6 mice were used in this study and hair of mice were removed by topical treatment. The mice were divided into five experimental groups according to the testing material such as saline (negative control), propylene glycol(vehicle control), azelaic acid, vitamin B6 and azelaic acid plus vitamin B6 in combination. Hair growth was documented photographically and histologically, and then analysed by the high quality hair analysis program system. The quantity of endocrine factors, IGF-I and TGF-${\beta}1$ in the skin of mice was measured by PCR analysis. Results: The topical treatment of azelaic acid and vitamin B6 in combination for 2 weeks to dorsal skin accelerated hair regrowth more than other groups. The azelaic acid and vitamin $B_6$-combined treatment also promoted hair follicle elongation and thickness compared to the others. Histologic studies showed increased number of basal cells in azelaic acid and vitamin $B_6$-combined treatment. Furthermore, the azelaic acid and vitamin $B_6$-combined group significantly increased the expression of IGF-I but decreased the expression of TGF-${\beta}1$ in the skin of mice compared to other groups. Conclusion: These results suggest that azelaic acid and vitamin $B_6$, when used together, have an additive effect and might be used as hair growth materials.

• Journal of Microbiology and Biotechnology
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• 제23권8호
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• pp.1133-1139
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• 2013

Enzymatic decomposition of gelatin layers on used X-ray films and repeated utilization of the enzyme for potential application in silver recovery were investigated using keratinolytic serine proteases from Purpureocillium lilacinum LPS # 876. At pH 9.0, the enzymatic reaction was enhanced by the increase of enzyme concentration or by the increase of the temperature up to $60^{\circ}C$. Under the conditions of 6.9 U/ml, $60^{\circ}C$, and pH 9.0, hydrolysis of the gelatin layers and the resulting release of silver particles were achieved within 6 min. The protective effect of polyols against thermal denaturation was investigated. The presence of glycerol and propylene glycol increased enzyme stability. When the reusability of the enzyme for gelatin hydrolysis was tested, it could be seen that it could be effectively reused for more cycles when glycerol was added, compared with the enzyme without protective agents. The results of these repeated treatments suggested that a continuous process of recycling silver from used X-ray is feasible. Keeping in mind that recycling is (at the present time) needed and imperative, it can be remarked that, in this research, three wastes were successfully used: hair waste in order to produce serine proteases; glycerol in order to enhance enzyme thermal stability; and used X-ray films in order to recover silver and PET films.

• Journal of Pharmaceutical Investigation
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• 제35권4호
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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 Pharmaceutical Investigation
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• 제33권2호
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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.

• Journal of Pharmaceutical Investigation
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• 제32권4호
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• pp.313-319
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• 2002

Rat skin permeation of various nonsteroidal antiinflammatory drugs (NSAIDs) was investigated in vitro using Franz diffusion cell at $37^{\circ}C$. The effect of various skin permeation enhancers was also observed as a preliminary study of developing transdermal delivery systems of NSAIDs. Lipophilicity of NSAIDs was determined from thε partition coefficient (log P) in 1-octanol/water and 1-octanol/IPB mutual-saturated solutions. The solubility was determined in water, isotonic phosphate buffer (IPB), and propylene glycol (PG) at $37^{\circ}C$. The rat skin permeation rate of acetaminophen, piroxicam, and aceclofenac was almost negligible, although they were saturated in PG. Addition of 1 % permeation enhancer increased the permeation rate of ketoprofen, ketorolac, and diclofenac. However, the skin permeation rate of ibuprofen did not increase with the addition of various enhancers. Among the permeation enhancers testεd, oleic acid was the most effective for various NSAIDs. Based on the daily dose, lipophilicity, and the skin permeation ratε achieved in this study, ketoprofen and ketorolac seem to be the most promising drug candidates for transdermal delivery systems, especially when formulated with unsaturated fatty acids, such as oleic acid.

• Applied Biological Chemistry
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• 제36권4호
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• pp.296-303
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• 1993

식품첨가물로 허용되어 있는 알긴산나트륨, 알긴산프로필렌글리콜(PGA), 카르복시메틸셀룰로오스나트륨(CMC), 펙틴 등 4종의 다당류를 이용하여 달걀 노른자의 수용성 단백질을 분리하기 위한 조건을 반응표면 분석법으로 조사하였다. Rotatable hexagon design으로 실험을 계획하여 다당류의 사용농도 5개 수준, 반응 pH 3개 수준에서 상층액 중의 단백질과 지방질 함량을 각각 측정하여 2차 회귀모형을 구하였다. 통계분석 결과 반응 pH가 다당류의 농도보다 난황 단백질-다당류 상호작용에 더 영향을 미치는 요인으로 밝혀졌다. 각 반응도의 contour plot을 작성, 분석하여 수용성 난황 단백질 분리의 조건으로 알긴산나트륨; 농도 $0.23{\sim}0.25%$, $pH\;5.9{\sim}6.0$, PGA; 농도 $0.15{\sim}0.17%$, $pH\;4.3{\sim}4.5$, CMC; 농도$0.30{\sim}0.31%$, pH 3.0 펙틴; 농도 $0.09{\sim}0.10%$, $pH\;5.6{\sim}5.8$을 설정하였다.

• 대한화장품학회지
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• 제38권4호
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• pp.263-270
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• 2012

아스코르빅산(비타민 C)은 수용액상에서 공기와 빛, 알칼리 등에 의해 쉽게 불안정화되는 성질이 있어 화장품에 적용에 있어서 제한적이다. 아스코르빅산은 수용액상에서 불안정성에 영향을 주는 가장 중요한 인자인 공기, 특히 산소와 열, 빛 등의 외부환경에 민감하게 반응하여 산화에 의해 쉽게 분해되는 문제점이 있다. 본 연구에서는 이러한 아스코르빅산의 안정성을 증가시키고자 폴리올과 유화방법을 변화시켜 안정화하는 연구를 수행하였고 실온과 고온에서 색상과 아스코르빅산의 함량변화를 HPLC로 측정하여 비교하였다. 그 결과 실험한 조건들 중 폴리올은 글리세린을 사용한 경우 아스코르빅산의 안정화 가장 좋았으며 비수유화방법을 사용한 경우에 있어서 가장 안정하였다. 이러한 결과들로부터 아스코르빅산이 본 실험의 비수유화로 안정성이 증가하며 안정한 화장품을 만드는 데 적용이 가능하다.

• 폴리머
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• 제34권5호
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• pp.442-449
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• 2010

본 연구에서는 hard segment 함량(%)별로 친수성의 폴리우레탄 프리폴리머를 합성한 후 다양한 발포 혼합 조성액을 이용하여 폴리우레탄 폼을 제조하였다. 그 결과 사슬연장제를 도입한 폴리우레탄 프리폴리머가 도입하지 않은 것에 비해 기계적 물성이 우수하였다. 또한 폴리우레탄 구조에 hard segment 함량(%)을 높임으로써 폴리우레탄의 기계적 물성을 향상시킬 수 있었다. 한편 발포 혼합조성액에서도 F-68, 글리세린, CMC 등의 원료 배합비를 조정함으로써 최종적으로 제조된 폴리우레탄 폼의 기계적 물성과 흡수도, 흡수속도, 모폴로지 등을 조절할 수 있었다. 제조된 폴리우레탄 폼은 세포배양 결과 세포적합성이 우수하였고, 동물실험 결과 대조군인 거즈에 비하여 월등한 창상치유 효과를 보였으므로 창상치료용 소재로서의 적용 가능성이 높음을 알 수 있었다.