• Polymer(Korea)
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• v.37 no.3
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• pp.347-355
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• 2013

In this study, the porous cellulose hydrogel as a carrier to enhance the skin delivery of quercetin and its glycoside, rutin known as flavonoid antioxidants was prepared and its properties were investigated. The optimum cellulose hydrogel for quercetin and rutin was made by the reaction of 2 wt% cellulose with 12% ECH. In the release test of the hydrogel containing the flavonoids, the release of quercetin was diffusion-controlled at $10{\sim}500{\mu}M$, but rutin was released by the erosion of hydrogel system at $10{\sim}50{\mu}M$. Both the encapsulation efficiency and release amount of rutin in hydrogel were higher than quercetin. However, in skin permeation experiment using Franz diffusion cell, quercetin showed higher skin permeation capacity than rutin. The hydrogel containing flavonoids showed remarkable transdermal permeation than the control group. These results suggest that porous cellulose hydrogel is potential drug delivery system to enhance transdermal permeation of water-insoluble flavonoid antioxidants.

• 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.

• Journal of the Korean Applied Science and Technology
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• v.17 no.1
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• pp.43-48
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• 2000

Drug delivery system(DDS) applied to various fields, such as medicine, cosmetics, agriculture and necessities of life. Among these application fields, DDS is often used as the method of drug dosage into the epidermic skin. We investigated characters of transdermal therapeutic system(TTS) and the skin permeability of that with applying DDS. Chitosan was selected as material of TTS. We investigated the permeation of chitosan ointment containing drug in rat skin using horizontal membrane cell model. Permeation properties of materials were investigated for water-soluble drug such as riboflavin in vitro. We used glycerin, PEG 600 and oleic acid as enhancers. Since dermis has more content water(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when glycerin was used in water-soluble drug. The permeation rate of content enhancer and drug was found to be faster than that of content water-soluble drug only. These results showed that skin permeation rate of drug across the composite was manly dependent on the property of ointment base and 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.

• Archives of Pharmacal Research
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• v.24 no.6
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• pp.572-577
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• 2001

The feasibility of skin penetration was studied for aspalatone (AM, acetylsalicylic acid maltol ester), a novel antithrombotic agent. In this studys hairless mouse dorsal skins were used as a model to select composition of vehicle and AM. Based on measurements of solubility and partition coefficient, the concentration of PC that showed the highest flux for AM across the hairless mouse skin was found to be 40%. The cumulative amount permeated at 48 h, however, appear inadequate, even when the PC concentration was employed. To identify a suitable absorption enhancer and its optimal concentration for AM, a number of absorption enhancers and a variety of concentration were screened for the increase in transdermal flux of AM. Amongst these, linoleic acid (LOA) at the concentration of 5% was found to have the largest enhancement factor (i.e., 132). However, a further increase in AM flux was not found in the fatty acid concentration greater than 5%, indicating the enhancement effect is in a bell-shaped currie. In a study of the effect of AM concentration on the permeation, there was no difference in the permeation rate between 0.5 and 1% for AM, below its saturated concentration. At the donor concentration of 2%, over the saturated condition, the flux of AM was markedly increased. A considerable degradation of AM was found during permeation studies, and the extent was correlated with protein concentrations in the epidermal and serosal extracts, and skin homogenates. In rat dorsal skins, the protein concentration decreased in the rank order of skin homogenate > serosal extract > epidermal extract. Estimated first order degradation rate constants were $6.15{\pm}0.14,{\;}0.57{\pm}0.02{\;}and{\;}0.011{\pm}{\;}0.004{\;}h^{-1}$ for skin homogenate, serosal extract and epidermal extract, respectively. Therefore, it appeared that AM was hydrolyzed to some extent into salicylmaltol by esterases in the dermal and subcutaneous tissues of skin. taken together, our data indicated that transdermal delivery of AM is feasible when the combination of PC and LOA is used as a vehicle. However, since AM is not metabolically stable, acceptable degradation inhibitors may be nervessary to fully realize the transdermal delivery of the drug.

• Journal of Pharmaceutical Investigation
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• v.33 no.1
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• pp.21-28
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• 2003

Ketorolac tromethamine(KT) is a nonsteroidal agent with potent analgesic and moderate anti-inflammatory activity. The lipid-water partition coefficient of KT was evaluated and KT gel was formulated as a gel containing different pH, different concentrations of polymer (poloxamer 407, carbopol 941), propylene glycol, ethanol and various enhancers. The resulting KT gels were evaluated with respect to their viscosity, in vitro drug permeation rate through hairless mouse skin and stability. In n-octanol and chloroform, the lipid-water partition coefficient of KT was the highest at pH 4 phosphate buffer. The apparent viscosity of KT gel increased with an increase in gel pH, polymer and enhancer concentration. But the apparent viscosity of KT gel decreased with an increase in ethanol concentration. The permeation rate of KT through hairless mouse skin from gels different pH was maximum at pH 4 which is close to KT $pK_{a}$ 3.54. The permeation rate decreased with an increase in polymer, propylene glycol concentration. But the permeation rate increased with an increase in ethanol. The increase of drug concentration from 1 to 3% induced linear increase in permeation rate. The best enhancer was the combination of $Labrasol^{\circledR},\;Transcutol^{\circledR}$, oleic acid and l-menthol. In the accelerated stability test(25, 40 and $50{\circ}C$), pH 5 gel was most stable and pH 4 gel was most unstable for 90 days.

• Polymer(Korea)
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• v.38 no.3
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• pp.391-396
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• 2014

Polymer microneedles can be fabricated by a micromolding method, an easy and cost-effective method. However, it is not easy to achieve uniform coating with an aqueous coating solution due to hydrophobic surface of polymer microneedles. 3-Dimensional coating polymer microneedles could deliver more than twice as much dose as in-plane metal microneedles by increasing coating area and the number of microneedles per unit area. A uniform coating was not obtained by addition of coating additives in the coating solution. The satisfied coating was achieved by treatment of surface of polymer microneedle with metal deposition and UV/ozone, and UV/ozone treatment was an ultimate surface treatment method based on biological safety. Calcein coating polymer microneedles were prepared by using UV/ozone treatment and followed dip-coating, and they delivered calcein in porcine skin successfully after 15 min of insertion.

• Korean Chemical Engineering Research
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• v.59 no.3
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• pp.429-434
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• 2021

The feasibility of lecithin as a material for dissolving microneedles to improve skin permeability of drugs and the effect of the composition of lecithin on the mechanical strength, solubility, and skin permeability of rhodamine B (RhB) of the dissolving microneedles were investigated. Dissolving microneedles with needles of uniform shape and size were fabricated with the mold made using the laser-writing technique, simpler and more efficient method compared to the photolithography method, the conventional method to fabricate the microneedle mold. The composition of lecithin in the microneedle affected the mechanical strength and solubility of the needle thus, the mechanical strength of the needle increased as the composition of lecithin in the needle increased, resulting in improving the skin permeability of RhB contained in the microneedles. When comparing the microneedles containing same composition of amylopectin (AP), the skin permeability of RhB of the microneedles containing lecithin was higher. These results indicate that lecithin can be used as a material for dissolving microneedles and the skin permeability of the microneedle could be controlled by changing the composition of lecithin.

• Polymer(Korea)
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• v.38 no.5
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• pp.676-681
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• 2014

Licorice, widely used as a herbal medicine, has flavonoids such as liquiritin and its aglycone, liquiritigenin that show anti-oxidant and anti-inflammatory properties. Licorice flavonoid-loaded cellulose hydrogels were prepared as carriers for skin drug delivery, and their properties were investigated. The porous cellulose hydrogel was made by reacting cellulose with epichlorohydrin as a cross-linking agent in NaOH/urea(1~10%) solutions. Through studies on the rheological properties and water uptake of the hydrogel, a NaOH/urea(6%) solution was established as being optimum for the synthesis of the cellulose hydrogel containing liquiritin and liquiritigenin. Scanning electron microscopy (SEM) observations of a cross-section of the prepared hydrogel indicated its porosity. In particular, in skin permeation experiments using a Franz diffusion cell, hydrogel containing the licorice flavonoids showed remarkable transdermal permeation compared to the control group. These results indicate that porous cellulose hydrogel is a potential drug delivery system to enhance the skin permeation of licorice flavonoids.

• Applied Chemistry for Engineering
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• v.34 no.2
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• pp.161-169
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• 2023

In this study, we prepared naproxen (NP) imprinted biodegradable polymer based multi-layer biomaterials using allbanggae starch (ABS), polyvinyl alcohol (PVA), and alginic acid (SA), and investigated their physicochemical properties and the controlled drug release effects. In addition, the prepared multi-layer biomaterials were characterized by FE-SEM and FT-IR. In order to confirm the controlled drug release effect for the transdermal drug delivery system (TDDS), the NP release properties of NP imprinted multi-layer biomaterials were investigated using various pH buffer solutions and artificial skin at 36.5 ℃. The results of NP release in various pH buffer solutions indicated that the NP release at high pH was about 1.3 times faster than that at low pH. In addition, NP release in multi-layer biomaterials was about 4.0 times slower than that in single-layer biomaterials. It was confirmed that the NP release rate in triple-layer biomaterials was 4.0 times slower than that in single-layer biomaterials while using artificial skin. Also, it could be found that NP in double-layer biomaterials and triple-layer biomaterials was released sustainably for 12 h. The NP release mechanism in pH buffer solutions followed the Fickian diffusion mechanism, but followed the non-Fickian diffusion mechanism with artificial skin.

• Journal of the Korean Society of Combustion
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• v.11 no.4
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• pp.9-13
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• 2006

Recent advances in energetic materials modeling and high-resolution hydrocode simulation enable enhanced computational analysis of bio-medical treatments that utilize high-pressure shock waves. Of particular interest is in designing devices that use such technology in medical treatments. For example, the generated micro shock waves with peak pressure on orders of 10 GPa can be used for treatments such as kidney stone removal, transdermal micro-particle delivery, and cancer cell removal. In this work, we present a new computational methodology for applying the high explosive dynamics to bio-medical treatments by making use of high pressure shock physics and multi-material wave interactions. The preliminary calculations conducted by the in-house code, GIBBS2D, captures various features that are observed from the actual experiments under the similar test conditions. We expect to gain novel insights in applying explosive shock wave physics to the bio-medical science involving drug injection. Our forthcoming papers will illustrate the quantitative comparison of the modeled results against the experimental data.