• Applied Chemistry for Engineering
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• v.24 no.3
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• pp.260-265
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• 2013

In this study, nano-emulsions containing 0.01, 0.03, 0.05, and 0.10% ethyl acetate fraction of Hippophae rhamnoides (H. rhamnoides) leaf extracts were prepared. The particle size, particle size distribution and skin permeability of the nano-emulsions were evaluated for five weeks. Nano-emulsion was prepared by the sequential use of homogenizer and microfluidizer. Nano-emulsion containing the ethyl acetate fraction exhibited a monodispersed form. Nano-emulsion containing 0.03% ethyl acetate fraction was the most stable for five weeks. The in vitro skin permeation study of nano-emulsion containing 0.03% ethyl acetate fraction was carried out using Franz diffusion cell. The nano-emulsion showed a better skin permeability than that of O/W emulsion. These results indicate that the nano-emulsion containing the ethyl acetate fraction of H. rhamnoides leaf extract showed a remarkable stability and skin permeability than that of O/W emulsion.

• Journal of Pharmaceutical Investigation
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• v.37 no.4
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• pp.237-242
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• 2007

The chemical formula of indapamide is 3-(aminosulfonyl)-4-chloro-N-(2,3-dihydro-2-methyl-1H-indol-l-yl)-benzamide, Indapamide is an oral antipertensive diuretic agent indicated for the treatment of hypertensive and edema. Indapamide inhibits carbonic anhydrase enzyme. Transdermal drug delivery systems, as compared to their corresponding classical oral or injectable dosage form counterparts, offer many advantages. The most important advantages are improved systemic bioavailability of the pharmaceutical active ingredients (PAI), because the first-pass metabolism by the liver and digestive system are avoided; and the controlled, constant drug delivery profile (that is, controlled zero-order absorption). Also of importance is the reduced dose frequency compared to the conventional oral dosage forms (that is, once-a-day, twice-a-week or once-a-week). Other benefits include longer duration of therapeutic action from a single application, and reversible action. For example, patches can be removed to reverse any adverse effects that may be caused by overdosing. In order to evaluate the effects of vehicles and penetration enhancers on skin permeation of Indapamide, the skin permeation rates of Indapamide from vehicles of different composition were determined using Franz cells fitted with excised hairless skins. Solubility of Indapamide in various solvents was investigated to select a vehicle suitable for the percutaneous absorption of Indapamide, The solvents used were Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol. Lauroglycol90 increase the permeability of indapamide approximately 3.75-fold compared with the control. Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol showed flux of $0.06ug/cm^2/hr,\;0.4ug/cm^2/hr,\;0.21ug/cm^2/hr,\;0.72ug/cm^2/hr,\;0.29ug/cm^2/hr$, respectively.

• Applied Chemistry for Engineering
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• v.23 no.2
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• pp.222-227
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• 2012

In this study, nano-emulsion containing ethyl acetate fraction of Polygonum aviculare (P. aviculare) extract was prepared and skin permeability of the nano-emulsion was evaluated. Nano-emulsion was prepared using homogenizer and microfluidizer by the high-energy method. The droplet size and loading efficiency of nano-emulsion containing ethyl acetate fraction of P. aviculare extract were determined. The mean droplet size was 238 nm and the loading efficiency was more than 98%. The size distribution of nano-emulsion was a monodispersed form and nano-emulsion was more stable than that of using typical emulsion without using the microfluidizer. The in vitro skin permeation study of nano-emulsion containing ethyl acetate fraction of P. aviculare extract was carried out using Franz diffusion cells. Compared to 1,3-butylene glycol, nano-emulsion showed greater values of cumulative permeation of ethyl acetate fraction from P. aviculare extract. These results indicate that the stability and skin permeability of nano-emulsion containing ethyl acetate fraction of P. aviculare exerting anti-oxidative and anti-aging activities were enhanced.

• Journal of the Korean Applied Science and Technology
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• v.41 no.1
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• pp.1-8
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• 2024

The safety of cosmetic ingredients is considered paramount. In order to enhance safety, a novel preservative, PE-gal, was bio-synthesized by utilizing the Escherichia coli enzyme 𝛽-galactosidase on the conventional preservative 2-phenoxyethanold (PE). The skin absorption of the bio-synthesized product, PE-gal, intended for use in cosmetics, was evaluated for permeability using the Franz Diffusion Cell Assay system, comparing it with the conventinal preservative PE. When using samples of the same mass concentration, the Flux and Kp values of PE increased over time, indicating a gradual increase in permeability. However, PE-gal did not exhibit sufficient permeability to measure. This suggests that the skin permeability of PE is higher than that of the PE-gal saccharide. According to Marzulli et al., when confirming the degree of permeation using Kp values, the permeation rate of PE was measured as "slow" at a concentration of 1mg/mL. Thus, the transdermal permeability of the divedened form of PE-gal was significantly lower compared to PE.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.103-103
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• 1993

목적: Estroge 결핍으로 나타나는 폐경기의 주요 증상을 경감 치료하기 위해, estrogen경구 투여시 위장장애, 위장에서의 대사, 간 초회효과, 자주 투여로 인한 환자의 불편 등의 단점이 있나, 이러한 점을 개선하기 위한 투여경로의 하나로 피부를 통해 일정약물을 장기간 일정속도로 송달시키는 경피 흡수 시스템의 개발이 필요하다. 따라서 (EE)의 장기제어방출을 위해 ethylene vinyl acetate (EVA)를 사용하여 장기 제어방출 및 경피 흡수의 최적화 조건을 설정하여 경피흡수 시스템을 위한 막의 개방을 목적으로 한다. 방법: VA 함량이 18-40％까지의 EVA를 사용하여 EE를 함유한 matrix를 casting 방법으로 제조하고 변형된 Keshary-Chien cell을 이용하여 방출실험을 실행하였다. 이때 방출에 미치는 여러 가지 인자로서 EVA 주의 VA함량, 막의 두께, receptor 중 PEG 400의 용량비율, 방출 매개체의 온도, loading 된 약물의 량 등에 대해 검토하였다. 그리고 점개한 mouse skin에 대한 투과 실험을 행하고 이에 미치는 PEG 400과 자질층의 역할을 검토하였다. 결과: EE의 용해도는 saline so PEG 400의 용량 비율이 증가함에 따라 지수 함수적으로 증가하였다. 그리고 VA 함량이 증가될수록, PEG 400의 용량비율, 방출 매개체의 온도, loading 된 약물의 양이 증가될수록 PEG 400의 용량비율, 방출 매개체의 온도, loading 된 약물의 양이 증가될수록 EE의 방출속도와 부과속도는 증가하였다. 또한 투과속도는 막두께의 역수와 직선상의 상관 관계를 보였다. 그리고 EVA matrix로부터 EE가 방출되는 양상은 diffusion-controlled model을 따랐으며 이때 단위면적당 방출된 총량은 T에 비례되었다. 절개한 mouse skin을 통한 EE의 permeation은 PEG 400의 첨가에 의해 상승되었다. 이와 같이 EVA 막이 EE의 부과 및 방출을 조절하는 것으로 보아 경피 흡수를 위해 사용될 수 있다고 사료된다.

• Proceedings of the Membrane Society of Korea Conference
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• 1995.04a
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• pp.11-15
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• 1995

Polysulfone (PS) membranes were prepared by the phase inversion process using water or isopropanol as nonsolvent. The Flory-Huggins theory for a ternary system nonsolvent/solvent/polymer is applied to describe the thermodynamic equilibria of the components. The calculated ternary phase equilibria show that demixing of a PS binary solution with n-methylpyrrolidone (NMP) will be fast in a water coagulation bath and will be delayed in an isopropanol bath. The prepared membranes were characterized by SEM, gas adsorption-desorption measurement, and permeability test. The membrane, which is precipitated by fast demixing in a water bath, has nodular structures in the skin region and includes finger-like cavities in the sublayer. The membrane coagulated by isopropanol has a very dense and thick skin structure, which is formed by delayed demixing. The membrane coagulated by isopropanol showed considerably lower pore volume and surface area compared to that observed with water coagulation method. With dimethylformamide (DMF) as solvent and 2-3 wt% of water, the solution can show the liquid-liquid phase separation due to agglomation of the polymer-lean phase from the homogeneous solution. The membranes, which were coagulated near an equilibrium state, show the large (micron size) round pores in the whole membranes. The pores do not contribute the permeation characteristics.

• Journal of Pharmaceutical Investigation
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• v.34 no.4
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• pp.275-281
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• 2004

We have studied the effect of polarity, current density, current duration, crosslinking density, swelling ratio, and permeation enhancers on the transdermal flux of ketoprofen from acrylamide hydrogel. Hydrogel was prepared by free radical crosslinking polymerization of acrylamide. Drug loading was made just before transport experiment by soaking the hydrogel in solution containing drug. In vitro flux study using hairless mouse skin was performed at $36.5^{\circ}C$ using side-by-side diffusion cell, and the drug was analysed using HPLC/UV system. The result showed that, compared to passive flux, the total amount of drug transported increased about 18 folds by the application of $0.4\;mA/cm^2$ cathodal current. Anodal delivery with same current density also increased the total amount of drug transported about 13 folds. It seemed that the increase in flux was due to the electrorepulsion and the increase in passive permeability of the skin by the current application. Flux increased as current density, the duration of current application and loading amount (swelling duration) increased. As the cross linking density of the hydrogel increased, flux clearly decreased. The effect of hydrophilic enhancers (urea, N-methyl pyrrolidone, Tween 20) and some hydrophobic enhancers (propylene glycol monolaurate and isopropyl myristate) was minimal. However, about 3 folds increase in flux was observed when 5% oleic acid was used. Overall, these results provide some useful information on the design of an optimized iontophoretic delivery system of ketoprofen.

• Archives of Pharmacal Research
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• v.24 no.6
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• pp.578-583
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• 2001

To investigate the feasibility of developing a new tenoxicam plaster, the effects of vehicles and penetration enhancers on the in vitro permeation of tenoxicam from a pressure-sensititre adhesive (PSA) matrices across the dorsal hairless mouse skin were studied. Vehicles employed in this study were propylene glycol (PC)-oleyl alcohol (OAI), PG-oleic acid (OA), and diethylene glycol monoethyl ether (DCMI)-propylene glycol monolaurate (PCML) cosolvents with/without fatty acids. In this studys amines such as triethanolamine (TEA) and tromethamine (TM) were additionally used as a solubilized. Among PSAs used, $Duro-Tak^{\circledR}$87-2510 showed much higher release rate than either $Duro-Tak^{\circledR}$ 87-2100 or $Duro-Tak^{\circledR}$87-2196. The relatively high flux rate was obtained with the formulation of DCMI-PCML (40:60, v/v) with 3% OA and 5% TM, and the flux increased as a function of the dose;the initial flux up to 12 h was $4.98{\pm}1.38{\;}{\mu\textrm{g}}/{\textrm{cm}^2}/h$ at the tenoxicam dose of $50{\;} mg/70{\;}{\textrm{cm}^2}$. This flux was much higher than that of a commercial piroxicam patch ($Trast^{\circledR}$) ($1.24{\pm}0.73{\;}{\mu\textrm{g}}/$\textrm{cm}^2/hr$) with almost only one-third that of the commercial patch. Therefore, these observations indicated that these composition of tenoxicam plaster may be practically applicable.

• Membrane Journal
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• v.22 no.3
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• pp.224-233
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• 2012

To improve permeation performance of gas separation membrane, polysulfone hollow fiber membrane was prepared by wet-dry phase inversion method using Triton X-100 as non-ionic additive. And variation of gas permeation behavior by additive was investigated. Various spinning conditions such as air gap, concentration of polymer, dope tank temperature were controlled and these effects were studied. The morphology and gas permeation property of hollow fiber membranes were investigated using scanning electron microscope (SEM) and bubble flow meter respectively. We confirmed that the membranes added with Triton X-100 had a smooth external skin at various air gap length conditions. The macrovoids of these hollow fiber membranes were more developed with increase of air-gap from 4 to 90 cm and that induced higher permeance. The permeance of polysulfone membranes has the higher value at comparatively lower concentration polymer (30 wt% polysulfone) and lower concentration of additive (15 wt% Triton X-100). When temperature in dope tank was controlled, the membranes prepared at $100^{\circ}C$ showed low permeance because of volatilization of additive and solvent.

• Journal of the Korean Applied Science and Technology
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• v.37 no.6
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• pp.1738-1751
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• 2020

The skin is divided into three parts: the epidermis, the dermis, and the subcutaneous fat, and the stratum corneum, which is located at the top of the epidermis, acts as a barrier that prevents drug delivery. Nanoemulsions are known to be effective in transdermal delivery of drugs through intercellular lipids because of their unique small particle size. In this study, phase inversion temperature (PIT) nanoemulsion containing α-bisabolol was optimized using response surface methodology (RSM) for effective skin absorption of α-bisabolol. As a preliminary experiment, the 25-2 fractional factorial design method and the 23 full factorial design method were performed. Box-Behnken design was performed based on the results of the factorial design method. The content of surfactant (6.3~12.6%), co-surfactant (5.2~7.8%) and α-bisabolol (0.5~5.0%) were used as factors, and the dependent variable was the particle size of the nanoemulsion. PIT nanoemulsion optimization was performed according to the RSM results, and as a result, the optimal nanoemulsion formulation conditions were predicted to be 10.4% surfactant content, 6.3% co-surfactant content, and 5.0% α-bisabolol content. As a result of the skin absorption test, the final skin absorption rate of the PIT nanoemulsion was 35.11±1.01%, and the final skin absorption rate of the general emulsion as a control was 28.25±1.69%, confirming that the skin absorption rate of the PIT nanoemulsion was better.