Poly(HPMA)-chlorambucil conjugate nanoparticles: facile fabrication and anti-cancer activity
Herein, the clinically approved nitrogen mustard, chlorambucil (Chl), is covalently embedded into a poly( N -(2-hydroxypropyl)methacrylamide, HPMA) vector via a hydrolysable ester bond to overcome the shortcomings of Chl as well as to achieve better efficacy. The well-defined poly-prodrug amphiphile...
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| Veröffentlicht in: | New journal of chemistry 2021-10, Vol.45 (39), p.18544-18551 |
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| container_issue | 39 |
| container_start_page | 18544 |
| container_title | New journal of chemistry |
| container_volume | 45 |
| creator | Li, Guichen Zhao, Minzhi Zhang, Jia Li, Haining Xu, Weibing Pu, Lumei Shi, Xinhe |
| description | Herein, the clinically approved nitrogen mustard, chlorambucil (Chl), is covalently embedded into a poly(
N
-(2-hydroxypropyl)methacrylamide, HPMA) vector
via
a hydrolysable ester bond to overcome the shortcomings of Chl as well as to achieve better efficacy. The well-defined poly-prodrug amphiphiles with Chl loading content >10 wt% can form uniform nanoparticles with an average diameter of 200 nm through a macromolecular self-assembly strategy. The detailed structure information and Chl release properties are carefully inspected. Cytotoxicity studies against the HepG2 and MCF-7 cell lines combined with flow cytometry reveal that the poly(HPMA)-Chl conjugate exhibits obvious targeting ability and markedly enhanced antitumor effect compared to the free Chl. After labelling with a fluorescent group, the cell uptake, lysosome escape and distribution in living organs of the poly-prodrug were also studied.
An acid-sensitive poly(HPMA)-Chl conjugate was developed and its antitumor effect towards HepG2 and MCF-7 cells was evaluated. |
| doi_str_mv | 10.1039/d1nj03134a |
| format | Article |
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N
-(2-hydroxypropyl)methacrylamide, HPMA) vector
via
a hydrolysable ester bond to overcome the shortcomings of Chl as well as to achieve better efficacy. The well-defined poly-prodrug amphiphiles with Chl loading content >10 wt% can form uniform nanoparticles with an average diameter of 200 nm through a macromolecular self-assembly strategy. The detailed structure information and Chl release properties are carefully inspected. Cytotoxicity studies against the HepG2 and MCF-7 cell lines combined with flow cytometry reveal that the poly(HPMA)-Chl conjugate exhibits obvious targeting ability and markedly enhanced antitumor effect compared to the free Chl. After labelling with a fluorescent group, the cell uptake, lysosome escape and distribution in living organs of the poly-prodrug were also studied.
An acid-sensitive poly(HPMA)-Chl conjugate was developed and its antitumor effect towards HepG2 and MCF-7 cells was evaluated.</description><identifier>ISSN: 1144-0546</identifier><identifier>EISSN: 1369-9261</identifier><identifier>DOI: 10.1039/d1nj03134a</identifier><ispartof>New journal of chemistry, 2021-10, Vol.45 (39), p.18544-18551</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids></links><search><creatorcontrib>Li, Guichen</creatorcontrib><creatorcontrib>Zhao, Minzhi</creatorcontrib><creatorcontrib>Zhang, Jia</creatorcontrib><creatorcontrib>Li, Haining</creatorcontrib><creatorcontrib>Xu, Weibing</creatorcontrib><creatorcontrib>Pu, Lumei</creatorcontrib><creatorcontrib>Shi, Xinhe</creatorcontrib><title>Poly(HPMA)-chlorambucil conjugate nanoparticles: facile fabrication and anti-cancer activity</title><title>New journal of chemistry</title><description>Herein, the clinically approved nitrogen mustard, chlorambucil (Chl), is covalently embedded into a poly(
N
-(2-hydroxypropyl)methacrylamide, HPMA) vector
via
a hydrolysable ester bond to overcome the shortcomings of Chl as well as to achieve better efficacy. The well-defined poly-prodrug amphiphiles with Chl loading content >10 wt% can form uniform nanoparticles with an average diameter of 200 nm through a macromolecular self-assembly strategy. The detailed structure information and Chl release properties are carefully inspected. Cytotoxicity studies against the HepG2 and MCF-7 cell lines combined with flow cytometry reveal that the poly(HPMA)-Chl conjugate exhibits obvious targeting ability and markedly enhanced antitumor effect compared to the free Chl. After labelling with a fluorescent group, the cell uptake, lysosome escape and distribution in living organs of the poly-prodrug were also studied.
An acid-sensitive poly(HPMA)-Chl conjugate was developed and its antitumor effect towards HepG2 and MCF-7 cells was evaluated.</description><issn>1144-0546</issn><issn>1369-9261</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid/><recordid>eNqFjj2LAjEURYMo-NnYCyl3i2ieGUfGbpEVG8HCUpDnM2qGmEgShfn3TiFYWlzOhdMcxoYgxyBVMTmBK6UClWGDdUDlhSimOTTrD1km5CzL26wbYyklwDyHDttvva1-1tvN36-gq_UBb8cHGcvJu_JxwaS5Q-fvGJIhq-OCn7HWusYxGMJkvOPoTvWSEYSOdOBIyTxNqvqsdUYb9eDNHhut_nfLtQiRDvdgbhiqwydZffMvXkxFVg</recordid><startdate>20211011</startdate><enddate>20211011</enddate><creator>Li, Guichen</creator><creator>Zhao, Minzhi</creator><creator>Zhang, Jia</creator><creator>Li, Haining</creator><creator>Xu, Weibing</creator><creator>Pu, Lumei</creator><creator>Shi, Xinhe</creator><scope/></search><sort><creationdate>20211011</creationdate><title>Poly(HPMA)-chlorambucil conjugate nanoparticles: facile fabrication and anti-cancer activity</title><author>Li, Guichen ; Zhao, Minzhi ; Zhang, Jia ; Li, Haining ; Xu, Weibing ; Pu, Lumei ; Shi, Xinhe</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-rsc_primary_d1nj03134a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><creationdate>2021</creationdate><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Li, Guichen</creatorcontrib><creatorcontrib>Zhao, Minzhi</creatorcontrib><creatorcontrib>Zhang, Jia</creatorcontrib><creatorcontrib>Li, Haining</creatorcontrib><creatorcontrib>Xu, Weibing</creatorcontrib><creatorcontrib>Pu, Lumei</creatorcontrib><creatorcontrib>Shi, Xinhe</creatorcontrib><jtitle>New journal of chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Li, Guichen</au><au>Zhao, Minzhi</au><au>Zhang, Jia</au><au>Li, Haining</au><au>Xu, Weibing</au><au>Pu, Lumei</au><au>Shi, Xinhe</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Poly(HPMA)-chlorambucil conjugate nanoparticles: facile fabrication and anti-cancer activity</atitle><jtitle>New journal of chemistry</jtitle><date>2021-10-11</date><risdate>2021</risdate><volume>45</volume><issue>39</issue><spage>18544</spage><epage>18551</epage><pages>18544-18551</pages><issn>1144-0546</issn><eissn>1369-9261</eissn><abstract>Herein, the clinically approved nitrogen mustard, chlorambucil (Chl), is covalently embedded into a poly(
N
-(2-hydroxypropyl)methacrylamide, HPMA) vector
via
a hydrolysable ester bond to overcome the shortcomings of Chl as well as to achieve better efficacy. The well-defined poly-prodrug amphiphiles with Chl loading content >10 wt% can form uniform nanoparticles with an average diameter of 200 nm through a macromolecular self-assembly strategy. The detailed structure information and Chl release properties are carefully inspected. Cytotoxicity studies against the HepG2 and MCF-7 cell lines combined with flow cytometry reveal that the poly(HPMA)-Chl conjugate exhibits obvious targeting ability and markedly enhanced antitumor effect compared to the free Chl. After labelling with a fluorescent group, the cell uptake, lysosome escape and distribution in living organs of the poly-prodrug were also studied.
An acid-sensitive poly(HPMA)-Chl conjugate was developed and its antitumor effect towards HepG2 and MCF-7 cells was evaluated.</abstract><doi>10.1039/d1nj03134a</doi><tpages>8</tpages></addata></record> |
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| source | Royal Society Of Chemistry Journals 2008-; Alma/SFX Local Collection |
| title | Poly(HPMA)-chlorambucil conjugate nanoparticles: facile fabrication and anti-cancer activity |
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