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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
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Journal of Pharmaceutical Investigation
Journal Basic Information
Journal DOI :
The Korean Society of Pharmaceutical Sciences and Technology
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Volume & Issues
Volume 41, Issue 6 - Dec 2011
Volume 41, Issue 5 - Oct 2011
Volume 41, Issue 4 - Aug 2011
Volume 41, Issue 3 - Jun 2011
Volume 41, Issue 2 - Apr 2011
Volume 41, Issue 1 - Feb 2011
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Succinylated Pullulan Acetate Microspheres for Protein Delivery
Woo, Young-Rong ; Seo, Seog-Jin ; Na, Kun ;
Journal of Pharmaceutical Investigation, volume 41, issue 6, 2011, Pages 323~329
DOI : 10.4333/KPS.2011.41.6.323
In order to develop new protein carrier replacing poly(DL-lactic acid-co-glycolic acid) (PLGA) microspheres, succinylated pullulan acetate (SPA) was investigated to fabricate a long term protein delivery carrier. SPA microspheres loaded with lysozyme (Lys) as a model protein drug were prepared by a water/oil/water (W/O/W) double emulsion method. An acidity test of SPA copolymers after hydrolysis was performed to estimate the change of protein stability during releasing proteins from the microspheres. There was no pH change of SPA copolymers, but pH of PLGA polymers after hydrolysis was significantly decreased to around pH 2, indicating that the long-term stability of proteins released from SPA microspheres can be guaranteed. Loading efficiency of proteins into SPA microspheres was three times higher than those into conventional PLGA microspheres, indication of inducing stronger charge interaction between proteins and succinyl groups in SPA microspheres. Although initial burst behaviors were monitored in Lys-loaded SPA microspheres due to relatively strong hydrophilic succinyl segments in SPA microspheres, initial burst issues would be circumvented if the ratio of charge density of succinyl moieties and hydrophobic acetate groups is harmonically controlled. Therefore, in this study, a new attempt of protein delivery system was made and functional SPA was successfully confirmed as a new protein carrier.
Enhanced Aqueous Stability of Hirsutenone with Antioxidant
Moon, Ki-Young ; Ahn, Byeong-Kil ; Lee, Sang-Gon ; Lee, Seo-Hyun ; Yeom, Dong-Woo ; Choi, Young-Wook ;
Journal of Pharmaceutical Investigation, volume 41, issue 6, 2011, Pages 331~336
DOI : 10.4333/KPS.2011.41.6.331
The instability of hirsutenone (HST), a potential therapeutic candidate for the treatment of atopic dermatitis (AD) and ovarian carcinoma, is one of the main concerns for the development of drug product. In the present study, aqueous stability of HST was investigated by kinetic analysis, and the effect of several factors covering temperature, nitrogen gas (
) flushing, and selection of proper antioxidant was compared. Cosolvent system composed of distilled water and methanol (9:1 v/v) was used as a vehicle to dissolve HST at the concentration of
. Samples of aqueous solution were prepared under the absence or presence of antioxidants, such as ascorbic acid (AA), sodium edetate (EDTA), and ascorbyl palmitate (AP), and subjected for stability test. The degradation of HST in aqueous solution was followed by the first order kinetics with an extremely short half life of less than a week at room temperature, and was accelerated as the temperature increased.
flushing brought a little enhancement in stability compared to control solution, but the effect was insufficient. The addition of AA and EDTA (0.1%) significantly enhanced the stability of HST at
, but the addition of AP (0.01%) was limited due to its water insolubility and revealed no promising result. The stability of HST was increased proportionally by the amount of AA added, showing the difference in degree of stabilization as an order of magnitude. Finally, we conclude that HST was stabilized by the addition of a suitable antioxidant, suggesting AA as the most effective stabilizer.
Iontophoretic Transport of Donepezil Hydrochloride through Skin: Flux Enhancement by Chemical Enhancer and Iontophoresis
Oh, Seaung-Youl ;
Journal of Pharmaceutical Investigation, volume 41, issue 6, 2011, Pages 337~345
DOI : 10.4333/KPS.2011.41.6.337
The objective of this work is to investigate the effect of chemical enhancer and current on the flux of donepezil hydrochloride (DH) through skin. Ethanol and N-methyl pyrrolidone (NMP) were used as chemical enhancers in combination with iontophoresis. We also have studied the effect of pH on flux and evaluated the role of electroosmosis. In vitro flux study was performed at
, using side-by-side diffusion cell and full thickness hairless mouse skin. Passive flux of DH without enhancer was very small. As the concentration of enhancer increased, passive flux increased. After current application, flux increased markedly and the time to reach maximum decreased. Without enhancer, maximum flux was about 50 fold larger than that obtained without current. These results indicate that electromigration is playing a major role for the transport. As the enhancer concentration increased, flux also increased. NMP and ethanol increased not only the passive delivery, but also the iontophoretic delivery. Flux results indicate that ethanol has better ability than NMP in enhancing the transport of DH. The magnitudes of increase in flux by these enhancers indicate that there is a large synergistic effect in flux enhancement. Flux results from pH study showed that electroosmotic flow is reversed at low pH and the flux is hindered. These results provided some information on the flux enhancing ability of ethanol and NMP in combination with iontophoresis. The data also provided some mechanistic insights into the role of electromigration and electroosmosis on flux through skin.
Controlled Transdermal Delivery of Loxoprofen from an Ethylene-Vinyl Acetate Matrix
Ryu, Sang-Rok ; Shin, Sang-Chul ;
Journal of Pharmaceutical Investigation, volume 41, issue 6, 2011, Pages 347~354
DOI : 10.4333/KPS.2011.41.6.347
Repeated oral administration of loxoprofen can induce many side effects such as gastric disturbances and acidosis. Therefore, we considered alternative routes of administration for loxoprofen to avoid such adverse effects. The aim of this study was to develop an ethylene-vinyl acetate (EVA) matrix system containing a permeation enhancer for enhanced transdermal delivery of loxoprofen. The EVA matrix containing loxoprofen was fabricated and the effects of drug concentration, temperature, enhancer and plasticizer on drug release were studied from the loxoprofen-EVA matrix. The solubility of loxoprofen was highest at 40% (v/v) PEG 400. The release rate of drug from drug-EVA matrix increased with increased loading dose and temperature. The release rate was proportional to the square root of loading dose. The activation energy (Ea), which was measured from the slope of log P versus 1000/T, was 5.67 kcal/mol for a 2.0% loaded drug dose from the EVA matrix. Among the plasticizer used, diethyl phthalate showed the highest release rate of loxoprofen. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the greatest enhancing effect. In conclusion, for the enhanced controlled transdermal delivery of loxoprofen, the application of the EVA matrix containing plasticizer and penetration enhancer could be useful in the development of a controlled drug delivery system.
Protective Effects of Acorn (Quercus acutissima CARR.) against IgE-mediated Allergic and Ovalbumin (OVA)-Induced Asthmatic Responses via Inhibition of Oxidative Stress
Chung, Mi-Ja ; Jo, Hang-Soo ; Choi, Ha-Na ; Cho, Soo-Muk ; Park, Yong-Il ;
Journal of Pharmaceutical Investigation, volume 41, issue 6, 2011, Pages 355~362
DOI : 10.4333/KPS.2011.41.6.355
This work was performed to investigate the protective effect of ethanol extract (AEx) from acorn (Quercus acutissima CARR.) against allergic mediated responses in asthma model cells and mice. The AEx inhibited antigen-stimulated cytokine production such as interleukin (IL)-4, IL-13 and tumor necrosis factor-
) and AEx also inhibited intracellular reactive oxygen species (ROS) generation against IgE-mediated allergic response in rat basophilic leukaemia RBL-2H3 cells. The ovalbumin (OVA)-sensitized mice were orally administered with AEx (100 or 300 mg/kg) and authentic tannic acid (75 mg/kg) every day for 15 days. Increased TNF-
production by OVA-sensitization/challenge was significantly reduced by administration of AEx. The serum triglyceride levels of asthma mice were significantly reduced after feeding for 15 days with tannic acid or AEx. The mice fed with tannic acid or AEx also exhibited a significant reduction in body weights compared to those of asthma control group. The AEx increased the heme oxygenase (HO)-1 mRNA expression in the asthma model mice and showed DPPH radical scavenging activity. These results indicate that AEx protects against IgEmediated allergic and OVA-induced asthmatic responses via direct and indirect antioxidant activities. Reduced triglyceride and body weights may provide additional protective benefits of AEx on allergic asthma.
Effect of Manufacturing Method and Acidifier on the Dissolution Rate of Carvedilol from Solid Dispersion Formulations
Lim, Dong-Kyun ; Bae, Jeong-Woo ; Song, Byung-Joo ; Jo, Han-Su ; Kim, Hyoung-Eun ; Lee, Dong-Won ; Khang, Gil-Son ;
Journal of Pharmaceutical Investigation, volume 41, issue 6, 2011, Pages 363~369
DOI : 10.4333/KPS.2011.41.6.363
In this study, we demonstrated the release behavior of carvedilol with the content of polyvinylpyrrolidone K-30 (PVP K-30) and the effect of citric acid and fumaric acid as acidifiers on the release behavior of drug. In addition, it tries to inquire into the release behavior difference of the carvedilol according to the manufacturing method. The release behavior of the tablets was compared with Dilatrand
in the simulated gastric fluid (pH1.2). Differential scanning calorimeter (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) were characterized for the physicochemical properties of the tablets. In case of mixing the carvedilol and PVP K-30, in case the ratio of the carvedilol and PVP K-30 was 1:5, the release behavior was the highest among. As well as the dissolution rate of tablets manufactured by lyophilization and rotary evaporator was higher than physical mixture. The dissolution rate of containing acidifiers was more improved. But, rather the excessive amount of the acidifier addition reduced the dissolution rate.
Solid State of Tulobuterol : Characterization, Dissolution, Transformation
Do, Eui-Seon ; Sohn, Young-Taek ;
Journal of Pharmaceutical Investigation, volume 41, issue 6, 2011, Pages 371~376
DOI : 10.4333/KPS.2011.41.6.371
The objective of this work was to investigate the existence of new crystal forms of tulobuterol which is used to prevent morning asthma attacks by
agonist and the transformation of crystal forms. Three crystal forms of tulobuterol have been isolated by recrystallization and Form 2 was transformed to Form 4 at 52% RH and 95% RH and these four crystal forms are characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD) and thermogravimetric analysis (TG). The DSC and PXRD patterns of four crystal forms of tulobuterol were different respectively. The dissolution patterns of these three crystal forms of tulobuterol were studied and they showed significant differences in the dissolution rate. After storage of 2 months at 0% RH (silica gel,
), 52% RH (saturated solution of
) and 95% RH (saturated solution of
), Form 1 and Form 3 were not transformed. But Form 2 was transformed to Form 4 at 52% RH and 95% RH.
Discrimination between Artemisia princeps and Artemisia capillaris Based on Near Infrared Spectroscopy Combined Multivariate Analysis
Lee, Dong-Young ; Jeon, Min-Ji ; Suh, Young-Bae ; Kim, Seung-Hyun ; Kim, Young-Choong ; Sung, Sang-Hyun ;
Journal of Pharmaceutical Investigation, volume 41, issue 6, 2011, Pages 377~380
DOI : 10.4333/KPS.2011.41.6.377
The Artemisia princeps (Compositae) has been used in traditional Korean medicine for the treatment of microbial infections and inflammatory diseases. Since A. princeps is generally difficult to be discriminated from A. capillaris, A. caplillaris has been misused in place of A. princeps. To solve this problem, a rapid and nondestructive method for discrimination of A. princeps and A. capillaris samples was developed using near infrared spectroscopy (NIRS) in the present study. A principal component analysis (PCA) and a partial least squares discrimination analysis (PLS-DA) were performed to discriminate two species. As a result, with the use of PLS-DA, A. princeps and A. capillaris were clustered according to their genus. These outcomes indicated that the NIRS could be useful for the discrimination between Artemisia princeps and Artemisia capillaris.
Combination of Curcumin and Paclitaxel-loaded Solid Lipid Nanoparticles to Overcome Multidrug Resistance
Li, Rihua ; Xu, Wenting ; Eun, Jae-Soon ; Lee, Mi-Kyung ;
Journal of Pharmaceutical Investigation, volume 41, issue 6, 2011, Pages 381~386
DOI : 10.4333/KPS.2011.41.6.381
Multi-drug resistance (MDR) has been known as a major hurdle in cancer chemotherapy. One of the most clinically significant causes of MDR was the efflux of anticancer agents mediated by p-glycoprotein (p-gp) over-expressed in MDR cancer cells. To overcome MDR, there have been several strategies such as co-administration with p-gp inhibitors and encapsulation of anticancer drugs into drug delivery systems. In the present study, curcumin was evaluated for its potential as p-gp inhibitor and MDR reversal activity when combined with paclitaxel incorporated into lipid nanoparticles (PTX/LN). Western blot assay showed curcumin did not modulate the level of p-gp expression in MCF-7/ADR which is a MDR variant of human breast cancer cell line, MCF-7, and over-expresses p-gp. However, curcumin inhibited p-gp-mediated efflux of calcein in a dose-dependent manner even though it showed lower activity compared to verapamil, a well-known p-gp inhibitor. Incorporation of paclitaxel into lipid nanoparticles partially recovered the anticancer activity of paclitaxel in MCF-7/ADR. The combined use of curcumin and PTX/LN exhibited further full reversal of MDR, suggesting susceptibility of PTX/LN to the efflux system. In conclusion, combined approach of using p-gp inhibitors and incorporation of the anticancer agents into nano-delivery systems would be an efficient strategy to overcome MDR.