Article(id=1248601551279907351, tenantId=1146029695717560320, journalId=1190317699101192196, issueId=1248601546695528820, articleNumber=1001-2494(2024)07-0605-07, orderNo=null, doi=10.11669/cpj.2024.07.006, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=research-article, receivedDate=1667664000000, receivedDateStr=2022-11-06, revisedDate=null, revisedDateStr=null, acceptedDate=null, acceptedDateStr=null, onlineDate=1775619407720, onlineDateStr=2026-04-08, pubDate=1712505600000, pubDateStr=2024-04-08, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1775619407720, onlineIssueDateStr=2026-04-08, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1775619407720, creator=13701087609, updateTime=1775619407720, updator=13701087609, issue=Issue{id=1248601546695528820, tenantId=1146029695717560320, journalId=1190317699101192196, year='2024', volume='59', issue='7', pageStart='561', pageEnd='656', issueExtLink='null', onlineDate='null', pubDate='null', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1775619406627, creator=13701087609, updateTime=1775619979013, updator=13701087609, preIssue=null, nextIssue=null, ext={EN=IssueExt(id=1248603947515142525, tenantId=1146029695717560320, journalId=1190317699101192196, issueId=1248601546695528820, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1248603947515142526, tenantId=1146029695717560320, journalId=1190317699101192196, issueId=1248601546695528820, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null}, startPage=605, endPage=611, ext={EN=ArticleExt(id=1248601551560925724, articleId=1248601551279907351, tenantId=1146029695717560320, journalId=1190317699101192196, language=EN, title=Pharmacodynamics Study of Paclitaxel-loaded Rhein Conjugate Micelles in Tumor-bearing Mice, columnId=null, journalTitle=Chinese Pharmaceutical Journal, columnName=null, runingTitle=null, highlight=null, articleAbstract=

OBJECTIVE To study the in vivo pharmacodynamics of paclitaxel-loaded TPGS-modified carboxymethyl chitosan-rhein conjugate micelles (PTX/TPGS-CR micelles) in tumor-bearing mice. METHODS The pH and osmotic pressure value of PTX/TPGS-CR micelles were determined. The 4T1 subcutaneous transplanted tumor model was established in Balb/c mice. Taxol^® was used as the positive control, and the tumor growth curve and tumor inhibition rate were used as the main indicators. The safety and efficacy of PTX/TPGS-CR micelles were investigated by observing the changes in body weight, organ index and pathological tissue sections of mice, and measuring the expression of P-gp protein in tumor tissues of each group. RESULTS The pH value was similar to that of 0.9% sodium chloride injection (5.0-7.0), and the osmotic pressure value was 736.6-757.2 kPa. The tumor inhibition rates of Taxol^® and PTX/TPGS-CR micelle in low, medium and high dose groups were 29.91%, 20.87%, 41.06% and 41.84%, respectively. The antitumor effect of PTX/TPGS-CR micelles was better than that of Taxol^® at the same dose (P<0.05), and showed a dose-dependent feature. During the administration period, the body weight and organ of the mice in the PTX/TPGS-CR micelle group at the same dose showed no significantly affected, indicating that PTX/TPGS-CR micelles had better safety. The results of P-gp expression in tumor tissue showed that TPGS-CR micelles could inhibit the expression of P-gp protein. CONCLUSION PTX/TPGS-CR micelle preparation is a nano preparation with high efficiency and low toxicity. It has a good antitumor effect and can reduce the toxicity of PTX. Moreover, it can improve the sensitivity of tumor cells to PTX by inhibiting the expression of P-gp, which is conducive to the treatment of tumors.

, correspAuthors=Xiaoying WANG, Wei XU, 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, authorCompany=null, fund=null, authors=null, authorsList=Weili LU, Huizhi OUYANG, Xueya XU, Chongxian LI, Yaling ZHENG, Xiaoying WANG, Wei XU), CN=ArticleExt(id=1248601553590968974, articleId=1248601551279907351, tenantId=1146029695717560320, journalId=1190317699101192196, language=CN, title=载紫杉醇的大黄酸偶联物胶束在荷瘤小鼠体内药效学研究, columnId=1190352405612040510, journalTitle=中国药学杂志, columnName=论著, runingTitle=null, highlight=null, articleAbstract=

目的 研究载紫杉醇(paclitaxel,PTX)的D-α-生育酚聚乙二醇1000琥珀酸酯(TPGS)修饰的羧甲基壳聚糖-大黄酸偶联物胶束(PTX/TPGS-CR胶束)在荷瘤小鼠体内的药效学。方法 测定PTX/TPGS-CR胶束的pH值及渗透压。采用Balb/c小鼠建立4T1皮下移植瘤模型,以Taxol^®作为阳性对照,以肿瘤生长曲线、抑瘤率等为主要考察指标,通过观察小鼠的体质量变化、脏器指数、病理组织HE染色切片,测定各组肿瘤组织样品P-糖蛋白(P-gp)蛋白表达情况,考察PTX/TPGS-CR胶束的安全性和有效性。结果 PTX/TPGS-CR胶束溶液的pH值与0.9%氯化钠注射液的pH值相近(5.0~7.0),渗透压为736.6~757.2 kPa。Taxol^®和PTX/TPGS-CR胶束低、中、高剂量组的抑瘤率分别为29.91%、20.87%、41.06%及41.84%。PTX/TPGS-CR胶束制剂的抑瘤效果优于同剂量Taxol^®(P<0.05),且对抑瘤效果显示剂量依赖性特征。给药期间,同等剂量下PTX/TPGS-CR胶束组小鼠体质量、器官未受到明显的影响,证明其安全性良好;肿瘤组织P-gp表达结果显示TPGS-CR胶束具有抑制P-gp表达的作用。结论 PTX/TPGS-CR胶束制剂是一种高效、低毒的纳米制剂;其具有良好的抑瘤效果,能降低PTX的毒副作用;并能通过抑制P-gp表达从而提高肿瘤细胞对PTX的敏感性,有利于肿瘤的治疗。

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陆伟利,男,硕士研究生 研究方向:缓控释及靶向药物制剂研究

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陆伟利,男,硕士研究生 研究方向:缓控释及靶向药物制剂研究

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¹⁾P<0.05,²⁾P<0.01, vs control group.

, figureFileSmall=Xf8PlaN6v74QxcQd/FlQ3A==, figureFileBig=BTJ1VLx5R8FBzJdrr+AW3w==, tableContent=null), ArticleFig(id=1249073369535157248, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=CN, label=图1, caption=尾静脉注射Taxol^®与低、中、高剂量羧甲基壳聚糖-大黄酸偶联物(PTX/TPGS-CR)胶束的荷4T1的Balb/c小鼠瘤体积变化. n=12,$\stackrel{-}{x}$±s

与对照组比较,¹⁾ P<0.05, ²⁾ P<0.01。

, figureFileSmall=Xf8PlaN6v74QxcQd/FlQ3A==, figureFileBig=BTJ1VLx5R8FBzJdrr+AW3w==, tableContent=null), ArticleFig(id=1249073369648402439, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=EN, label=Fig.2, caption=Effects of Taxol^® and low, medium and high dose PTX/TPGS-CR micelles by tail vein injection on tumor weight and tumor inhibition rate of 4T1-bearing Balb/c mice. n=12,$\stackrel{-}{x}$±s

¹⁾P<0.05, ²⁾ P<0.01, vs control group.

, figureFileSmall=qmJhnIaVVWRBk7vJJIP7FA==, figureFileBig=TP5FWIxw+c/ecqx7/6sbQQ==, tableContent=null), ArticleFig(id=1249073369723899914, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=CN, label=图2, caption=尾静脉注射Taxol^®与低、中、高剂量PTX/TPGS-CR胶束对荷4T1的Balb/c小鼠瘤质量及抑瘤率的影响. n=12,$\stackrel{-}{x}$±s

与对照组比较,¹⁾ P<0.05, ²⁾ P<0.01。

, figureFileSmall=qmJhnIaVVWRBk7vJJIP7FA==, figureFileBig=TP5FWIxw+c/ecqx7/6sbQQ==, tableContent=null), ArticleFig(id=1249073369795203086, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=EN, label=Fig.3, caption=Effects of Taxol^® and low, medium and high dose PTX/TPGS-CR micelles by tail vein injection on 4T1-bearing Balb/c mice, figureFileSmall=CpQm7bfqr+uqkZrFgeA5zg==, figureFileBig=yIVpYxTtUcBFQopX5FTAfw==, tableContent=null), ArticleFig(id=1249073369908449298, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=CN, label=图3, caption=尾静脉注射Taxol^®与低、中、高剂量PTX/TPGS-CR胶束对荷4T1的Balb/c小鼠治疗效果图, figureFileSmall=CpQm7bfqr+uqkZrFgeA5zg==, figureFileBig=yIVpYxTtUcBFQopX5FTAfw==, tableContent=null), ArticleFig(id=1249073369983946774, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=EN, label=Fig.4, caption=Effects of Taxol^® and low, medium and high dose PTX/TPGS-CR micelles on body weight changes of 4T1-bearing Balb/c mice by tail vein injection. n=12,$\stackrel{-}{x}$±s, figureFileSmall=wf0C/Yqam0gtKqLs2lmTTg==, figureFileBig=AAXSYe/pfK9i9qC7OHviOg==, tableContent=null), ArticleFig(id=1249073370063638553, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=CN, label=图4, caption=尾静脉注射Taxol^®与低、中、高剂量PTX/TPGS-CR胶束对荷4T1的Balb/c小鼠体质量变化的影响. n=12,$\stackrel{-}{x}$±s, figureFileSmall=wf0C/Yqam0gtKqLs2lmTTg==, figureFileBig=AAXSYe/pfK9i9qC7OHviOg==, tableContent=null), ArticleFig(id=1249073371607142433, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=EN, label=Fig.5, caption=Effects of Taxol^® and low, medium and high dose PTX/TPGS-CR micelles by tail vein injection on visceral index of 4T1-bearing Balb/c mice. n=12,$\stackrel{-}{x}$±s

¹⁾ P<0.05, vs control group.

, figureFileSmall=EMl3ttvMdjAHLuM9dqaS3w==, figureFileBig=k4l9kzf/3NWoVShzJdCTtQ==, tableContent=null), ArticleFig(id=1249073371678445605, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=CN, label=图5, caption=尾静脉注射Taxol^®与低、中、高剂量PTX/TPGS-CR胶束对荷4T1的Balb/c小鼠脏器指数的影响. n=12,$\stackrel{-}{x}$±s

与对照组比较,¹⁾ P<0.05。

, figureFileSmall=EMl3ttvMdjAHLuM9dqaS3w==, figureFileBig=k4l9kzf/3NWoVShzJdCTtQ==, tableContent=null), ArticleFig(id=1249073371791691822, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=EN, label=Fig.6, caption=Pathological sections of organs and tumors of 4T1-bearing Balb/c mice administered by tail vein injection of Taxol^® and PTX/TPGS-CR micelles in low, medium and high dose groups (×400), figureFileSmall=xIORlESgFDtMuSJoRtp5KQ==, figureFileBig=MMKYKqNjD/hiVpNap/VcNg==, tableContent=null), ArticleFig(id=1249073371875577907, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=CN, label=图6, caption=尾静脉注射Taxol^®与低、中、高剂量PTX/TPGS-CR胶束的荷4T1的Balb/c小鼠脏器及肿瘤的病理切片(×400), figureFileSmall=xIORlESgFDtMuSJoRtp5KQ==, figureFileBig=MMKYKqNjD/hiVpNap/VcNg==, tableContent=null), ArticleFig(id=1249073371938492471, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=EN, label=Fig.7, caption=Western blot results of tumor tissue in Balb/c mice

a-Control; b-10 mg·kg^-1 Taxol^®; c-5 mg·kg^-1 PTX/TPGS-CR micelles; d-10 mg·kg^-1 PTX/TPGS-CR micelles; e-20 mg·kg^-1 PTX/TPGS-CR micelles.

, figureFileSmall=7j+iX0T/FhWlnE5P3YWy/g==, figureFileBig=1lMiTaownzJH2XXT2oLwCA==, tableContent=null), ArticleFig(id=1249073372047544380, tenantId=1146029695717560320, journalId=1190317699101192196, articleId=1248601551279907351, language=CN, label=图7, caption=Balb/c小鼠肿瘤组织的Western blot实验结果

a-对照组; b-10 mg·kg^-1市售Taxol^®; c-5 mg·kg^-1 PTX/TPGS-CR胶束; d-10 mg·kg^-1 PTX/TPGS-CR胶束; e-20 mg·kg^-1 PTX/TPGS-CR胶束。

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