Article(id=1304388145202618677, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304388108988997783, articleNumber=null, orderNo=null, doi=10.7501/j.issn.0253-2670.2026.12.008, pmid=null, cstr=null, oa=null, hot=0, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=1767283200000, receivedDateStr=2026-01-02, revisedDate=null, revisedDateStr=null, acceptedDate=null, acceptedDateStr=null, onlineDate=1788919968175, onlineDateStr=2026-09-09, pubDate=null, pubDateStr=null, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1788919968175, onlineIssueDateStr=2026-09-09, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1788919968175, creator=13701087609, updateTime=1788919968175, updator=13701087609, issue=Issue{id=1304388108988997783, tenantId=1146029695717560320, journalId=1302319053441957962, year='2026', volume='57', issue='12', pageStart='4509', pageEnd='4948', issueExtLink='null', onlineDate='null', pubDate='1782576000000', pubDateStr='2026-06-28', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1788919959542, creator='13701087609', updateTime=1788923461082, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1304402795579330582, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304388108988997783, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1304402795579330583, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304388108988997783, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=4594, endPage=4608, ext={EN=ArticleExt(id=1304388147031335224, articleId=1304388145202618677, tenantId=1146029695717560320, journalId=1302319053441957962, language=EN, title=Preparation and oral pharmacokinetics study of vitexin liposomes co-modified with deoxycholic acid and chitosan, columnId=null, journalTitle=Chinese Traditional and Herbal Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=Objective Vitexin liposomes (Vit-Lips), chitosan modified Vit-Lips (CS-Vit-Lips) and deoxycholic acid and chitosan co-modified Vit-Lips (DA/CS-Vit-Lips) were prepared, and their oral pharmacokinetic behavior were compared. Methods Deoxycholic acid-chitosan complex (DA/CS) was synthesized. Film-ultrasonic method was used to prepare Vit-Lips. Encapsulation rate, drug loading and particle size were used as evaluation indexes, single factor investigation combined with Box-Behnken design-response surface methodology (BBD-RSM) were used to investigate the optimal prescriptions of Vit-Lips. CS-Vit-Lips and DA/CS-Vit-Lips were prepared by introducing chitosan and DA/CS, respectively. Transmission electron microscopy (TEM) was used to observe the microstructure of the three kinds of liposomes, and their particle stability in gastrointestinal fluids were compared. Using vitexin as reference, the drug release of Vit-Lips, CS-Vit-Lips and DA/CS-Vit-Lips in simulate gastrointestinal fluid were compared, and their drug release mechanism were also studied. The absorption of the vitexin and its three kinds of liposomes in different intestinal segments was investigated, and the intestinal absorption parameters were calculated. Blood samples were collected after gastric administration of vitexin and its three kinds of liposomes at a dose of 20 mg/kg (vitexin), respectively. Main pharmacokinetic parameters and relative oral bioavailability were also calculated. Results The optimal formulation of Vit-Lips: phospholipids to cholesterol dose ratio was 7.95:1, lipids to drug dose ratio was 9.63:1 and hydration time was 30.00 min. CS-Vit-Lips and DA/CS-Vit-Lips were prepared using chitosan and DA/CS solution with mass fraction of 0.8%, respectively. Entrapment efficiency of Vit-Lips, CS-Vit-Lips and DA/CS-Vit-Lips were (82.31 ± 0.96)%, (84.93 ± 1.17)%, (85.15 ± 1.38)%, drug loading were (7.33 ± 0.09)%, (6.24 ± 0.08)%, (6.30 ± 0.11)%, particles size were (197.70 ± 5.07), (233.06 ± 7.19), (237.93±6.96) nm, and ζ potential were (−28.81 ± 0.86), (27.75 ± 1.10), (26.14 ± 1.13) mV, respectively. The appearance of three kinds of liposomes was spherical vesicular, particle stability of CS-Vit-Lips and DA/CS-Vit-Lips was higher than that of Vit-Lips in simulated gastrointestinal fluid. Vit-Lips, CS-Vit-Lips and DA/CS-Vit-Lips enhanced cumulative release rate to 91.02%, 86.74% and 83.15%, respectively. The drug release process of the three kinds of liposomes conformed to Weibull model. The three kinds of liposomes effectively improved the absorption rate constant (Ka) and apparent absorption coefficient (Papp) of vitexin. Compared to vitexin, Vit-Lips, CS-Vit-Lips and DA/CS-Vit-Lips increased relative oral bioavailability to 1.10-fold, 3.08-fold and 4.70-fold, respectively. The half-life time (t1/2) of CS-Vit-Lips and DA/CS-Vit-Lips had significantly prolonged (P < 0.01) and the peak concentration (Cmax) was significantly increased (P < 0.01). Conclusion CS-Vit-Lips and DA/CS-Vit-Lips effectively promoted the oral absorption of vitexin, and the advantage of DA/CS-Vit-Lips were more obvious, laying an experimental foundation for further research., authors=SONG Yaqiong, LI Xiao, MU Weiwei, JI Shaoping, authorsList=SONG Yaqiong, LI Xiao, MU Weiwei, JI Shaoping, authorCompany=null, correspAuthors=null, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1304388145429111095, articleId=1304388145202618677, tenantId=1146029695717560320, journalId=1302319053441957962, language=CN, title=脱氧胆酸和壳聚糖双修饰的牡荆素脂质体制备及口服动力学研究, columnId=1304140189132149234, journalTitle=中草药, columnName=药剂与工艺, runingTitle=null, highlight=null, articleAbstract=目的 制备牡荆素脂质体(vitexin liposomes,Vit-Lips)、壳聚糖修饰的Vit-Lips(chitosan modified Vit-Lips,CS-Vit-Lips)及脱氧胆酸和壳聚糖双修饰的Vit-Lips(deoxycholic acid and chitosan co-modified Vit-Lips,DA/CS-Vit-Lips),比较3种脂质体口服药动学行为。方法 合成脱氧胆酸-壳聚糖结合物(deoxycholic acid-chitosan complex,DA/CS)。薄膜超声法制备Vit-Lips,采用包封率、载药量和粒径为考察指标,单因素实验结合Box-Behnken设计-响应面法(Box-Behnken design-response surface methodology,BBD-RSM)优化Vit-Lips处方,引入壳聚糖和DA/CS分别制备CS-Vit-Lips和DA/CS-Vit-Lips。透射电子显微镜(transmission electron microscopy,TEM)观察3种脂质体的微观结构,比较其在模拟胃肠液中的粒径稳定性。考察牡荆素原料药及其3种脂质体在模拟胃肠液中释药情况,研究释药机制。考察不同肠段对牡荆素及其3种脂质体的吸收情况,计算肠吸收参数。按照20 mg/kg剂量(以牡荆素计)分别ig牡荆素原料药及其3种脂质体,采集血样,计算主要药动学参数及相对生物利用度。结果 Vit-Lips最佳处方工艺:磷脂与胆固醇用量比为7.95∶1,脂药用量比为9.63∶1,水化时间为30.00 min。采用0.8%的壳聚糖溶液和DA/CS溶液分别制备CS-Vit-Lips和DA/CS-Vit-Lips。Vit-Lips、CS-Vit-Lips、DA/CS-Vit-Lips的包封率分别为(82.31±0.96)%、(84.93±1.17)%、(85.15±1.38)%,载药量分别为(7.33±0.09)%、(6.24±0.08)%、(6.30±0.11)%,平均粒径分别为(197.70±5.07)、(233.06±7.19)、(237.93±6.96)nm,ζ电位分别为(−28.81±0.86)、(27.75±1.10)、(26.14±1.13)mV。3种脂质体外观为类圆形的囊泡状。CS-Vit-Lips和DA/CS-Vit-Lips在模拟胃肠液中粒径稳定性高于Vit-Lips。Vit-Lips、CS-Vit-Lips和DA/CS-Vit-Lips分别将牡荆素的累积释放率提高至91.02%、86.74%和83.15%,3者的释药过程均符合Weibull模型。3种脂质体有效改善了牡荆素吸收速率常数(Ka)和表观吸收系数(Papp)。以牡荆素原料药为参考,Vit-Lips、CS-Vit-Lips和DA/CS-Vit-Lips相对口服吸收生物利用度分别增加至1.10倍、3.08倍和4.70倍,其中,CS-Vit-Lips和DA/CS-Vit-Lips的半衰期(t₁/₂)极显著性延长(P<0.01),达峰浓度(Cmax)极显著性提高(P<0.01)。结论 CS-Vit-Lips和DA/CS-Vit-Lips有效促进了牡荆素口服吸收,DA/CS-Vit-Lips优势更明显,为进一步研究奠定实验基础。, authors=宋亚琼1,2, 李晓1,2, 穆卫卫1,2, 季少平1,2,3, authorsList=宋亚琼, 李晓, 穆卫卫, 季少平, authorCompany=1 郑州健康学院,河南 郑州 450064;
2 河南省核蛋白医学检测工程技术研究中心,河南 郑州 450064;
3 河南大学,河南 开封 475001, correspAuthors=季少平, authorNote=宋亚琼: 宋亚琼(1989—),女,汉族,硕士,讲师,研究方向为临床药学及心脑血管疾病治疗。E-mail:yagiongsong@zzsqmc.edu.cn, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=mq7uPwtyz3bmSIRd9PJKKg==, pdfFileSize=2152991, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=国家自然科学基金项目 (31371386); 国家自然科学基金项目 (30871239))}, authors=null, keywords=[Keyword(id=1304401911768179085, tenantId=1146029695717560320, journalId=1302319053441957962, articleId=1304388145202618677, language=CN, orderNo=1, keyword=牡荆素), Keyword(id=1304401911856259470, tenantId=1146029695717560320, journalId=1302319053441957962, articleId=1304388145202618677, language=CN, orderNo=2, keyword=脂质体), Keyword(id=1304401911923368335, 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中草药 |药剂与工艺 2026 , 57 (12) : 4594 -4608
脱氧胆酸和壳聚糖双修饰的牡荆素脂质体制备及口服动力学研究
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宋亚琼1,2, 李晓1,2, 穆卫卫1,2, 季少平1,2,3
作者信息
    1 郑州健康学院,河南 郑州 450064;
    2 河南省核蛋白医学检测工程技术研究中心,河南 郑州 450064;
    3 河南大学,河南 开封 475001
通讯作者:
季少平
作者简介:
宋亚琼: 宋亚琼(1989—),女,汉族,硕士,讲师,研究方向为临床药学及心脑血管疾病治疗。E-mail:yagiongsong@zzsqmc.edu.cn
Preparation and oral pharmacokinetics study of vitexin liposomes co-modified with deoxycholic acid and chitosan
  • SONG Yaqiong, LI Xiao, MU Weiwei, JI Shaoping
  • Affiliations
    doi: 10.7501/j.issn.0253-2670.2026.12.008
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    目的 制备牡荆素脂质体(vitexin liposomes,Vit-Lips)、壳聚糖修饰的Vit-Lips(chitosan modified Vit-Lips,CS-Vit-Lips)及脱氧胆酸和壳聚糖双修饰的Vit-Lips(deoxycholic acid and chitosan co-modified Vit-Lips,DA/CS-Vit-Lips),比较3种脂质体口服药动学行为。方法 合成脱氧胆酸-壳聚糖结合物(deoxycholic acid-chitosan complex,DA/CS)。薄膜超声法制备Vit-Lips,采用包封率、载药量和粒径为考察指标,单因素实验结合Box-Behnken设计-响应面法(Box-Behnken design-response surface methodology,BBD-RSM)优化Vit-Lips处方,引入壳聚糖和DA/CS分别制备CS-Vit-Lips和DA/CS-Vit-Lips。透射电子显微镜(transmission electron microscopy,TEM)观察3种脂质体的微观结构,比较其在模拟胃肠液中的粒径稳定性。考察牡荆素原料药及其3种脂质体在模拟胃肠液中释药情况,研究释药机制。考察不同肠段对牡荆素及其3种脂质体的吸收情况,计算肠吸收参数。按照20 mg/kg剂量(以牡荆素计)分别ig牡荆素原料药及其3种脂质体,采集血样,计算主要药动学参数及相对生物利用度。结果 Vit-Lips最佳处方工艺:磷脂与胆固醇用量比为7.95∶1,脂药用量比为9.63∶1,水化时间为30.00 min。采用0.8%的壳聚糖溶液和DA/CS溶液分别制备CS-Vit-Lips和DA/CS-Vit-Lips。Vit-Lips、CS-Vit-Lips、DA/CS-Vit-Lips的包封率分别为(82.31±0.96)%、(84.93±1.17)%、(85.15±1.38)%,载药量分别为(7.33±0.09)%、(6.24±0.08)%、(6.30±0.11)%,平均粒径分别为(197.70±5.07)、(233.06±7.19)、(237.93±6.96)nm,ζ电位分别为(−28.81±0.86)、(27.75±1.10)、(26.14±1.13)mV。3种脂质体外观为类圆形的囊泡状。CS-Vit-Lips和DA/CS-Vit-Lips在模拟胃肠液中粒径稳定性高于Vit-Lips。Vit-Lips、CS-Vit-Lips和DA/CS-Vit-Lips分别将牡荆素的累积释放率提高至91.02%、86.74%和83.15%,3者的释药过程均符合Weibull模型。3种脂质体有效改善了牡荆素吸收速率常数(Ka)和表观吸收系数(Papp)。以牡荆素原料药为参考,Vit-Lips、CS-Vit-Lips和DA/CS-Vit-Lips相对口服吸收生物利用度分别增加至1.10倍、3.08倍和4.70倍,其中,CS-Vit-Lips和DA/CS-Vit-Lips的半衰期(t₁/₂)极显著性延长(P<0.01),达峰浓度(Cmax)极显著性提高(P<0.01)。结论 CS-Vit-Lips和DA/CS-Vit-Lips有效促进了牡荆素口服吸收,DA/CS-Vit-Lips优势更明显,为进一步研究奠定实验基础。
    牡荆素  /  脂质体  /  薄膜超声法  /  Box-Behnken设计-响应面法  /  壳聚糖  /  脱氧胆酸  /  修饰  /  在体单向肠灌流  /  药动学行为
    Objective Vitexin liposomes (Vit-Lips), chitosan modified Vit-Lips (CS-Vit-Lips) and deoxycholic acid and chitosan co-modified Vit-Lips (DA/CS-Vit-Lips) were prepared, and their oral pharmacokinetic behavior were compared. Methods Deoxycholic acid-chitosan complex (DA/CS) was synthesized. Film-ultrasonic method was used to prepare Vit-Lips. Encapsulation rate, drug loading and particle size were used as evaluation indexes, single factor investigation combined with Box-Behnken design-response surface methodology (BBD-RSM) were used to investigate the optimal prescriptions of Vit-Lips. CS-Vit-Lips and DA/CS-Vit-Lips were prepared by introducing chitosan and DA/CS, respectively. Transmission electron microscopy (TEM) was used to observe the microstructure of the three kinds of liposomes, and their particle stability in gastrointestinal fluids were compared. Using vitexin as reference, the drug release of Vit-Lips, CS-Vit-Lips and DA/CS-Vit-Lips in simulate gastrointestinal fluid were compared, and their drug release mechanism were also studied. The absorption of the vitexin and its three kinds of liposomes in different intestinal segments was investigated, and the intestinal absorption parameters were calculated. Blood samples were collected after gastric administration of vitexin and its three kinds of liposomes at a dose of 20 mg/kg (vitexin), respectively. Main pharmacokinetic parameters and relative oral bioavailability were also calculated. Results The optimal formulation of Vit-Lips: phospholipids to cholesterol dose ratio was 7.95:1, lipids to drug dose ratio was 9.63:1 and hydration time was 30.00 min. CS-Vit-Lips and DA/CS-Vit-Lips were prepared using chitosan and DA/CS solution with mass fraction of 0.8%, respectively. Entrapment efficiency of Vit-Lips, CS-Vit-Lips and DA/CS-Vit-Lips were (82.31 ± 0.96)%, (84.93 ± 1.17)%, (85.15 ± 1.38)%, drug loading were (7.33 ± 0.09)%, (6.24 ± 0.08)%, (6.30 ± 0.11)%, particles size were (197.70 ± 5.07), (233.06 ± 7.19), (237.93±6.96) nm, and ζ potential were (−28.81 ± 0.86), (27.75 ± 1.10), (26.14 ± 1.13) mV, respectively. The appearance of three kinds of liposomes was spherical vesicular, particle stability of CS-Vit-Lips and DA/CS-Vit-Lips was higher than that of Vit-Lips in simulated gastrointestinal fluid. Vit-Lips, CS-Vit-Lips and DA/CS-Vit-Lips enhanced cumulative release rate to 91.02%, 86.74% and 83.15%, respectively. The drug release process of the three kinds of liposomes conformed to Weibull model. The three kinds of liposomes effectively improved the absorption rate constant (Ka) and apparent absorption coefficient (Papp) of vitexin. Compared to vitexin, Vit-Lips, CS-Vit-Lips and DA/CS-Vit-Lips increased relative oral bioavailability to 1.10-fold, 3.08-fold and 4.70-fold, respectively. The half-life time (t1/2) of CS-Vit-Lips and DA/CS-Vit-Lips had significantly prolonged (P < 0.01) and the peak concentration (Cmax) was significantly increased (P < 0.01). Conclusion CS-Vit-Lips and DA/CS-Vit-Lips effectively promoted the oral absorption of vitexin, and the advantage of DA/CS-Vit-Lips were more obvious, laying an experimental foundation for further research.
    vitexin  /  liposomes  /  film-ultrasonic method  /  Box-Behnken design-response surface methodology  /  chitosan  /  deoxycholic acid  /  modify  /  in situ single-pass intestinal perfusion  /  pharmacokinetic behavior
    宋亚琼, 李晓, 穆卫卫, 季少平. 脱氧胆酸和壳聚糖双修饰的牡荆素脂质体制备及口服动力学研究. 中草药, 2026 , 57 (12) : 4594 -4608 . DOI: 10.7501/j.issn.0253-2670.2026.12.008
    SONG Yaqiong, LI Xiao, MU Weiwei, JI Shaoping. Preparation and oral pharmacokinetics study of vitexin liposomes co-modified with deoxycholic acid and chitosan[J]. Chinese Traditional and Herbal Drugs, 2026 , 57 (12) : 4594 -4608 . DOI: 10.7501/j.issn.0253-2670.2026.12.008

      国家自然科学基金项目 (31371386); 国家自然科学基金项目 (30871239)

    参考文献 引证文献
    排序方式:
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    王杰, 荀航, 袁海华, 等. 基于网络药理学和铁死亡探讨牡荆苷改善心肌缺血再灌注损伤的潜在作用机制[J]. 现代药物与临床, 2024, 39(5): 1123-1133.
    曹霞. 微流控技术牡荆素脂质体的制备及光热和光动力协同抗肿瘤研究[D]. 镇江: 江苏大学, 2022.
    王媛媛. 山楂叶提取物磷脂复合物的构建及其口服生物利用度研究[D]. 南京: 南京中医药大学, 2022.
    Gu C B, Liu Z W, Yuan X H, et al. Preparation of vitexin nanoparticles by combining the antisolvent precipitation and high pressure homogenization approaches followed by lyophilization for dissolution rate enhancement [J]. Molecules, 2017, 22(11): 2038.
    王强. 牡荆素白蛋白纳米粒的制备及其药动学研究[D]. 合肥: 安徽中医药大学, 2023.
    王丽, 高小玲, 李思翰, 等. 五味子乙素-磷脂酰胆碱复合物制备工艺优化及理化性质研究[J]. 化学研究与应用, 2025, 37(7): 2115-2123.
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    2026年第57卷第12期
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    doi: 10.7501/j.issn.0253-2670.2026.12.008
    • 接收时间:2026-01-02
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    2种不同金属材料的力学参数

    Family
    属数
    Number of
    genus
    种数
    Number of
    species
    占总种数比例
    Percentage of
    total species (%)

    Genus
    种数
    Number of
    species
    占总种数比例
    Percentage of total
    species (%)
    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
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