Improved oral bioavailability of capsaicin via liposomal nanoformulation: preparation, in vitro drug release and pharmacokinetics in rats

Yuan Zhu,Miaomiao Wang,Jiajia Zhang,Wei Peng,Caleb Kesse Firempong,Wenwen Deng,Qilong Wang,Shicheng Wang,Feng Shi,Jiangnan Yu,Ximing Xu,Weiming Zhang 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.4

This study innovatively prepared an effectivecapsaicin-loaded liposome, a nanoformulation with fewerirritants, for oral administration. The in vitro and in vivoproperties of the liposomal encapsulation were investigatedand the potential possibility of oral administration evaluated. The liposomal agent composed of phospholipid, cholesterol,sodium cholate and isopropyl myristate was prepared usingfilm-dispersion method. A level A in vitro–in vivo correlation(IVIVC) was established for the first time, which demonstratedan excellent IVIVC of both formulated and freecapsaicin in oral administration. Physicochemical characterizationsincluding mean particle size, zeta (f) potentialand average encapsulation efficiency of capsaicin-loadedliposome were found to be 52.2 ± 1.3 nm, -41.5 ±2.71 mv and 81.9 ± 2.43 %, respectively. In vivo, liposomalencapsulation allowed a 3.34-fold increase in relativebioavailability compared to free capsaicin. The gastricmucosa irritation studies indicated that the liposomal systemwas a safe carrier for oral administration. These resultssupport the fact that capsaicin, an effective drug for thetreatment of neuropathic pain, could be encapsulated inliposome for improved oral bioavailability. The excellentIVIVC of capsaicin-loaded liposome could also be a promisingtool in liposomal formulation development with anadded advantage of reduced animal testing.

Preparation and In Vitro Evaluation of Povidone-Sodium Cholate- Phospholipid Mixed Micelles for the Solubilization of Poorly Soluble Drugs

Yuan Zhu,Shanshan Tong,Li Wang,Min Peng,Xia Cao,Ximing Xu,Jiangnan Yu 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.6

Mixed micelles made of polyvinylpyrrolidone (PVP), sodium cholate, and phospholipids were prepared to improve the solubility of poorly water-soluble drugs. Sylibin, a drug used in treating liver diseases, was incorporated into the mixed micelles. The formulation of sylibin containing PVP-sodium cholate-phospholipid mixed micelles with an optimized composition (PVP/sodium cholate/phospholipid/silybin = 3:3:4:1~2 by weight) was obtained based on the study of pseudoternary phase diagrams. The critical micelle concentration was used to evaluate the micellar stability towards dilution. The results showed that addition of PVP to sodium-cholate-phospholipid mixed micelles increased stability. The solubility of sylibin in PVP-sodium cholate-phospholipid mixed micelles was higher than that in pure water or in sodium cholate-phospholipid mixed micelles. In a stability study, we found that PVP-sodium cholate-phospholipid mixed micelles showed good stability. After 3 months storage at 40oC, just 2.6% sylibin was lost with only minor changes of the particle size when compared to a reference formulation containing sodium cholate and phospholipid mixed micelles. In addition, the developed formulation significantly improved in vitro drug release. The time required to release 50% sylibin (t50%) from sodium cholate and phospholipid mixed micelles was 326 h, while the t50% from PVP-sodium cholate-phospholipid mixed micelles was only 51.1 h. Our results suggest that these mixed micelles might have significant potential application to the biomedical field.

Visualising Corpus-based Discourse Studies from 1995 to 2019 by Using a Bibliometric Analysis

Yuping Fu,Yuanzhu Liang,Zongjie Zhang,Yong-cheol Lee 한국외국어교육학회 2021 Foreign languages education Vol.28 No.2

This study employed a bibliometric method to visualize the evolution of corpus-based discourse studies between 1995 and 2019, with a total of 2,174 English-language documents and their 83,184 references collected from Scopus, the Social Science Citation Index, and the Arts & Humanities Citation Index. Co-citation analysis of the predominant authors, references, and publication sources disclosed that the field has expanded over the past 25 years from primary pattern analysis of descriptive and functional grammar to principal investigations of interdisciplinary issues, some of which are central to pragmatics and sociolinguistics. This shift of research focus is also evidenced by keyword analysis. Scholars have been progressively more fascinated by such social issues as news discourse, business discourse, gender and language, and identity. Some emerging topics like social media, media discourse, legal discourse, and the metadiscourse interpersonal model may represent research hotspots and trends in this area. Bibliometric approaches play an important role in providing hands-on evidence-based comparisons and visualizations of previous research outputs using different time bands.

Time-Varying Amplitude-Frequency Characteristics Analysis of VSC Internal Voltage under Grid Fault

Jingyi Liu,Yuanzhu Chang,Jiabing Hu,Lei Shang 전력전자학회 2019 ICPE(ISPE)논문집 Vol.2019 No.5

As the voltage source converters (VSCs) are widely used as the important interface between the new energy applications and the power systems, the transient characteristics of VSC have great influence on the operation of the modern power systems. In this paper, internal voltage concept is introduced to represent the external characteristics of VSC. The amplitude/frequency characteristics of VSC internal voltage under non-severe grid fault and severe grid fault are analyzed and compared. The results show that under non-severe grid fault, the amplitude/frequency characteristics of VSC internal voltage are periodic time-varying. And the amplitude and frequency are the linear combination of modes of the close-loop system, while in severe grid fault, the characteristics of amplitude and frequency are aperiodic time-varying and are decided by the modes and the nonlinear elements. The results and conclusion are validated in Matlab/Simulink.

AC Network Response Behaviors to Time-Varying Amplitude-Frequency Internal Voltage of Voltage Source Converters

Zhenhai Xie,Yuanzhu Chang,Jiabing Hu 전력전자학회 2019 ICPE(ISPE)논문집 Vol.2019 No.5

During an AC fault, voltage source converter (VSC) has a different excitation-response characteristic compared with the synchronous generator (SG). As a result, for power systems with a high penetration of VSC-based equipment, the network response behaviors are mainly determined by the VSCs’ internal voltage whose amplitude and frequency are time-varying. However, the lumped parameter π-equivalent circuit model is established based on a sine steady-state signal. Thus, in order to analyze the network response behavior, an excitation-response relation model of AC network is proposed. Then, the response behaviors of node-voltage vectors are compared when using two different types line model in electromagnetic transient program (EMTP). Finally, the determinants of network response behaviors are analyzed. The conclusions of this paper indicate that the π-equivalent circuit model is improper and the distributed parameter line model is suggested to simulate the transient behaviors of a power system with high penetration of VSCs.

Fault Current Analysis of Type-3 Wind Turbine Considering Dynamic Influence of Phase Locked Loop

Xiaomeng Yu,Yuanzhu Chang,Jiabing Hu,Lei Shang 전력전자학회 2019 ICPE(ISPE)논문집 Vol.2019 No.5

As Type-3 wind turbine (WT) has already become a vital source in power system, analyzing its fault current is necessary. Although phase-angle jump of stator voltage always occurs during short circuit, it is neglected in existing research and the influence of phase locked loop (PLL) on fault current is still unclear. In this paper, an analytical model of Type-3 WT considering both magnitude drop and phase-angle jump is first developed. Then, the variable-frequency phenomenon of fault current component is discovered by comparing the results of modal analysis and Hilbert-Huang Transformation (HHT). Moreover, the dominant branch causing this phenomenon is extracted so that the whole system can be decomposed into a linear subsystem and a nonlinear subsystem. Based on these subsystems, an analytical expression of fault current is deduced and validated. The conclusion of this paper indicates that the variable-frequency phenomenon may result in protective relays’ maloperation.

Frequencies, Inheritance of Porcine FSH-${\beta}$ Retroposon and its Association with Reproductive Traits

Li, Feng'e,Xiong, Yuanzhu,Deng, Changyan,Jiang, Siwen,Zheng, Rong Asian Australasian Association of Animal Productio 2002 Animal Bioscience Vol.15 No.2

The fragment in intron I of FSH-${\beta}$ gene was amplified by PCR. According to the polymorphism, we analyzed the distribution of FSH-${\beta}$ retroposon in different pig breeds; its inheritance pattern in Large White${\times}$Meishan reference family; and the association of FSH-${\beta}$ retroposon with litter size, female reproductive organs measurement, ultrasonic backfat and other traits. The results showed that almost each Chinese indigenous pig had the retroposon, while foreign pig breeds rarely had; the frequencies of porcine FSH-${\beta}$ retroposon were strongly associated with breeds (p<0.01); the pattern of inheritance was consistent with Mendelian fashion; total number born (TNB) and number born alive (NBA) were increased per FSH-${\beta}$ retroposon (p<0.01) with additive effects of 1.2-1.8 and 1.4-1.8 pigs/litter, respectively; between the FSH-${\beta}$ retroposon carriers and non-carriers, there was an insignificant difference in the measurement of female reproductive organs, body weight at birth, backfat thickness, loin meat height, lean meat percentage, teat number, days to 100 kg, and average daily gain.

Construction of Genetic Microsatellite Maps for Some Chromosomes in Chinese Swine Reference Population

Su, Yuhong,Xiong, Yuanzhu,Zhang, Qin,Liu, Weimin,Jiang, Siwen,Yu, Li,Xia, Xuanyan,Zeng, Rong,Deng, Changyan Asian Australasian Association of Animal Productio 2002 Animal Bioscience Vol.15 No.10

In aiming to identify the genes or genetic regions responsible for quantitative traits, a swine reference population had been constructed using three Large White boars and seven Meishan dams as parents. Five $F_1$ males and 23 $F_1$ females were intercrossed to generate 147 $F_2$ offspring. Thirty-one microsatellite markers covering Sus scrofa chromosomes (SSC) 2, 4, 6 and 7 were genotyped for all members. Construction of genetic microsatellite maps was performed using the CRIMAP software package. The lengths of these chromosomes were longer than MARC maps. They were 158.6cM, 180.3cM, 197.3cM and 171.4cM, respectively. A two modified orders of markers were observed for SSC6 and SSC7. The female map on SSC6 was shorter than male map, and the contrary was on SSC 2, 4 and 7.

FSHR Gene Mutation and Its Effect on Litter Size in Pigs

Zhang, Shujun,Xiong, Yuanzhu,Den, Changyan,Xiao, Senmu,Xu, Jianxiang,Xia, Yu,Liu, Xiaohua,Wang, Chunfang,Sun, Shulin Asian Australasian Association of Animal Productio 2004 Animal Bioscience Vol.17 No.2

The polymorphism of the locus FSHRB in intron6-Exon7 of FSHR gene was investigated by PCR-RFLPs in Erhualian, Large White and Landrace${\times}$Large White; The association of polymorphism and litter size was analyzed by using SAS. The results showed that 1) the polymorphism of the locus FSHRB was significantly associated with litter size; 2) the total born number (TBN) and number born alive (NBA) of the sows with BB genotype were increased (p<0.05) with additive effects of 1.02-1.42 and 1.04-1.27 pigs per litter, respectively; 3) among the sows with genotype AA, AB or BB, there was an insignificant difference in born weight and weaning weight. This gene may be an effective potential tool used in conjunction with traditional selection methods.

Age-dependent Changes of Differential Gene Expression Profile in Backfat Tissue between Hybrids and Parents in Pigs

Ren, ZH.Q.,Xiong, Yuanzhu,Deng, CH.Y.,Zuo, B.,Liu, Y.G.,Lei, M.G. Asian Australasian Association of Animal Productio 2005 Animal Bioscience Vol.18 No.5

Large White, an introduced European pig breed, and Meishan, a Chinese indigenous pig breed, were hybridized directly and reciprocally and a total of 260 pigs, including purebreds, Large White and Meishan, and their hybrids, White${\times}$Meishan (LM) and Meishan${\times}$Large White (ML) pigs, were bred in our laboratory. The mRNA differential display PCR (DD-PCR) was used to detect the age-dependent changes of differential gene expression in backfat tissue between hybrids and parents. Some measures were taken to reduce the false positives in our experiment. Among the total of 2,686 bands obtained, 1,952 bands (about 72.67%) were reproducible and eight patterns (fifteen kinds) of gene expression were observed. The percentage of differentially expressed genes between hybrids and parents is 56.86% at the age of four months and 57.71% at the age of six months. This indicated that the differences of gene expression between hybrids and their parents were very obvious. U-test was used to compare the patterns of gene expression between the age of four and six months, and results showed that bands occurring in only one hybrid and bands displayed in one hybrid and one parent were significantly different at p<0.05, and bands visualized in only two hybrids were significantly different at p<0.01. These indicated that differential gene expression between hybrids and parents changed at different ages.