• Journal of Pharmaceutical Investigation
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• v.35 no.6
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• pp.403-409
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• 2005

For transdermal delivery of large molecular drugs such as vaccine and protein drugs, novel microneedle treatment device with roll was designed. The roll dimension is 1.43 cm diameter and 2.8 cm perimeter. Total number of microneedle on the roll is 3,360 with $230\;{\mu}m$ height and $740\;{\mu}m$ distance. The pore with $150\;{\mu}m$ depth and $35\;{\mu}m$ diameter on the skin was made by the designed microneedle device. This system could be achieved without pain. The permeation rates of FITC labelled ovalbumin (FITC-OVA, molecular weight: 45,000 g/mol) as a model protein were determined by modified Franz diffusion cells using skins of hairless mice or SD rats which were treated by using microneedle device two or four times. The average penetration fluxes of model protein increased from 674 to $872\;{\mu}g/cm^{2}{\cdot}hr$ as the number of treatment to make pore increased from two to four times. In conclusion, we confirmed the possibility of using the designed microneedle treatment device for transdermal delivery of the large molecular drugs.

• Journal of the Korean Applied Science and Technology
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• v.27 no.4
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• pp.407-414
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• 2010

New biological treatments were being developed at a record place, but their potential could be compromised by a significant obstacle: the delivery of these drugs into a body. Pharmaceutical delivery is now nearly as important as product. New systems are being developed, and Drug Delivery Markets Series cover these new systems. Transdermal Delivery System(TDS) is often used as a method of drug dosage into the epidermic skin. An approach used to delivery drugs through the skin for therapeutic use as an alternative to oral, intravascular, subcutaneous and transmucosal routes. Various transdermal drug delivery technologies are described including the use of suitable formulations, carriers and penetration enhancers. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other methods of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharides, such as karaya gum and glucomannan, were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, drug contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in fibric acid(ciprofibrate) such as lipophilic drug in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate. Especially, this result suggests a possible use of polysaccharide gel ointment matrix as a transdermal delivery system of anti-hyperlipoproteinemic agent.

• Journal of Pharmaceutical Investigation
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• v.38 no.4
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• pp.223-228
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• 2008

The purpose of this study was to investigate the feasibility of developing transdermal drug delivery system (TDDS) for fentanyl used for the management of chronic cancer pain. The effect of type of pressure sensitive adhesive on the permeation of fentanyl from polyisobutylene (PIB), silicone and acrylic adhesive was evaluated. Due to the good adhesive force and relatively steady flux for 3 days, both acrylic and PIB adhesives were chosen for further study. The permeation rate of fentanyl was the highest from acrylic adhesive with hydroxyl functional group. Permeation rate increased linearly as the concentration of fentanyl in acrylic adhesive was increased from 2.5% to 10%. In case of PIB adhesive, crystals of fentanyl were developed above 5% drug load. $Crovol^{(R)}$ A40, $Crovol^{(R)}$ PK40 and Plurol $oleique^{(R)}$ provided higher flux of fentanyl.

• Archives of Pharmacal Research
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• v.27 no.3
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• pp.351-356
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• 2004

A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol: ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.

• Journal of Pharmaceutical Investigation
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• v.37 no.6
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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.

• Journal of Pharmaceutical Investigation
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• v.39 no.3
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• pp.177-183
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• 2009

A rapid and sensitive reversed-phase high performance liquid chromatography (HPLC) method was developed for the determination of piroxicam in the rabbit plasma. After a treatment of plasma sample by liquid-liquid extraction, the drug was analyzed on an HPLC system with ultraviolet detection at 330 nm. HPLC was carried out using reversed-phase isocratic elution with a C18 column, a mobile phase of a mixture of acetonitril, doubly deionized water and acetic acid 43.74:56.00:0.26 v/v%) at a flow rate of 1.1 mL/min. The chromatograms showed good resolution and sensitivity and no interference of plasma. The calibration curve for the drug in plasma sample was linear over the concentration range of 0.01-2.0 ${\mu}$g/mL. The intra- and inter-day assay accuracies of this method ranged from 86.82% to 108.33% of normal values and the precision did not exceed 13% of relative standard deviation. The plasma concentration of piroxicam decreased to below the quantifiable limit at 12 hr after the i.v. bolus administration to rabbits following dose of 0.375 mg/kg yielding a apparen t plasma half life of 1.38 hr. The transdermal route prolongs plasma levels of piroxicam. The bioavailability, calculated from the dose-adjusted ratio of the $AUC_{transdermal}$ to the $AUC_{i.v.}$, was 7.44%. The plasma concentration of piroxicam was detected by 48 hr after the transdermal administration of patch at a dose of 32 mg/kg. This method was suitable for cutaneous absorption studies of piroxicam in the rabbit after transdermal administration of different types of dosages of the drug.

• Journal of the Korean Applied Science and Technology
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• v.29 no.4
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• pp.552-560
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• 2012

Drug delivery technologies are patent protected formulation technologies that modify drug release profile, absorption, distribution, and elimination for the benefit of improving product efficacy and safety, as well as patient convenience and compliance. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stop if the drug dosage lead to side effect. Polysaccharide, such as karaya gum and locust bean gum(LBG)/water-soluble chitosan oligomer(WSCO) were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, tacrine contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in tacrine such as lipophilic drug in vitro. We used glycerin, PEG 400, and PEG 800 as enhancers. Therefore, transdermal absorption of tacrine could be improved by changing vehicle composition or by using penetration enhancers. Especially it would be anticipated that the high permeation efficacy could be obtained by using vehicle that has enhancing effect for itself and by adding enhancers to it.

• Journal of the Korean Chemical Society
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• v.37 no.5
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• pp.527-536
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• 1993

The characteristics of the controlled drug release were studied for biodegradable transdermal drug delivery system. A biodegradable polymeric matrix was prepared from chitosan, silver sulfadiazine, and glycerine. The release behavior of silver sulfadiazine from chitosan matrix was consistent with the Higuchi's diffusion controlled model. The release time was delayed by increasing the content of silver sulfadiazine and thickness of the matrix, whereas decreased as glycerine concentration increased. The apparent constant (K) of release rate was proportional to the content of drug or glycerine and the thickness of chitosan matrix. These results indicated that chitosan matrix shows some potential as a drug delivery system for transdermal therapeutic application.

• Archives of Pharmacal Research
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• v.18 no.4
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• pp.224-230
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• 1995

Recently, many attempts have been made to use hydrogels of various polymers as delivery systems of various drugs and bioactive materials to prolong and control their phamacological activities. In this study, we have evaluated the physico-chemical properties of methacrylic acid-methyacrylic acid methyl ester copolymer 9Eudispert mv)m a acrylic resin hydorgel, and its application to transdermal delivery system. In the dissolution tests, the release rate of salicylic acid (SA) and sodium salicylate (SOd. SA) were faster than lidocain (LD) and lidocain-HCl(LD-HCl). As the concentration of Eudispert mv polymer increased, the extensibility of Eudispert mu hydrogel decreased, whereas the swelling ratio increased. The more NaOH and polymer concentration increased, the more osmotic pressure linearly increased. The skin permeation of Sod. SA, an acidic model drug, was remarkably enhanced by Eudispert mv hydrogel. All fatty acids, except for Sod. glycolate, dramatically increased the skin permeation flux in Eudispert mu hydrogel containing LD-Hcl, a basic model drug. Consequently, it is suggested that Eudispert mv hydrogel may be used as potential transdermal delivery vehicle.

• Journal of Pharmaceutical Investigation
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• v.29 no.1
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• pp.29-36
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• 1999

Aceclofenac is an non-steroidal antiinflammatory drug which has been used in the treatment of rheumatoidal rthritis and osteo-arthritis. In order to decrease the gastric ulcerogenic effects and contol the plasma level of aceclofenac, we have developed the transdermal delivery system of aceclofenac plaster, which were formulated employing matrix polymers of acrylates and penetration-enhancers such as $Lauroglycol^{\circledR}$, $Transcutol^{\circledR}$, oleic acid and linoleic acid. Using Franz diffusion cells mounted with a rat skin, transdermal penetration characteristics of the formulations were evaluated by the HPLC assay of aceclofenac and diclofenac, an active metabolite, in the receptor compartment of pH 7.2 phosphate buffered solution. Skin penetration was increased when the content of aceclofenac increased, showing the flux $(J,\;{\mu}g/cm^2/hr)$ of 0.37 and 2.50 for 2% and 6.75% of the content, respectively. The flux$(J,\;{\mu}g/cm^2/hr)$ from plasters made of $Durotak^{\circledR}$ 87-2074, $Durotak^{\circledR}$ 87-2510 and $Durotak^{\circledR}$ 87-2097 were 2.50, 2.77 and 4.39, respectively. $Durotak^{\circledR}$ 87-2074 showed the lowest penetration due to the carboxylic acid group in the polymer, which might form a strong hydrogen bonding with a secondary amine of aceclofenac. Although both $Durotak^{\circledR}$ 87-2510 and $Durotak^{\circledR}$ 87-2097 are amine-resistant adhesives, $Durotak^{\circledR}$ 872510 showed lower penetration than $Durotak^{\circledR}$ 87-2097 because of the hydroxyl group in $Durotak^{\circledR}$ 87-2510, which might form a weak hydrogen bonding with aceclofenac. These results reveal that the functional group in acrylic polymers would greatly affect the release of aceclofenac from the matrix, which is the rate-limiting step in the penetration of aceclofenac through rat skins. The penetration of aceclofenac from plasters using different penetration-enhancers increased in the following order: Transcutol < linoleic acid < oleic acid. And the flux from the plasters containing oleic acid as a penetrationenhancer was 2.22 times greater than that of creams, which suggest that a newly deveolped aceclofenac plaster could be used in the treatment of rheumatoidal arthritis and osteo-arthritis as an advanced transdermal delivery system.