A simple method to improve the stability of docetaxel micelles
Self-assembled polymeric micelles have been widely applied in drug delivery systems. In this study, we found that pH value of micellar system solution was the decisive factor of physical stability. Furthermore, the weak basic solution could maintain the solution clarification for a relative long tim...
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Veröffentlicht in: | Scientific reports 2016-11, Vol.6 (1), p.36957, Article 36957 |
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description | Self-assembled polymeric micelles have been widely applied in drug delivery systems. In this study, we found that pH value of micellar system solution was the decisive factor of physical stability. Furthermore, the weak basic solution could maintain the solution clarification for a relative long time. To investigate the stability of polymeric micelles in different pH solutions, the micellar particle size and the docetaxel content remaining in solution were detected at predetermined time points. The crystallographic assay of freeze-drying powder was characterized by an X-ray diffractometer.
In vitro
release results indicated that the PBS had little influence on the sustained-release effect of docetaxel-loaded polymeric micelles (DPM). Besides, the safety of micellar formulation was determined by an MTT assay on HEK293 cells, and the anti-tumor activity was tested on MCF-7 cells. The results demonstrated that DPM adjusted with PBS (DPM (PBS)) was of low toxicity and maintained the effectiveness of docetaxel.
In vivo
antitumor results indicated that DPM (PBS) had better antitumor efficacy than common docetaxel injection (DTX). Thus it was concluded that regulation of micellar solution PH by PBS is a safe and effective method to improve the physical stability of DPM. It might promote the application of micellar formulation in clinical applications. |
doi_str_mv | 10.1038/srep36957 |
format | Article |
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In vitro
release results indicated that the PBS had little influence on the sustained-release effect of docetaxel-loaded polymeric micelles (DPM). Besides, the safety of micellar formulation was determined by an MTT assay on HEK293 cells, and the anti-tumor activity was tested on MCF-7 cells. The results demonstrated that DPM adjusted with PBS (DPM (PBS)) was of low toxicity and maintained the effectiveness of docetaxel.
In vivo
antitumor results indicated that DPM (PBS) had better antitumor efficacy than common docetaxel injection (DTX). Thus it was concluded that regulation of micellar solution PH by PBS is a safe and effective method to improve the physical stability of DPM. It might promote the application of micellar formulation in clinical applications.</description><identifier>ISSN: 2045-2322</identifier><identifier>EISSN: 2045-2322</identifier><identifier>DOI: 10.1038/srep36957</identifier><identifier>PMID: 27833135</identifier><language>eng</language><publisher>London: Nature Publishing Group UK</publisher><subject>140/131 ; 631/154/152 ; 692/308/153 ; Antitumor activity ; Antitumor agents ; Breast cancer ; Clinical trials ; Controlled release ; Drug delivery ; Drug delivery systems ; Drugs ; Freeze drying ; Humanities and Social Sciences ; Lung cancer ; Micelles ; multidisciplinary ; Particle size ; pH effects ; Polymers ; Powder ; Science ; Therapeutic applications ; Toxicity</subject><ispartof>Scientific reports, 2016-11, Vol.6 (1), p.36957, Article 36957</ispartof><rights>The Author(s) 2016</rights><rights>Copyright Nature Publishing Group Nov 2016</rights><rights>Copyright © 2016, The Author(s) 2016 The Author(s)</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c438t-13b9d9b6b3f4c0420c1728874c2477468c3719930ebba752bd0038eda47205d3</citedby><cites>FETCH-LOGICAL-c438t-13b9d9b6b3f4c0420c1728874c2477468c3719930ebba752bd0038eda47205d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC5105067/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC5105067/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,723,776,780,860,881,27901,27902,41096,42165,51551,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27833135$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Zhang, Lan</creatorcontrib><creatorcontrib>Tan, LiWei</creatorcontrib><creatorcontrib>Chen, LiJuan</creatorcontrib><creatorcontrib>Chen, XiaoXin</creatorcontrib><creatorcontrib>Long, ChaoFeng</creatorcontrib><creatorcontrib>Peng, JinRong</creatorcontrib><creatorcontrib>Qian, ZhiYong</creatorcontrib><title>A simple method to improve the stability of docetaxel micelles</title><title>Scientific reports</title><addtitle>Sci Rep</addtitle><addtitle>Sci Rep</addtitle><description>Self-assembled polymeric micelles have been widely applied in drug delivery systems. In this study, we found that pH value of micellar system solution was the decisive factor of physical stability. Furthermore, the weak basic solution could maintain the solution clarification for a relative long time. To investigate the stability of polymeric micelles in different pH solutions, the micellar particle size and the docetaxel content remaining in solution were detected at predetermined time points. The crystallographic assay of freeze-drying powder was characterized by an X-ray diffractometer.
In vitro
release results indicated that the PBS had little influence on the sustained-release effect of docetaxel-loaded polymeric micelles (DPM). Besides, the safety of micellar formulation was determined by an MTT assay on HEK293 cells, and the anti-tumor activity was tested on MCF-7 cells. The results demonstrated that DPM adjusted with PBS (DPM (PBS)) was of low toxicity and maintained the effectiveness of docetaxel.
In vivo
antitumor results indicated that DPM (PBS) had better antitumor efficacy than common docetaxel injection (DTX). Thus it was concluded that regulation of micellar solution PH by PBS is a safe and effective method to improve the physical stability of DPM. It might promote the application of micellar formulation in clinical applications.</description><subject>140/131</subject><subject>631/154/152</subject><subject>692/308/153</subject><subject>Antitumor activity</subject><subject>Antitumor agents</subject><subject>Breast cancer</subject><subject>Clinical trials</subject><subject>Controlled release</subject><subject>Drug delivery</subject><subject>Drug delivery systems</subject><subject>Drugs</subject><subject>Freeze drying</subject><subject>Humanities and Social Sciences</subject><subject>Lung cancer</subject><subject>Micelles</subject><subject>multidisciplinary</subject><subject>Particle size</subject><subject>pH effects</subject><subject>Polymers</subject><subject>Powder</subject><subject>Science</subject><subject>Therapeutic applications</subject><subject>Toxicity</subject><issn>2045-2322</issn><issn>2045-2322</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>C6C</sourceid><sourceid>BENPR</sourceid><recordid>eNplkEtLAzEUhYMoVmoX_gEJuFIYzXMy2RRK8QUFN92HSSbTTpmZ1CQt9t8baS0V7yb3cj_OuTkA3GD0iBEtnoK3a5pLLs7AFUGMZ4QScn7SD8AohBVKxYlkWF6CAREFpZjyKzCewNB069bCzsalq2B0MM3ebS2MSwtDLHXTNnEHXQ0rZ2wsv2wLu8bYtrXhGlzUZRvs6PAOwfzleT59y2Yfr-_TySwzjBYxw1TLSupc05oZxAgyWJCiEMwQJgTLC0MFlpIiq3UpONEVSl-zVckEQbyiQzDey643urOVsX30ZavWvulKv1OubNTfTd8s1cJtFceIo1wkgbuDgHefGxuiWrmN79PJChfJmDIui0Td7ynjXUi51kcHjNRP2OoYdmJvT086kr_RJuBhD4S06hfWn1j-U_sGvdaIHw</recordid><startdate>20161111</startdate><enddate>20161111</enddate><creator>Zhang, Lan</creator><creator>Tan, LiWei</creator><creator>Chen, LiJuan</creator><creator>Chen, XiaoXin</creator><creator>Long, ChaoFeng</creator><creator>Peng, JinRong</creator><creator>Qian, ZhiYong</creator><general>Nature Publishing Group UK</general><general>Nature Publishing Group</general><scope>C6C</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7X7</scope><scope>7XB</scope><scope>88A</scope><scope>88E</scope><scope>88I</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AEUYN</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M2P</scope><scope>M7P</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>Q9U</scope><scope>5PM</scope></search><sort><creationdate>20161111</creationdate><title>A simple method to improve the stability of docetaxel micelles</title><author>Zhang, Lan ; Tan, LiWei ; Chen, LiJuan ; Chen, XiaoXin ; Long, ChaoFeng ; Peng, JinRong ; Qian, ZhiYong</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c438t-13b9d9b6b3f4c0420c1728874c2477468c3719930ebba752bd0038eda47205d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>140/131</topic><topic>631/154/152</topic><topic>692/308/153</topic><topic>Antitumor activity</topic><topic>Antitumor agents</topic><topic>Breast cancer</topic><topic>Clinical trials</topic><topic>Controlled release</topic><topic>Drug delivery</topic><topic>Drug delivery systems</topic><topic>Drugs</topic><topic>Freeze drying</topic><topic>Humanities and Social Sciences</topic><topic>Lung cancer</topic><topic>Micelles</topic><topic>multidisciplinary</topic><topic>Particle size</topic><topic>pH effects</topic><topic>Polymers</topic><topic>Powder</topic><topic>Science</topic><topic>Therapeutic applications</topic><topic>Toxicity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Zhang, Lan</creatorcontrib><creatorcontrib>Tan, LiWei</creatorcontrib><creatorcontrib>Chen, LiJuan</creatorcontrib><creatorcontrib>Chen, XiaoXin</creatorcontrib><creatorcontrib>Long, ChaoFeng</creatorcontrib><creatorcontrib>Peng, JinRong</creatorcontrib><creatorcontrib>Qian, ZhiYong</creatorcontrib><collection>Springer Nature OA Free Journals</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Biology Database (Alumni Edition)</collection><collection>Medical Database (Alumni Edition)</collection><collection>Science Database (Alumni Edition)</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest One Sustainability</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Natural Science Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Science Database</collection><collection>Biological Science Database</collection><collection>Publicly Available Content Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central Basic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Scientific reports</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Zhang, Lan</au><au>Tan, LiWei</au><au>Chen, LiJuan</au><au>Chen, XiaoXin</au><au>Long, ChaoFeng</au><au>Peng, JinRong</au><au>Qian, ZhiYong</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A simple method to improve the stability of docetaxel micelles</atitle><jtitle>Scientific reports</jtitle><stitle>Sci Rep</stitle><addtitle>Sci Rep</addtitle><date>2016-11-11</date><risdate>2016</risdate><volume>6</volume><issue>1</issue><spage>36957</spage><pages>36957-</pages><artnum>36957</artnum><issn>2045-2322</issn><eissn>2045-2322</eissn><abstract>Self-assembled polymeric micelles have been widely applied in drug delivery systems. In this study, we found that pH value of micellar system solution was the decisive factor of physical stability. Furthermore, the weak basic solution could maintain the solution clarification for a relative long time. To investigate the stability of polymeric micelles in different pH solutions, the micellar particle size and the docetaxel content remaining in solution were detected at predetermined time points. The crystallographic assay of freeze-drying powder was characterized by an X-ray diffractometer.
In vitro
release results indicated that the PBS had little influence on the sustained-release effect of docetaxel-loaded polymeric micelles (DPM). Besides, the safety of micellar formulation was determined by an MTT assay on HEK293 cells, and the anti-tumor activity was tested on MCF-7 cells. The results demonstrated that DPM adjusted with PBS (DPM (PBS)) was of low toxicity and maintained the effectiveness of docetaxel.
In vivo
antitumor results indicated that DPM (PBS) had better antitumor efficacy than common docetaxel injection (DTX). Thus it was concluded that regulation of micellar solution PH by PBS is a safe and effective method to improve the physical stability of DPM. It might promote the application of micellar formulation in clinical applications.</abstract><cop>London</cop><pub>Nature Publishing Group UK</pub><pmid>27833135</pmid><doi>10.1038/srep36957</doi><oa>free_for_read</oa></addata></record> |
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subjects | 140/131 631/154/152 692/308/153 Antitumor activity Antitumor agents Breast cancer Clinical trials Controlled release Drug delivery Drug delivery systems Drugs Freeze drying Humanities and Social Sciences Lung cancer Micelles multidisciplinary Particle size pH effects Polymers Powder Science Therapeutic applications Toxicity |
title | A simple method to improve the stability of docetaxel micelles |
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