Article(id=1322631198623515024, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1322631195876242221, articleNumber=null, orderNo=null, doi=10.7501/j.issn.0253-2670.2026.17.007, pmid=null, cstr=null, oa=null, hot=0, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=1771603200000, receivedDateStr=2026-02-21, revisedDate=null, revisedDateStr=null, acceptedDate=null, acceptedDateStr=null, onlineDate=1793269451051, onlineDateStr=2026-10-29, pubDate=null, pubDateStr=null, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1793269451051, onlineIssueDateStr=2026-10-29, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1793269451051, creator=13701087609, updateTime=1793269451051, updator=13701087609, issue=Issue{id=1322631195876242221, tenantId=1146029695717560320, journalId=1302319053441957962, year='2026', volume='57', issue='17', pageStart='6661', pageEnd='7072', issueExtLink='null', onlineDate='null', pubDate='1789142400000', pubDateStr='2026-09-12', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1793269450396, creator='13701087609', updateTime=1793269538381, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1322631565008556693, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1322631195876242221, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1322631565008556694, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1322631195876242221, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=6730, endPage=6742, ext={EN=ArticleExt(id=1322631200544506258, articleId=1322631198623515024, tenantId=1146029695717560320, journalId=1302319053441957962, language=EN, title=Trifolin-phospholipids complex/chitosan nanoparticles: Preparation, oral pharmacokinetics in vivo and evaluation of protective effect on acute liver injury, columnId=null, journalTitle=Chinese Traditional and Herbal Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=Objective To prepare trifolin-phospholipids complex/chitosan nanoparticles (Tri-PC/CS-NPs), and investigate its in vivo pharmacokinetic behavior and protective effect on acute liver injury. Methods Trifolin-phospholipids complex (Tri-PC) was prepared by solvent evaporation method. Single factor experiments combined Box-Behnken design-response surface methodology (BBD-RSM) were used to optimize the prescriptions of Tri-PC/CS-NPs. Transmission electron microscope (TEM) was employed to observe microscopic appearance of Tri-PC/CS-NPs, X-ray powder diffraction (XRPD) was used to analyze crystal form of Tri-PC/CS-NPs. Saturated solubility, oil/water partition coefficient and drug release behavior in simulated gastrointestinal fluids of trifolin, Tri-PC and Tri-PC/CS-NPs were compared. SD rats were administered intragastrically with trifolin, Tri-PC and Tri-PC/CS-NPs, respectively. Blood drug concentration was determined, and the main pharmacokinetic parameters were calculated. The model of acute liver injury was established, and the protective effect of trifolin, Tri-PC, Tri-PC/CS-NPs on acute liver injury were compared. Results Optimal formulations of Tri-PC/CS-NPs: the volume of water phase was 20.50 mL, the mass ratio of Tri-PC to chitosan was 4.15:1, and the mass fraction of Poloxamer 188 was 0.10%. Envelopment efficiency, drug loading, particle size and ζ potential were (84.80 ± 1.21)%, (15.56 ± 0.10)%, (197.74 ± 5.58) nm and (32.69 ± 1.14) mV, respectively. The appearance of Tri-PC/CS-NPs were spherical. The state of trifolin changed into amorphous form in Tri-PC and Tri-PC/CS-NPs. Tri-PC and Tri-PC/CS-NPs significantly enhanced the saturated solubility and oil/water partition coefficient of trifolin (P < 0.01). Cumulative release rate of Tri-PC and Tri-PC/CS-NPs were 56.68% and 88.45% in 18 h, respectively. The drug release process of Tri-PC/CS-NPs conformed to the Weibull model. Compared with trifolin, the relative bioavailability of Tri-PC and Tri-PC/CS-NPs was enhanced to 2.41-fold and 5.36-fold, respectively. Tri-PC and Tri-PC/CS-NPs effectively enhanced the protective effect of trifolin against acute liver injury, and the protective effect of Tri-PC/CS-NPs was superior to that of Tri-PC. Conclusion Tri-PC/CS-NPs changed the pharmacokinetic behavior of trifolin in vivo , effectively promoted the absorption of trifolin, and enhanced the protective effect of trifolin on acute liver injury., authors=YAO Jie1 , JI Xinying1 , WANG Yunhua1 , ZHANG Tipeng1 , SHI Yanhua1 , DU Juan1 , SHANG Huijie1 , ZHANG Fuli1,2 , authorsList=YAO Jie, JI Xinying, WANG Yunhua, ZHANG Tipeng, SHI Yanhua, DU Juan, SHANG Huijie, ZHANG Fuli, authorCompany=1 Zhengzhou Health College, Zhengzhou 450064, China; 目的 制备三叶苷-磷脂复合物/壳聚糖纳米粒（trifolin-phospholipids complex/chitosan nanoparticles，Tri-PC/CS-NPs），考察Tri-PC/CS-NPs体内药动学行为及对急性肝损伤的保护作用。方法 采用溶剂挥发法制备三叶苷-磷脂复合物（trifolin-phospholipids complex，Tri-PC）。采用单因素实验结合Box-Behnken设计-效应面法（Box-Behnken design-response surface methodology，BBD-RSM）优化Tri-PC/CS-NPs处方工艺。采用透射电子显微镜（transmission electron microscope，TEM）观察Tri-PC/CS-NPs形貌，X射线粉末衍射法（X-ray powder diffraction，XRPD）分析Tri-PC/CS-NPs晶型。比较三叶苷、Tri-PC、Tri-PC/CS-NPs的饱和溶解度、油水分配系数及其在模拟胃肠液中的释药行为。SD大鼠分别ig给予三叶苷、Tri-PC、Tri-PC/CS-NPs，测定血药浓度，计算主要药动学参数。建立急性肝损伤大鼠模型，比较三叶苷、Tri-PC、Tri-PC/CS-NPs对急性肝损伤大鼠的保护作用。结果 Tri-PC/CS-NPs最佳处方：水相体积为20.50 mL，Tri-PC与壳聚糖质量比为4.15∶1，泊洛沙姆188质量分数为0.10%。Tri-PC/CS-NPs的包封率、载药量、粒径及ζ电位分别为（84.80±1.21）%、（15.56±0.10）%、（197.74±5.58）nm和（32.69±1.14）mV。Tri-PC/CS-NPs外貌为类球形。三叶苷在Tri-PC和Tri-PC/CS-NPs中均以无定形形态存在。Tri-PC和Tri-PC/CS-NPs极显著性提高了三叶苷的饱和溶解度及油水分配系数（P ＜0.01）。Tri-PC和Tri-PC/CS-NPs在18 h内累积释放率分别为56.68%和88.45%。Tri-PC/CS-NPs的释药行为符合Weibull模型。以三叶苷为参考，Tri-PC和Tri-PC/CS-NPs相对生物利用度分别增加至2.41倍和5.36倍。Tri-PC和Tri-PC/CS-NPs有效增强了三叶苷对急性肝损伤大鼠的保护作用，且Tri-PC/CS-NPs效果优于Tri-PC。结论 Tri-PC/CS-NPs改变了三叶苷的体内药动学行为，有效促进了三叶苷的体内吸收，并增强了三叶苷对急性肝损伤的保护作用。, authors=姚杰1 , 姬新颖1 , 王赟华1 , 张体鹏1 , 时艳华1 , 杜娟1 , 尚慧杰1 , 张付利1,2 , authorsList=姚杰, 姬新颖, 王赟华, 张体鹏, 时艳华, 杜娟, 尚慧杰, 张付利, authorCompany=1 郑州健康学院, 河南 郑州 450064;
中草药
|药剂与工艺
2026
, 57
(17) :
6730
-6742
三叶苷-磷脂复合物/壳聚糖纳米粒的制备、口服药动学及对急性肝损伤保护作用评价
全屏
姚杰1 , 姬新颖1 , 王赟华1 , 张体鹏1 , 时艳华1 , 杜娟1 , 尚慧杰1 , 张付利1,2
作者信息
1 郑州健康学院, 河南 郑州 450064;
通讯作者:
张付利
作者简介:
姚杰: 姚杰（1982—），女，硕士，讲师，研究方向为临床药学及中医学。Tel:(0371)86176371 E-mail:haihai2008001@126.com
Trifolin-phospholipids complex/chitosan nanoparticles: Preparation, oral pharmacokinetics in vivo and evaluation of protective effect on acute liver injury
YAO Jie1 , JI Xinying1 , WANG Yunhua1 , ZHANG Tipeng1 , SHI Yanhua1 , DU Juan1 , SHANG Huijie1 , ZHANG Fuli1,2
Affiliations
1 Zhengzhou Health College, Zhengzhou 450064, China;
doi: 10.7501/j.issn.0253-2670.2026.17.007
文章导航
目的 制备三叶苷-磷脂复合物/壳聚糖纳米粒（trifolin-phospholipids complex/chitosan nanoparticles，Tri-PC/CS-NPs），考察Tri-PC/CS-NPs体内药动学行为及对急性肝损伤的保护作用。方法 采用溶剂挥发法制备三叶苷-磷脂复合物（trifolin-phospholipids complex，Tri-PC）。采用单因素实验结合Box-Behnken设计-效应面法（Box-Behnken design-response surface methodology，BBD-RSM）优化Tri-PC/CS-NPs处方工艺。采用透射电子显微镜（transmission electron microscope，TEM）观察Tri-PC/CS-NPs形貌，X射线粉末衍射法（X-ray powder diffraction，XRPD）分析Tri-PC/CS-NPs晶型。比较三叶苷、Tri-PC、Tri-PC/CS-NPs的饱和溶解度、油水分配系数及其在模拟胃肠液中的释药行为。SD大鼠分别ig给予三叶苷、Tri-PC、Tri-PC/CS-NPs，测定血药浓度，计算主要药动学参数。建立急性肝损伤大鼠模型，比较三叶苷、Tri-PC、Tri-PC/CS-NPs对急性肝损伤大鼠的保护作用。结果 Tri-PC/CS-NPs最佳处方：水相体积为20.50 mL，Tri-PC与壳聚糖质量比为4.15∶1，泊洛沙姆188质量分数为0.10%。Tri-PC/CS-NPs的包封率、载药量、粒径及ζ电位分别为（84.80±1.21）%、（15.56±0.10）%、（197.74±5.58）nm和（32.69±1.14）mV。Tri-PC/CS-NPs外貌为类球形。三叶苷在Tri-PC和Tri-PC/CS-NPs中均以无定形形态存在。Tri-PC和Tri-PC/CS-NPs极显著性提高了三叶苷的饱和溶解度及油水分配系数（P ＜0.01）。Tri-PC和Tri-PC/CS-NPs在18 h内累积释放率分别为56.68%和88.45%。Tri-PC/CS-NPs的释药行为符合Weibull模型。以三叶苷为参考，Tri-PC和Tri-PC/CS-NPs相对生物利用度分别增加至2.41倍和5.36倍。Tri-PC和Tri-PC/CS-NPs有效增强了三叶苷对急性肝损伤大鼠的保护作用，且Tri-PC/CS-NPs效果优于Tri-PC。结论 Tri-PC/CS-NPs改变了三叶苷的体内药动学行为，有效促进了三叶苷的体内吸收，并增强了三叶苷对急性肝损伤的保护作用。
三叶苷
/
磷脂复合物
/
壳聚糖
/
纳米粒
/
Box-Behnken设计-效应面法
/
溶解度
/
油水分配系数
/
生物利用度
/
急性肝损伤
Objective To prepare trifolin-phospholipids complex/chitosan nanoparticles (Tri-PC/CS-NPs), and investigate its in vivo pharmacokinetic behavior and protective effect on acute liver injury. Methods Trifolin-phospholipids complex (Tri-PC) was prepared by solvent evaporation method. Single factor experiments combined Box-Behnken design-response surface methodology (BBD-RSM) were used to optimize the prescriptions of Tri-PC/CS-NPs. Transmission electron microscope (TEM) was employed to observe microscopic appearance of Tri-PC/CS-NPs, X-ray powder diffraction (XRPD) was used to analyze crystal form of Tri-PC/CS-NPs. Saturated solubility, oil/water partition coefficient and drug release behavior in simulated gastrointestinal fluids of trifolin, Tri-PC and Tri-PC/CS-NPs were compared. SD rats were administered intragastrically with trifolin, Tri-PC and Tri-PC/CS-NPs, respectively. Blood drug concentration was determined, and the main pharmacokinetic parameters were calculated. The model of acute liver injury was established, and the protective effect of trifolin, Tri-PC, Tri-PC/CS-NPs on acute liver injury were compared. Results Optimal formulations of Tri-PC/CS-NPs: the volume of water phase was 20.50 mL, the mass ratio of Tri-PC to chitosan was 4.15:1, and the mass fraction of Poloxamer 188 was 0.10%. Envelopment efficiency, drug loading, particle size and ζ potential were (84.80 ± 1.21)%, (15.56 ± 0.10)%, (197.74 ± 5.58) nm and (32.69 ± 1.14) mV, respectively. The appearance of Tri-PC/CS-NPs were spherical. The state of trifolin changed into amorphous form in Tri-PC and Tri-PC/CS-NPs. Tri-PC and Tri-PC/CS-NPs significantly enhanced the saturated solubility and oil/water partition coefficient of trifolin (P < 0.01). Cumulative release rate of Tri-PC and Tri-PC/CS-NPs were 56.68% and 88.45% in 18 h, respectively. The drug release process of Tri-PC/CS-NPs conformed to the Weibull model. Compared with trifolin, the relative bioavailability of Tri-PC and Tri-PC/CS-NPs was enhanced to 2.41-fold and 5.36-fold, respectively. Tri-PC and Tri-PC/CS-NPs effectively enhanced the protective effect of trifolin against acute liver injury, and the protective effect of Tri-PC/CS-NPs was superior to that of Tri-PC. Conclusion Tri-PC/CS-NPs changed the pharmacokinetic behavior of trifolin in vivo , effectively promoted the absorption of trifolin, and enhanced the protective effect of trifolin on acute liver injury.
trifolin
/
phospholipids complex
/
chitosan
/
nanoparticles
/
Box-Behnken design-response surface methodology
/
solubility
/
oil/water partition coefficient
/
bioavailability
/
acute liver injury
姚杰, 姬新颖, 王赟华, 张体鹏, 时艳华, 杜娟, 尚慧杰, 张付利.
三叶苷-磷脂复合物/壳聚糖纳米粒的制备、口服药动学及对急性肝损伤保护作用评价.
中草药,
2026
, 57
(17)
: 6730
-6742
.
DOI: 10.7501/j.issn.0253-2670.2026.17.007
YAO Jie, JI Xinying, WANG Yunhua, ZHANG Tipeng, SHI Yanhua, DU Juan, SHANG Huijie, ZHANG Fuli.
Trifolin-phospholipids complex/chitosan nanoparticles: Preparation, oral pharmacokinetics in vivo and evaluation of protective effect on acute liver injury[J].
Chinese Traditional and Herbal Drugs ,
2026
, 57
(17)
: 6730
-6742
.
DOI: 10.7501/j.issn.0253-2670.2026.17.007
参考文献
引证文献
刘鸿基, 曾琛悦, 曾霞, 等. 甜茶木姜叶柯及其主要活性成分三叶苷药理作用研究进展[J]. 广东药科大学学报, 2024, 40(3): 129-135.
2026年第57卷第17期
PDF下载
25
4
引用本文
BibTeX
文章信息
doi: 10.7501/j.issn.0253-2670.2026.17.007
接收时间：2026-02-21
首发时间：2026-10-29
https://castjournals.cast.org.cn/joweb/zcy/CN/10.7501/j.issn.0253-2670.2026.17.007
引用本文
BibTeX
2种不同金属材料的力学参数
科 属数 种数 占总种数比例 属 种数 占总种数比例 鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78 小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39 多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39 红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87 小菇属 Mycena 11 5.26 光柄菇属 Pluteus 5 2.39 红菇属 Russula 17 8.13 栓菌属 Trametes 5 2.39
关闭全屏
BibTeX
EndNote
RefWorks
TxT
PDF下载
全屏
25
4
关闭全屏
北京市海淀区学院南路86号
010-62662699（运营及技术支持）
qkjq@cast.org.cn
