• 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.

• Journal of Pharmaceutical Investigation
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• 제37권4호
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• pp.243-247
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• 2007

Retinoids have many important and diverse functions and particularly, have been widely used as anti-aging agent and for the treatment of acne and psoriasis in cosmetics. However, retinoids have low stability against the air, light, water, oxygen and heat, thus, to stabilize the retinoids in formulations is very critical procedure. In this study, cubic liquid crystalline phase of monoolein was applied to stabilize the retinylpalmitate (RP) and to enhance the transdermal permeation. Cubic liquid crystalline phase significantly enhanced the stability of RP. After 15 days, the content of RP in the cubic formulation was 94.7% while the content of RP in ethanol solution was below 0.5% at room temperature. Although BHT containing crystalline phase showed the slightly increased stability of RP, there were no significant differences in RP stability between with or without antioxidants (ascorbic acid, ${\alpha}$-tocopherol, BHT, BHA) at $40^{\circ}C$. The skin retention of RP in crystalline formulations was approximately $5.3{\sim}6.4$ times greater than that of o/w cream formulation. Incorporation of RP into cubic liquid crystalline phase of monoolein effectively stabilized the RP and worked as excellent topical vehicle for RP. Liquid crystalline phase is considered to be suitable formulation for RP for topical delivery system as a stabilizer and permeation enhancing agent.

• Bulletin of the Korean Chemical Society
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• 제28권9호
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• pp.1535-1538
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• 2007

The work presented in this paper represents a study of the rate and extent of transdermal penetration of three synthetic hexapeptides consisting only of glycine (Gly) and phenylalanine (Phe) as the constituent amino acids and they include Phe-Gly-Gly-Gly-Gly-Gly (Pep-1), Phe-Phe-Gly-Gly-Gly-Gly (Pep-2), and Phe-Phe-Phe- Gly-Gly-Gly (Pep-3). The present study demonstrated the extent to which the peptides having a high metabolic stability were transdermally transported from the various vehicles. The results of this study appear to indicate that minor differences in the lipophilicity of the synthetic hexapeptides have a slight influence on the rate and extent of transport. In the presence of terpene permeation enhancers, together with ethanol (i.e., menthone/ EtOH, carveol/EtOH or cineole/EtOH), the peptides were more rapidly penetrated through the skin and among the terpenes tested, cineole was the most effective for all three peptides. The maximum enhancement ratio of approximately 2 was achieved by cineole in 50% ethanol solution.

• Membrane and Water Treatment
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• 제9권4호
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• pp.221-231
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• 2018

A new procedure to produce poly(vinylidene fluoride)/boron nitride hybrid membrane is presented for application in membrane distillation (MD) process. The influence of hexagonal boron nitride (h-BN) incorporation on the performance of the polymeric membranes is studied through the present investigation. For this aim, h-BN nanopowders were successfully synthesized using the simple chemical vapor deposition (CVD) route and subsequent solvent treatments. The resulting h-BN nanosheets were blended with poly(vinylidene fluoride) (PVDF) solution. Then, the prepared composite solution was subjected to phase inversion process to obtain PVDF/h-BN hybrid membranes. Various examinations such as scanning electron microscopy (SEM), wettability, permeation flux, mechanical strength and liquid entry pressure (LEP) measurements are performed to evaluate the prepared membrane. Moreover, Air gap membrane distillation (AGMD) experiments were carried out to investigate the salt rejection performance and the durability of membranes. The results show that our hybrid PVDF/h-BN membrane presents higher water permeation flux (${\sim}18kg/m^2h$) compared to pristine PVDF membrane. In addition, the experimental data confirms that the prepared nanocomposite membrane is hydrophobic (water contact angle: ${\sim}103^{\circ}$), has a porous skin layer (>85%), as well competitive fouling resistance and operational durability. Furthermore, the total salt rejection efficiency was obtained for PVDF/h-BN membrane. The results prove that the novel PVDF/h-BN membrane can be easily synthesized and applied in MD process for salt rejection purposes.

• 멤브레인
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• 제21권1호
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• pp.98-105
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• 2011

본 연구에서는 셀룰로오스 트리아세테이트(CTA) 고분자를 이용한 중공사형 분리막을 상분리법에 의해 제조하였으며, 제조된 중공사 분리막의 기체분리 성능을 평가하였다. 제조된 중공사형 분리막의 기체분리 특성을 부여하기 위해서 1,4-dioxane을 10 wt.% 내외로 첨가하였다. 1,4-dioxane의 첨가에 의해 중공사 표면에 치밀층 형성을 위해서는 1,4-dioxane이 표면에서 증발되는 것이 필수적이며, 이를 위해 air-gap의 조절에 의해 중공사 표면에 치밀층이 생성되도록 하였다. 제조된 CTA 중공사형 기체분리막의 표면 및 단면의 모폴로지 측정을 위하여 전자주사현미경을 사용하였다. 또한 CTA 중공사형 기체분리막의 산소, 질소, 이산화탄소에 대한 기체투과도를 측정하였으며, 이 때 $P_{CO2}$ = 17 GPU, ${\alpha}_{CO2/N2}$ = 48을 나타내었다.

• Journal of Pharmaceutical Investigation
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• 제38권6호
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• pp.373-380
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• 2008

In order to develop optimal formulation and iontophoresis condition for the transdermal delivery of levodopa, we have evaluated the effect of two permeation enhancers, ethanol and oleic acid in microemulsion, on transdermal delivery of levodopa. In vitro flux studies were performed at $33^{\circ}C$, using side-by-side diffusion cell and full thickness hairless mouse skin. Current density applied was $0.4\;mA/cm^2$ and current was off after 6 hours application. Levodopa was analysed by HPLC at 280 nm. The o/w microemulsions of oleic acid in buffer solution (pH 2.5 & 4.5) were prepared using oleic acid, Tween 80 and ethanol. The existence of microemulsion regions were investigated in pseudo-ternary phase diagrams. Contrary to our expectation, cumulative amount of levodopa transported from microemulsion (pH 2.5) for 10 hours was similar to that from aqueous solution in all delivery methods (passive, anodal and cathodal). When pH of the micro-emulsion was pH 4.5, cumulative amount of levodopa transported for 10 hours increased about 40% (anodal) to 50% (cathodal), when compared to that from aqueous solution. Flux from pH 4.5 microemulsion showed higher value than that from pH 2.5 in all delivery methods. These results seem to indicate that electroosmosis plays more dominant role than electrorepulsion in the flux of levodopa at pH 2.5. The effect of ethanol on iontophoretic flux was studied using pH 2.5 phosphate buffer solution containing 3% or 5% (v/v) ethanol. Flux enhancement was observed in passive and anodal delivery as the concentration of the ethanol increased. Without ethanol, cathodal delivery showed higher flux than anodal delivery. Anodal delivery increased the cumulative amount of levodopa transported 1.6 fold by 5% ethanol after 10 hours. However, in cathodal delivery, no flux enhancement of levodopa was observed during current application and only marginal increase in cumulative amount transported after 10 hours was observed by 5% ethanol. These results seem to be related to the decrease in dielectric constant of the medium and the lipid extraction of the ethanol, which decrease the electroosmotic flow, and thus decrease the flux. Overall, the results provide important insights into the role of electroosmosis and electrorepulsion in the transport of levodopa through skin, and provide some useful informations for optimal formulation for levodopa.

• Korean Chemical Engineering Research
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• 제58권1호
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• pp.29-35
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• 2020

본 연구에서는 경피흡수가 잘 안되는 주름개선 펩티드인 GHK, GHK-Cu, Pal-GHK에 대하여 세포투과 펩티드인 알르기닌 올리고머(tetra-D-arginine, R4)와 hexa-D-arginine, R6)를 첨가한 후 경피 투과도를 측정하여 그 결과를 다음 6가지 경우로 분석하였다. 첫번째로 주름개선 펩티드만 함유한 경우는 구리이온(Cu₂⁺)과 팔미트산이 경피 투과율을 증진시키는 것을 알 수 있다. 두번째로, GHK에 알르기닌 올리고머(R4, R6)를 첨가한 경우는 알르기닌 올리고머(R4, R6)가 경피 투과율을 증가시켰으며, R4에서 더 좋은 경피 투과율 증가를 나타났다. 세번째로, GHK-Cu에 R4, R6를 첨가한 경우는 경피 투과율 증가가 나타났으며, R6 < R4 경피 투과율 순서로 나타났다. 네번째로 Pal-GHK에 R4, R6를 첨가한 경우에도 경피 투과율 증가가 나타났으며, R6 < R4 경피 투과율 순서로 나타났다. 다섯번 째로, R4를 GHK, GHK-Cu, Pal-GHK에 첨가한 경우에는 GHK+R4 < GHK-Cu+R4 < Pal-GHK+R4 순서로 경피 투과율 증가가 나타났다. 마지막으로 R6를 GHK, GHK-Cu, Pal-GHK에 첨가한 경우에는 GHK+R4 < GHK-Cu+R4 < Pal-GHK+R4 순서로 경피 투과율 증가가 나타났다. 이를 통하여 주름 개선 펩티드인 GHK, GHK-Cu, Pal-GHK의 피부 투과를 증가를 위한 최적의 조건을 제시하여 그 효능을 극대화할 수 있는 방안을 제시함으로써 주름 개선 기능성 화장품에서의 폭넓은 활용과 응용을 제안하고자 한다.

• 공업화학
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• 제26권2호
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• pp.165-172
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• 2015

쿼세틴과 쿼세틴의 배당체인 루틴은 천연 항산화제로 잘 알려진 플라보노이드이다. 본 연구에서는 플라보노이드(쿼세틴과 루틴)를 담지한 양이온 리포좀을 제조하여 세포 및 피부 투과성과 자외선(UVA)에 대한 HaCaT 세포 보호 효과를 평가하였다. 빈 양이온 리포좀의 입자 크기는 100~130 nm이며, 입자 표면 전위는 + 33.05 mV를 나타내었다. 포집효율은 루틴을 담지한 리포좀과 양이온 리포좀이 쿼세틴을 담지한 경우보다 높았다. 세포 내 이입율 비교결과, 양이온 리포좀이 일반 리포좀에 비해 약 5배 정도 높음을 확인했다. In vitro 상에서, 쿼세틴과 루틴이 용해된 PBS (phosphate-buffered saline) 수용액, 동량의 쿼세틴과 루틴을 담지한 리포좀과 양이온 리포좀의 피부투과율을 비교하였다. 양이온 리포좀에 담지하였을 경우 가장 높은 피부투과율을 보였다. 플라보노이드를 담지한 양이온 리포좀의 자외선(UVA $25J/cm^2$)에 대한 HaCaT 세포 보호 효과를 측정한 결과, 자외선만 조사한 군에 비해 플라보노이드 담지 양이온 리포좀을 처리한 군에서 높은 세포 보호 효과를 보였다. 결과적으로, 양이온 리포좀은 플라보노이드를 피부 속으로 전달하는데 있어서 매우 유용한 피부 전달 시스템임을 확인하였다. 따라서, 세포 보호 및 피부 흡수 증진 효과를 가지는 양이온 리포좀은 항노화 및 항산화 화장품 제형으로써 활용 가능성이 있음을 시사한다.

• 한국식품영양과학회지
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• 제35권9호
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• pp.1232-1236
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• 2006

포도주에 함유된 항보체 활성 다당류를 규명 및 분리하기 위하여 포도와 관련된 과실주로부터 조다당 획분을 시판되고 있는 적포도주, 백포도주 및 머루주로부터 농축과 에탄올 침전을 통하여 조제하였다. 항보체 활성의 검토 결과, 적포도주의 조다당 획분(RW-0)이 백포도주의 획분(WW-0)보다 더 높은 활성을 보여주었다. 항보체 활성을 갖는 포도주의 조다당 획분 중 Sephadex G-75의 gel permeation chromatography를 통하여 고분자 획분으로 RW-1과 WW-1으로, 저분자 획분으로 RW-2와 WW-2로 분획되었으며 머루주의 경우에는 분획되지 않았다. 분획된 획분 중 RW-1이 가장 높은 활성을 보여주었으며 91.3%의 당이 함유되어 있음을 확인할 수 있었다. 적포도주의 항보체 활성이 백포도주의 획분보다 높은 활성을 갖는 것은 펙틴과 헤미셀룰로오즈 등이 함유된 포도껍질로부터 활성 다당이 기인하는 것으로 보이며, 높은 당 함량과 수율을 보이는 고분자 획분, RW-1과 WW-1이 저분자 획분보다 활성이 높음을 알 수 있었다.

• Biomolecules & Therapeutics
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• 제5권1호
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• pp.82-86
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• 1997

Pharmacokinetics of a new capsaicin analog, DA-5018 were evaluated after a subcutaneous injection or topical application of $[^{14}C]$--labelled or unlabelled DA-5018 to rats and rabbits. After subcutaneous injection of $_{14}$c-labelled or unlabelled DA-5018, 0.5 mg/kg (equivalent to DA-5018) to rats, the plasma total activity peaked at 2 hr with the terminal half life of 5.34 hr, however, unlabelled-DA-5018 peaked at 1 hr with the terminal half life of 1.26 hr. Moreover, the AUC (0.726 versus 0.2337g hr/ml) and MRT (7.82 versus 3.55 hr) increased significantly based on total radioactivity compared with intact DA-5018. Above data indicated that DA-5018 is extensively metabolized in rats and the terminal half- life of the metabolite(5) had a longer half-life than that of DA-5018. The cumulative percentages of biliary excretion of dose after subcutaneous injection of $[^{14}C]$DA-5018 was 40.2%, however, the value was only 2.14% when unlabelled DA-5018 was injected. After topical application of 0.1% or 0.3% $_{14}$C-labelled or unlabelled DA-5018 cream, 500 mg/kg to rats, the plasma and tissue concentrations except applied skin were under the detection limit. After consecutive 7 days topical application of unlabelled DA-5018, 0.1% and 0.3% cream to rats, the plasma concentrations were also under the detection limit. But the urinary excretion of DA-5018 was significantly increased by repeated topical administration. After topical application of unlabelled DA-5018, 0.1% and 0.3% cream to rabbits, the plasma and urine concentrations were under the detection limit. Above data indicated that the skin permeation of DA-5018 was lower and the metabolism of DA-5018 was higher in rabbits than that in rats.