• 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.

• The Journal of Korean Physical Therapy
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• v.13 no.3
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• pp.719-726
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• 2001

Transdermal drug delivery offers various advantages over conventional drug delivery systems, such as avoidance gastrointestinal degradation and hepatic first-pass effect. encourages patient compliance. and possible sustained release of drugs. However, transdermal transport of drugs is low permeability of the stratum corneum, the superficial layer of the skin. Many physicochemical and biological factors influencing transdermal transport is described together with the corresponding experimental and clinical results. Phonophoresis is medical treatment with drugs introduced into the skin by ultrasound energy. Enhanced drug penetration is through to result from the biophysical alterations of skin structure by ultrasound waves. The frequency used for phonophoresis is usually from 20 kHz to 15MHz. Phonophoresis can be categorized in to three ranges: low-frequency range(below 1 MHz). therapeutic frequency range(1 to 3MHz), and high-frequency range(above 3 MHz). The depth of penetration of ultrasound into skin is inversely proportional to the frequency. Cavitation may cause mechanical stress. temperature elevation, or enhanced chemical reactivity causing drug transport. One theory is that ultrasound affects the permeation of the stratum corneum lipid structure as the limiting step in permeating through the skin. The range of indications for phonophoresis is wide. Aspecific classification of the range of indications is obtained by classification of pathological conditions. The continuous research is needed for many interesting issucs of phonophoretic transdermal delivory in new future.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.37 no.2
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• pp.97-119
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• 2011

World consumers are now focusing on their health, well-being and appearance more than ever before. This trend is creating heightened demand for products formulated as cosmeceuticals with active ingredients. A significant number of innovative formulations are now being used in cosmetics with real consumer-perceivable benefits and optimized sensory attributes, resulting in an economic uplift of cosmetic industry. To obtain skin care formulations with real consumer-perceivable benefits through dermal delivery of active ingredients, formulators are resorting to technology that until recently was used in pharmaceutical products. These various delivery systems are now being used in cosmecuetical formulations. Novel delivery systems reviewed here possess enormous potential as next-generation smarter carrier systems.

• 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.30 no.4
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• pp.247-252
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• 2000

The advantages of transdermal administration are avoiding hepatic first pass effect, minimizing inter- and intra-patient variation, maintaining steady-state plasma level to provide long-term therapy from a single dose, and allowing a rapid termination of drug input. Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease. For the development of transdermal systems containing clenbuterol, two limiting factors - long lag time and low flux - must be overcome. In this study, we attempted to select optimal formulation for preparation of clenbuterol patch using hairless mouse skin and flow-through diffusion cell. The flux of clenbuterol increased as the percent of clenbuterol dose dependently in the concentration range of 5-15%. Based on this result, we fixed the concentration of clenbuterol as 15%. The effect of various penetration enhancers on percutaneous absorption of clenbuterol through hairless mouse skin was investigated. Labrafil was the most effective enhancer, which increased the permeability of clenbuterol approximately 4-fold compared with the control without penetration enhancer. Optimal enhancer concentration was 3%. The effect of various adhesives on penetration of clenbuterol was also investigated. Among the adhesives studied, MA-31 was the most effective adhesive. Furthermore, the clenbuterol patch composed of 15% clenbuterol, 3% Labrafil and 82% MA-31, which gave most excellent penetration of drug in in vitro penetration study, maintained therapeutic plasma levels in in vivo study using S.D. rats. These studies demonstrated a good feasibility of clenbuterol administration through the intact skin using a transdermal patch, and show a possibility of the development of clenbuterol patches.

• Archives of Pharmacal Research
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• v.28 no.9
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• pp.1097-1102
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• 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.

• Journal of Pharmaceutical Investigation
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• v.32 no.4
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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 Microscopy
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• v.40 no.4
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• pp.185-191
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• 2010

Short peptides are potentially effective materials as cosmeceuticals, but their delivery across the skin can be problematic due to the ionic nature of peptides and the structure of the skin. For short peptide to be utilized as cosmeceuticals, its ability to penetrate the skin must be altered. In this study, we conjugated the widely used procollagen type I signal peptide, KTTKS, with oleic acid to improve the lipophilic properties of the peptide, and used the oleic acid-conjugated peptides to construct cosmeceutical nanosomes. Then we examined the penetration of cosmeceutical nanosomes prepared from isotope-labeled peptide into the skin after transdermal application using autoradiography. Because of its hydrophilic property of penta-peptide, the penta-peptide itself was not able to be penetrated through the stratum corneum of the skin. In contrast, nanosomes made from olecic acid conjugated penta-peptide were able to be penetrated through the stratum corneum effectively. Autoradiography showed the precise penetration points to dermal layer, demonstrating the appropriateness of this method for clarifying the mechanism of penetration of transdermal delivery systems.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.38 no.2
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• pp.147-154
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• 2012

In this study, we prepared elastic liposome containing rutin, known as antioxidants, and evaluated the physical characterization and enhanced skin permeation effect. The elastic liposome was prepared using the different ratios of egg phospholipids and $Tego^{(R)}$ care 450. The mean diameter of rutin loaded elastic liposomes formulations ranged between 205.7 ~ 298.0 nm and deforability 20.9 ~ 42.5, The loading efficiency was observed to be 52.0 ~ 71.0 %. The highest loading efficiency (71.0 %) and deformability (42.5) were observed at the optimal ratio of 85 : 15 (egg phospholipids : $Tego^{(R)}$ care 450) in the 0.1 % rutin loaded elastic liposome formulations. The elastic liposome formulation was selected for further transdermal permeation study. The elastic liposome(129.9 ${\mu}g/cm^2$) exhibited a significantly higher skin permeation compared with general liposome (98.0 ${\mu}g/cm^2$) and 1,3-butylene glycol (76.3 ${\mu}g/cm^2$) solution. These results suggest that the elastic liposome formulation using $Tego^{(R)}$ care 450 as a major edge activator could be useful for the delivery of active ingredient through the skin barrier.

• Journal of Pharmaceutical Investigation
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• v.37 no.2
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• pp.85-94
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• 2007

The objective of this study is to prepare a stable delivery systems containing polyethoxylated retinamide(PERA) - derivatives of retinoic acid, effective anti-wrinkle and anti-acne agent. Cubic liquid crystalline phase gel (CLCPG) and cubosomes containing various concentrations of PERA were prepared to investigate the physicochemical properties. Furthermore, stability and transdermal absorption efficacy of the CLCPG containing PERA were investigated in comparison with oil-in-water (O/W) emulsions which are predominantly used as a topical formulation. CLCPG increase the stability of PERA in comparison with O/W emulsion. For tropical application, CLCPG containing PERA shows higher moisturizing effect than that of O/W emulsion. In skin permeation test, CLCPG shows higher PERA deposit on epidermis. With its specific physicochemical property caused by the glyceryl oleate, CLCPG itself could be used for stabilizer of various actives and applied as an effective delivery system for topical application. Cubosome, nano-sized dispersed CLCPG, is also expected to be applied in a various field of industry like food, cosmetics and pharmaceuticals.