http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Micro-/nano-sized delivery systems of ginsenosides for improved systemic bioavailability
Kim, Hyeongmin,Lee, Jong Hyuk,Kim, Jee Eun,Kim, Young Su,Ryu, Choong Ho,Lee, Hong Joo,Kim, Hye Min,Jeon, Hyojin,Won, Hyo-Joong,Lee, Ji-Yun,Lee, Jaehwi The Korean Society of Ginseng 2018 Journal of Ginseng Research Vol.42 No.3
Ginsenosides, dammarane-type triterpene saponins obtained from ginseng, have been used as a natural medicine for many years in the Orient due to their various pharmacological activities. However, the therapeutic potential of ginsenosides has been largely limited by the low bioavailability of the natural products caused mainly by low aqueous solubility, poor biomembrane permeability, instability in the gastrointestinal tract, and extensive metabolism in the body. To enhance the bioavailability of ginsenosides, diverse micro-/nano-sized delivery systems such as emulsions, polymeric particles, and vesicular systems have been investigated. The delivery systems improved the bioavailability of ginsenosides by enhancing solubility, permeability, and stability of the natural products. This mini-review aims to provide comprehensive information on the micro-/nano-sized delivery systems for increasing the bioavailability of ginsenosides, which may be helpful for designing better delivery systems to maximize the versatile therapeutic potential of ginsenosides.
Seong Yeon Kim,Yeon Joo Na,Dongju Kim,Yeongseok Kim,Hyeong Min Kim,Sung-Ha Hwang,Jiyeon Kwak,Hyo-Jeong Kuh,Jaehwi Lee 대한생리학회-대한약리학회 2012 The Korean Journal of Physiology & Pharmacology Vol.16 No.3
The objective of the present study was to establish the method of measurement of hydrogen peroxide and to estimate the anti-oxidative effect of genistein in the skin. UVB induced skin oxidation and anti-oxidative effect of genistein formulations were evaluated by determining levels of hydrogen peroxide. The mechanism involved in the determination of hydrogen peroxide is based on a color reaction between ferric ion (Fe<sup>3+</sup>) and xylenol orange, often called FOX assay and subsequent monitoring of absorbance values of the reactant at 540 nm. The reaction was to some extent pH-dependent and detection sensitivity was greatest at pH 1.75. Genistein liposomal gel demonstrated better anti-oxidative effect with regard to lowering hydrogen peroxide levels elevated by UVB irradiation compared to genistein-suspended gel. A linear relationship has been observed between anti-oxidative effect of genistein and drug deposition in the skin tissue. Genistein liposomal gel resulting in the localization of the drug in the deeper skin led to improved anti-oxidative effect compared to genistein gel. The suggested method for evaluation of oxidation of the skin can be used as a tool to screen effective anti-oxidative agents and their delivery systems acting on the skin.
Immunotoxicological Effects of Aripiprazole: In vivo and In vitro Studies
Baek, Kwang-Soo,Ahn, Shinbyoung,Lee, Jaehwi,Kim, Ji Hye,Kim, Han Gyung,Kim, Eunji,Kim, Jun Ho,Sung, Nak Yoon,Yang, Sungjae,Kim, Mi Seon,Hong, Sungyoul,Kim, Jong-Hoon,Cho, Jae Youl The Korean Society of Pharmacology 2015 The Korean Journal of Physiology & Pharmacology Vol.19 No.4
Aripiprazole (ARI) is a commonly prescribed medication used to treat schizophrenia and bipolar disorder. To date, there have been no studies regarding the molecular pathological and immunotoxicological profiling of aripiprazole. Thus, in the present study, we prepared two different formulas of aripiprazole [Free base crystal of aripiprazole (ARPGCB) and cocrystal of aripiprazole (GCB3004)], and explored their effects on the patterns of survival and apoptosis-regulatory proteins under acute toxicity and cytotoxicity test conditions. Furthermore, we also evaluated the modulatory activity of the different formulations on the immunological responses in macrophages primed by various stimulators such as lipopolysaccharide (LPS), pam3CSK, and poly(I:C) via toll-like receptor 4 (TLR4), TLR2, and TLR3 pathways, respectively. In liver, both ARPGCB and GCB3004 produced similar toxicity profiles. In particular, these two formulas exhibited similar phospho-protein profiling of p65/nuclear factor $(NF)-{\kappa}B$, c-Jun/activator protein (AP)-1, ERK, JNK, p38, caspase 3, and bcl-2 in brain. In contrast, the patterns of these phospho-proteins were variable in other tissues. Moreover, these two formulas did not exhibit any cytotoxicity in C6 glioma cells. Finally, the two formulations at available in vivo concentrations did not block nitric oxide (NO) production from activated macrophage-like RAW264.7 cells stimulated with LPS, pam3CSK, or poly(I:C), nor did they alter the morphological changes of the activated macrophages. Taken together, our present work, as a comparative study of two different formulas of aripiprazole, suggests that these two formulas can be used to achieve similar functional activation of brain proteins related to cell survival and apoptosis and immunotoxicological activities of macrophages.
Immunotoxicological Effects of Aripiprazole: <em>In vivo</em> and <em>In vitro</em> Studies
Kwang-Soo Baek,Shinbyoung Ahn,Jaehwi Lee,Ji Hye Kim,Han Gyung Kim,Eunji Kim,Jun Ho Kim,Nak Yoon Sung,Sungjae Yang,Mi Seon Kim,Sungyoul Hong,Jong-Hoon Kim,Jae Youl Cho 대한생리학회-대한약리학회 2015 The Korean Journal of Physiology & Pharmacology Vol.19 No.4
Aripiprazole (ARI) is a commonly prescribed medication used to treat schizophrenia and bipolar disorder. To date, there have been no studies regarding the molecular pathological and immunotoxicological profiling of aripiprazole. Thus, in the present study, we prepared two different formulas of aripiprazole [Free base crystal of aripiprazole (ARPGCB) and cocrystal of aripiprazole (GCB3004)], and explored their effects on the patterns of survival and apoptosis-regulatory proteins under acute toxicity and cytotoxicity test conditions. Furthermore, we also evaluated the modulatory activity of the different formulations on the immunological responses in macrophages primed by various stimulators such as lipopolysaccharide (LPS), pam3CSK, and poly(I:C) via toll-like receptor 4 (TLR4), TLR2, and TLR3 pathways, respectively. In liver, both ARPGCB and GCB3004 produced similar toxicity profiles. In particular, these two formulas exhibited similar phospho-protein profiling of p65/nuclear factor (NF)-κB, c-Jun/activator protein (AP)-1, ERK, JNK, p38, caspase 3, and bcl-2 in brain. In contrast, the patterns of these phospho-proteins were variable in other tissues. Moreover, these two formulas did not exhibit any cytotoxicity in C6 glioma cells. Finally, the two formulations at available <em>in vivo</em> concentrations did not block nitric oxide (NO) production from activated macrophage-like RAW264.7 cells stimulated with LPS, pam3CSK, or poly(I:C), nor did they alter the morphological changes of the activated macrophages. Taken together, our present work, as a comparative study of two different formulas of aripiprazole, suggests that these two formulas can be used to achieve similar functional activation of brain proteins related to cell survival and apoptosis and immunotoxicological activities of macrophages.
Kim Dohyun,Shin Daehyun,Koo Jain,Kim Jungseop,Na Seon Jeong,Bang Joon Seok,Na Dong Hee,Lee Jaehwi 대한화학회 2022 Bulletin of the Korean Chemical Society Vol.43 No.6
This study aimed to investigate the effects of various factors, including contact time, disk shape, and polymer molecular weight, on the in vitro mucoadhesive properties of disks prepared using hydrophilic polymers. Mucoadhesive performance was evaluated by measuring the peak detachment force and work of adhesion values using tensile tests. The mucoadhesive force and work of adhesion values increased with increasing contact time between the polymeric disks and mucin gel layer until 60 s. Increased mucoadhesive performances were typically observed when the disks comprised high-molecular-weight polymers, which indicates the increase in the entanglement. Increasing the thicknesses of the disks allowed the disks to absorb more water and thereby have more flexible polymeric chains, enhancing the mucoadhesive capacity. The proportional increase in the mucoadhesive force and work values were observed with increasing the surface areas of the disks. In conclusion, this study comprehensively demonstrated the effects of various experimental factors on mucoadhesion.
Kim, Jeong Tae,Barua, Sonia,Kim, Hyeongmin,Hong, Seong-Chul,Yoo, Seung-Yup,Jeon, Hyojin,Cho, Yeongjin,Gil, Sangwon,Oh, Kyungsoo,Lee, Jaehwi The Korean Society of Applied Pharmacology 2017 Biomolecules & Therapeutics(구 응용약물학회지) Vol.25 No.4
In this study, the effect of particle size of genistein-loaded solid lipid particulate systems on drug dissolution behavior and oral bioavailability was investigated. Genistein-loaded solid lipid microparticles and nanoparticles were prepared with glyceryl palmitostearate. Except for the particle size, other properties of genistein-loaded solid lipid microparticles and nanoparticles such as particle composition and drug loading efficiency and amount were similarly controlled to mainly evaluate the effect of different particle sizes of the solid lipid particulate systems on drug dissolution behavior and oral bioavailability. The results showed that genistein-loaded solid lipid microparticles and nanoparticles exhibited a considerably increased drug dissolution rate compared to that of genistein bulk powder and suspension. The microparticles gradually released genistein as a function of time while the nanoparticles exhibited a biphasic drug release pattern, showing an initial burst drug release, followed by a sustained release. The oral bioavailability of genistein loaded in solid lipid microparticles and nanoparticles in rats was also significantly enhanced compared to that in bulk powders and the suspension. However, the bioavailability from the microparticles increased more than that from the nanoparticles mainly because the rapid drug dissolution rate and rapid absorption of genistein because of the large surface area of the genistein-solid lipid nanoparticles cleared the drug to a greater extent than the genistein-solid lipid microparticles did. Therefore, the findings of this study suggest that controlling the particle size of solid-lipid particulate systems at a micro-scale would be a promising strategy to increase the oral bioavailability of genistein.
Comparison of time series clustering methods and application to power consumption pattern clustering
Kim, Jaehwi,Kim, Jaehee The Korean Statistical Society 2020 Communications for statistical applications and me Vol.27 No.6
The development of smart grids has enabled the easy collection of a large amount of power data. There are some common patterns that make it useful to cluster power consumption patterns when analyzing s power big data. In this paper, clustering analysis is based on distance functions for time series and clustering algorithms to discover patterns for power consumption data. In clustering, we use 10 distance measures to find the clusters that consider the characteristics of time series data. A simulation study is done to compare the distance measures for clustering. Cluster validity measures are also calculated and compared such as error rate, similarity index, Dunn index and silhouette values. Real power consumption data are used for clustering, with five distance measures whose performances are better than others in the simulation.