• Archives of Pharmacal Research
• /
• 제28권9호
• /
• pp.1097-1102
• /
• 2005

An O/W microemulsion system was developed to enhance the skin permeability of ace-clofenac. Of the oils studied, Labrafil? M 1944 CS was chosen as the oil phase: of the microemulson, as it showed a good solubilizing capacity. Pseudo-ternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, Cremophor ELP, and co-surfactant, ethanol, for micoemulsion formation. Eight different formulations with various values of oil of $6-30\%$, water of $0-80\%$, and the mixture of surfactant and co-surfactant (at the ratio of 2) of $14-70\%$. The in vitro transdermal permeability of aceclofenac from the microemulsions was evaluated using Franz diffusion cells mounted with rat skin. The level of aceclofenac permeated was analyzed by HPLC and the droplet size' of the microemulsions was characterized using a Zetasizer Nano-ZS. Terpenes were added to the microemulsions at a level of $5\%$, and their effects on the skin permeation of aceclofenac were investigated. The mean diameters of the microemulsions ranged between approximately $10\~100nm$, and the skin permeability of the aceclofenac incorporated into the microemulsion systems was 5-fold higher than that of the ethanol vehicle. Of the various terpenes added, limonene had the best enhancing ability. These results indicate that the microemulsion pystem studied is a promising tool for the percutaneous delivery of aceclofenac.

• 공업화학
• /
• 제24권3호
• /
• pp.260-265
• /
• 2013

본 연구에서는 비타민나무 잎 추출물의 에틸아세테이트 분획 0.01, 0.03, 0.05, 0.10% 함유한 나노에멀젼을 제조하였고, 5주 동안 이들 나노에멀젼의 입자 크기, 입도분포 및 피부 투과능을 평가하였다. 나노에멀젼은 균질기(homogenizer) 처리 후 고압유화기(micro-fluidizer)를 이용하여 제조하였다. 비타민나무 잎 추출물의 에틸아세테이트 분획을 함유한 나노에멀젼은 단분산 형태를 나타내었다. 5주 동안 실험에서, 0.03% 에틸아세테이트 분획을 함유한 나노에멀젼이 가장 안정하였다. 0.03% 에틸아세테이트 분획 함유 나노에멀젼의 in vitro 피부 투과 실험을 Franz diffusion cell을 이용하여 수행하였다. Oil-in-water (O/W) 에멀젼과 비교할 때 나노에멀젼이 피부 흡수가 더 잘되는 것으로 나타났다. 이러한 결과들은 비타민나무 잎 추출물을 함유한 나노에멀젼이 O/W 에멀젼보다 안정성과 피부 투과능이 우수함을 나타낸다.

• Journal of Pharmaceutical Investigation
• /
• 제36권5호
• /
• pp.321-329
• /
• 2006

Albuterol, a selective ${\beta}_2$-adrenergic receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease, chronic bronchitis and pulmonary emphysema. The percutaneous permeation of albuterol sulfate was investigated in hairless mouse skin in vitro with and without pretreatment with enhancers. The enhancing effects of ethanol and various penetration enhancers such as terpenes, non-ionic surfactants, pyrrolidones, and fatty acids on the permeation of albuterol sulfate were evaluated using Franz diffusion cells. Among terpenes studied, 1,8-cineole was the most effective enhancer, which increased the permeability of albuterol sulfate approximately 33-fold compared with the control without enhancer pretrement, followed by d-limonene with enhancement ratio of 21.79. 2-Pyrrolidone-5-carboxylic acid increased the permeability of albuterol sulfate approximately 5.5-fold compared with the control. Other pyrrolidones tested showed only slight permeability enhancing effect with enhancement ratio less than 2.8. Nonionic surfactants showed moderate enhancing effects. Lauric acid increased the permeability of albuterol sulfate approximately 30-fold with decreasing the lag time from 2.85 to 0.64 hr. Oleic acid and linoleic acid showed enhancement ratio of 24.55 and 22.91, respectively. These findings would allow a more rational approach for designing formulations for the transdermal delivery of albuterol sulfate and similar drugs.

• Archives of Pharmacal Research
• /
• 제19권6호
• /
• pp.435-440
• /
• 1996

The effect of benzalkonium chloride on skin permeability of partially modified antisense phosphorothioate oligonucleotides (PS-ODN), which are designed as scar formation inhibitor, was investigated using Franz Diffusion Cell. When the concentration ratio of PS-ODN-quarternary ammonium salt complex is more than 1:100, the apparent partition coefficient (APC) of each complex was increased in the following order; tetraphenyl phosphonium chloride (TPP) < cetyltrimethyl ammonium bromide(CTAB) < benzalkonium chloride (BZ). The permeability of PS-ODN through the rat skin increased in the presence of BZ. The fluxs of PS-ODN with BZ were increased by addition of Pluronic F 68 or Triton X-100 to phosphate buffered saline (PBS), respectively. When the mole ratio of PS-ODN to BZ is 1:10, the fluxs penetrated of PS-ODN with BZ was greatest. The increase of the permeability in the presence of BZ might be due to the formation of lipophilic ion-pair complex between PS-ODN and BZ. By regulation of mole ratio of PS-ODN to BZ, the development of topical dosage forms using PS-ODN as scar formation inhibitor will be possible with minimal systemic exposure.

• Journal of Pharmaceutical Investigation
• /
• 제27권4호
• /
• pp.271-277
• /
• 1997

Because omeprazole(OMP) is very unstable in aqueous condition, $OMP-{\beta}-CD$, the inclusion complex of OMP and ${\beta}-cyclodextrin({\beta}-CD)$ was made and physicochemical properties of it were compared with those of OMP. Skin permeability of OMP and $OMP-{\beta}-CD$ in propylene glycol vehicle and the reciprocal action of ${\beta}-CD$ with various enhancers were examined through hairless mouse. Adhesive patches were prepared with polyisobutylene and the skin permeability and stability of OMP were investigated. The inclusion complex showed higher solubility and lower partition coefficient than OMP itself. DMSO, 1-methyl 2-pyrrolidone and sodium cholate had an enhancing effect. However ethanol and polysorbate 80 hardly showed the enhancing effect of OMP. When sodium lauryl sulfate and sodium cholate as enhancer were added in patch, the former case showed higher permeability of OMP.

• Journal of Pharmaceutical Investigation
• /
• 제35권3호
• /
• pp.165-171
• /
• 2005

Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. However, it is difficult for itraconazloe to be delivered by topical system due to its poor aqueous solubility. First, niosomes containing drug were prepared with span 60, cholesterol. tocopherol and poloxamer 407 as vesicle forming agents in an effort to increase solubility of itraconazole. And then prepared niosomes were dispersed in O/W creams (containing xanthan gum, glycerin, vaseline, glyceryl monostearate and $Cerix^{\circledR}-5$) or gels (containing xanthan gum and poloxamer 407). Both creams and gels were evaluated with respect to their rheological properties, in vitro permeation through excised skin of hairless mouse. Creams or gels containing niosome showed pseudoplastic flow and hysteresis loop. For both creams and gels, viscosity was increased with increasing the content of glycerine or vaseline and the content of gel forming polymer, respectively. In creams, the permeability of drug to skin was decreased with increasing the viscosity of cream. The permeability of drug was affected by pH as well as viscosity of gel. In vitro permeation test results demonstrated that cream formulations showed better permeability than gels. In conclusion, these results suggest that creams formulation containing niosome can be useful for the topical delivery of intraconazole.

• 한국응용과학기술학회지
• /
• 제41권1호
• /
• pp.1-8
• /
• 2024

화장품 소재는 안전성이 무엇보다 중요시된다. 화장품에 사용되는 기존의 보존제인 PE에 대장균 효소 𝛽-gal을 이용하여 안전성이 증가된 PE-gal을 생합성하였다. 화장품 소재로 사용하기 위해 생합성된 생성물인 PE-gal의 피부 흡수도를 기존의 보존제인 PE와 비교하기 위해 Franz Diffusion cell Assay 시스템을 이용하여 경피투과도를 측정하였다. 같은 질량농도의 시료를 사용하였을 때 PE의 Flux 값, Kp 값은 시간이 지날수록 증가하는 것으로 나타났으나 PE-gal은 투과도를 측정할 수 있을 만큼 투과되지 못하였다. 이는 PE의 피부투과도가 생합성된 PE-gal 배당체보다 높다는 것을 나타낸다. Marzulli 등에 따라 Kp 값을 이용하여 투과 정도를 확인하였을 때 PE의 투과속도는 1mg/mL의 농도에서 느림(slow)으로 측정되었다. 따라서 배당체 형태의 PE-gal은 PE에 비해 경피 투과도가 현저히 낮게 나타났다.

• 대한화장품학회지
• /
• 제25권4호
• /
• pp.145-154
• /
• 1999

A novel retinol derivative, polyethoxylated retinamide(Medimin A) was synthesized, as an anti-aging agent. Collagen synthesis, skin permeation, stability, and toxicity of Medimin A were evaluated and compared with those of retinol and retinyl palmitate. In vitro collagen synthesis was evaluated by quantitative assay of $[^3H]-proline$ incorporation into collagenase sensitive protein in fibroblast cultures. For in vitro skin permeation experiments, Franz diffusion cells(effective diffusion area: 1,766 $cm^2$) and the excised skin of female hairless mouse aged 8 weeks were used, The stabilities of retinoids were evaluated at two different temperature($25^{\circ}C\;and\;40^{\circ}C$) and under UV in solubilized state and in O/W emulsion. To estimate the safety, acute oral toxicity, acute dermal toxicity, primary skin irritation, acute eye irritation and human patch test were performed. The effect of Medimin A on collagen synthesis was similar to that of retinol. The skin permeability of Medimin A was higher than those of retinol and retinyl palmitate. The Medimin A was more stable than retinol and retinyl palmitate. Medimin A was nontoxic in various toxicological tests. These results suggest that Medimin A would be a good anti-aging agent for enhancing bioavailability and stability.

• KSBB Journal
• /
• 제25권3호
• /
• pp.297-302
• /
• 2010

Ketoprofen is one of the propionic acid class of nonsteroidal anti-inflammatory drug with analgesic and antipyretic effects. The most common side effects from ketoprofen after oral administration are gastrointestinal irritation, diarrhea, abdominal pain and retention of fluid. Ketoprofen was formulated as water-soluble gels to reduce these side effects. To increase the skin permeability of ketoprofen, microsphere containing ketoprofen was prepared with chitosan and ploy-$\varepsilon$-caprolactone. And then prepared microsphere was manufactured as an adhesive hydrogel with polyvinylpyrrolidone K-25, polyethylene glycol 4000, and various permeation enhancers. The flux and permeability of ketoprofen were evaluated. As the concentration of tween 80 and enhancers increased, the flux of ketroprofen was accelerated. Also the permeation rate was facilitated by enhancers, but did not affect the lag time. From these results, the adhesive hydrogel using microsphere could be a good delivery system for ketoprofen to improve the skin permeation.

• 한국지하수토양환경학회:학술대회논문집
• /
• 한국지하수토양환경학회 2000년도 추계학술대회
• /
• pp.81-84
• /
• 2000

Two-layer aquifer system with fractional flow dimension is composed of contiguous two layers: Layer 1 (lower layer) and Layer 2 (upper layer) with different permeability and specific storage each other. For this aquifer system, we assume that groundwater flow originates only from Layer 1 on the pumping well. The aquifer system considers wellbore storage and skin effects on the pumping well. Dimensionless drawdown curves for different flow dimensions are analyzed for different lambda (λ, crossflow coefficient) values, kappa ($textsc{k}$, permeability ratio between Layer 1 and Layer 2) values and omega ($\omega$, storativity ratio between Layer 1 and Layer 2) values. The curves for Layer 1 and Layer 2 show characteristic trend each other.