pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer

Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun...
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Autor*in:	Hao DL [verfasserIn] Xie R [verfasserIn] De GJ [verfasserIn] Yi H [verfasserIn] Zang C [verfasserIn] Yang MY [verfasserIn] Liu L [verfasserIn] Ma H [verfasserIn] Cai WY [verfasserIn] Zhao QH [verfasserIn] Sui F [verfasserIn] Chen YJ [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2020

Schlagwörter:	artesunate micelles ph responsive polymer prodrug poly(2-ethyl-2-oxazoline) poly(β-amino ester)

Übergeordnetes Werk:	In: International Journal of Nanomedicine - Dove Medical Press, 2018, (2020), Seite 1771-1786
Übergeordnetes Werk:	year:2020 ; pages:1771-1786

Links:	Link aufrufen Link aufrufen Journal toc

Katalog-ID:	DOAJ061556378

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520			\|a Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun Chen Tel/ Fax +86-10-84036059Email qhzhaoicmm.ac.cn; yjchen@icmm.ac.cnPurpose: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model.Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core.Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%+- 1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor.Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.Keywords: artesunate, micelles, pH responsive, polymer prodrug, poly(2-ethyl-2-oxazoline), poly(β-amino ester)
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allfields	(DE-627)DOAJ061556378 (DE-599)DOAJ4bdfa964c95744eea285336c8d5f18f4 DE-627 ger DE-627 rakwb eng R5-920 Hao DL verfasserin aut pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun Chen Tel/ Fax +86-10-84036059Email qhzhaoicmm.ac.cn; yjchen@icmm.ac.cnPurpose: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model.Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core.Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%+- 1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor.Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.Keywords: artesunate, micelles, pH responsive, polymer prodrug, poly(2-ethyl-2-oxazoline), poly(β-amino ester) artesunate micelles ph responsive polymer prodrug poly(2-ethyl-2-oxazoline) poly(β-amino ester) Medicine (General) Xie R verfasserin aut De GJ verfasserin aut Yi H verfasserin aut Zang C verfasserin aut Yang MY verfasserin aut Liu L verfasserin aut Ma H verfasserin aut Cai WY verfasserin aut Zhao QH verfasserin aut Sui F verfasserin aut Chen YJ verfasserin aut In International Journal of Nanomedicine Dove Medical Press, 2018 (2020), Seite 1771-1786 (DE-627)537879560 (DE-600)2377464-2 11782013 nnns year:2020 pages:1771-1786 https://doaj.org/article/4bdfa964c95744eea285336c8d5f18f4 kostenfrei https://www.dovepress.com/ph-responsive-artesunate-polymer-prodrugs-with-enhanced-ablation-effec-peer-reviewed-article-IJN kostenfrei https://doaj.org/toc/1178-2013 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 2020 1771-1786
spelling	(DE-627)DOAJ061556378 (DE-599)DOAJ4bdfa964c95744eea285336c8d5f18f4 DE-627 ger DE-627 rakwb eng R5-920 Hao DL verfasserin aut pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun Chen Tel/ Fax +86-10-84036059Email qhzhaoicmm.ac.cn; yjchen@icmm.ac.cnPurpose: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model.Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core.Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%+- 1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor.Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.Keywords: artesunate, micelles, pH responsive, polymer prodrug, poly(2-ethyl-2-oxazoline), poly(β-amino ester) artesunate micelles ph responsive polymer prodrug poly(2-ethyl-2-oxazoline) poly(β-amino ester) Medicine (General) Xie R verfasserin aut De GJ verfasserin aut Yi H verfasserin aut Zang C verfasserin aut Yang MY verfasserin aut Liu L verfasserin aut Ma H verfasserin aut Cai WY verfasserin aut Zhao QH verfasserin aut Sui F verfasserin aut Chen YJ verfasserin aut In International Journal of Nanomedicine Dove Medical Press, 2018 (2020), Seite 1771-1786 (DE-627)537879560 (DE-600)2377464-2 11782013 nnns year:2020 pages:1771-1786 https://doaj.org/article/4bdfa964c95744eea285336c8d5f18f4 kostenfrei https://www.dovepress.com/ph-responsive-artesunate-polymer-prodrugs-with-enhanced-ablation-effec-peer-reviewed-article-IJN kostenfrei https://doaj.org/toc/1178-2013 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 2020 1771-1786
allfields_unstemmed	(DE-627)DOAJ061556378 (DE-599)DOAJ4bdfa964c95744eea285336c8d5f18f4 DE-627 ger DE-627 rakwb eng R5-920 Hao DL verfasserin aut pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun Chen Tel/ Fax +86-10-84036059Email qhzhaoicmm.ac.cn; yjchen@icmm.ac.cnPurpose: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model.Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core.Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%+- 1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor.Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.Keywords: artesunate, micelles, pH responsive, polymer prodrug, poly(2-ethyl-2-oxazoline), poly(β-amino ester) artesunate micelles ph responsive polymer prodrug poly(2-ethyl-2-oxazoline) poly(β-amino ester) Medicine (General) Xie R verfasserin aut De GJ verfasserin aut Yi H verfasserin aut Zang C verfasserin aut Yang MY verfasserin aut Liu L verfasserin aut Ma H verfasserin aut Cai WY verfasserin aut Zhao QH verfasserin aut Sui F verfasserin aut Chen YJ verfasserin aut In International Journal of Nanomedicine Dove Medical Press, 2018 (2020), Seite 1771-1786 (DE-627)537879560 (DE-600)2377464-2 11782013 nnns year:2020 pages:1771-1786 https://doaj.org/article/4bdfa964c95744eea285336c8d5f18f4 kostenfrei https://www.dovepress.com/ph-responsive-artesunate-polymer-prodrugs-with-enhanced-ablation-effec-peer-reviewed-article-IJN kostenfrei https://doaj.org/toc/1178-2013 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 2020 1771-1786
allfieldsGer	(DE-627)DOAJ061556378 (DE-599)DOAJ4bdfa964c95744eea285336c8d5f18f4 DE-627 ger DE-627 rakwb eng R5-920 Hao DL verfasserin aut pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun Chen Tel/ Fax +86-10-84036059Email qhzhaoicmm.ac.cn; yjchen@icmm.ac.cnPurpose: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model.Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core.Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%+- 1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor.Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.Keywords: artesunate, micelles, pH responsive, polymer prodrug, poly(2-ethyl-2-oxazoline), poly(β-amino ester) artesunate micelles ph responsive polymer prodrug poly(2-ethyl-2-oxazoline) poly(β-amino ester) Medicine (General) Xie R verfasserin aut De GJ verfasserin aut Yi H verfasserin aut Zang C verfasserin aut Yang MY verfasserin aut Liu L verfasserin aut Ma H verfasserin aut Cai WY verfasserin aut Zhao QH verfasserin aut Sui F verfasserin aut Chen YJ verfasserin aut In International Journal of Nanomedicine Dove Medical Press, 2018 (2020), Seite 1771-1786 (DE-627)537879560 (DE-600)2377464-2 11782013 nnns year:2020 pages:1771-1786 https://doaj.org/article/4bdfa964c95744eea285336c8d5f18f4 kostenfrei https://www.dovepress.com/ph-responsive-artesunate-polymer-prodrugs-with-enhanced-ablation-effec-peer-reviewed-article-IJN kostenfrei https://doaj.org/toc/1178-2013 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 2020 1771-1786
allfieldsSound	(DE-627)DOAJ061556378 (DE-599)DOAJ4bdfa964c95744eea285336c8d5f18f4 DE-627 ger DE-627 rakwb eng R5-920 Hao DL verfasserin aut pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun Chen Tel/ Fax +86-10-84036059Email qhzhaoicmm.ac.cn; yjchen@icmm.ac.cnPurpose: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model.Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core.Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%+- 1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor.Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.Keywords: artesunate, micelles, pH responsive, polymer prodrug, poly(2-ethyl-2-oxazoline), poly(β-amino ester) artesunate micelles ph responsive polymer prodrug poly(2-ethyl-2-oxazoline) poly(β-amino ester) Medicine (General) Xie R verfasserin aut De GJ verfasserin aut Yi H verfasserin aut Zang C verfasserin aut Yang MY verfasserin aut Liu L verfasserin aut Ma H verfasserin aut Cai WY verfasserin aut Zhao QH verfasserin aut Sui F verfasserin aut Chen YJ verfasserin aut In International Journal of Nanomedicine Dove Medical Press, 2018 (2020), Seite 1771-1786 (DE-627)537879560 (DE-600)2377464-2 11782013 nnns year:2020 pages:1771-1786 https://doaj.org/article/4bdfa964c95744eea285336c8d5f18f4 kostenfrei https://www.dovepress.com/ph-responsive-artesunate-polymer-prodrugs-with-enhanced-ablation-effec-peer-reviewed-article-IJN kostenfrei https://doaj.org/toc/1178-2013 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 2020 1771-1786
language	English
source	In International Journal of Nanomedicine (2020), Seite 1771-1786 year:2020 pages:1771-1786
sourceStr	In International Journal of Nanomedicine (2020), Seite 1771-1786 year:2020 pages:1771-1786
format_phy_str_mv	Article
institution	findex.gbv.de
topic_facet	artesunate micelles ph responsive polymer prodrug poly(2-ethyl-2-oxazoline) poly(β-amino ester) Medicine (General)
isfreeaccess_bool	true
container_title	International Journal of Nanomedicine
authorswithroles_txt_mv	Hao DL @@aut@@ Xie R @@aut@@ De GJ @@aut@@ Yi H @@aut@@ Zang C @@aut@@ Yang MY @@aut@@ Liu L @@aut@@ Ma H @@aut@@ Cai WY @@aut@@ Zhao QH @@aut@@ Sui F @@aut@@ Chen YJ @@aut@@
publishDateDaySort_date	2020-01-01T00:00:00Z
hierarchy_top_id	537879560
id	DOAJ061556378
language_de	englisch
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callnumber-first	R - Medicine
author	Hao DL
spellingShingle	Hao DL misc R5-920 misc artesunate misc micelles misc ph responsive misc polymer prodrug misc poly(2-ethyl-2-oxazoline) misc poly(β-amino ester) misc Medicine (General) pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer
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topic_title	R5-920 pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer artesunate micelles ph responsive polymer prodrug poly(2-ethyl-2-oxazoline) poly(β-amino ester)
topic	misc R5-920 misc artesunate misc micelles misc ph responsive misc polymer prodrug misc poly(2-ethyl-2-oxazoline) misc poly(β-amino ester) misc Medicine (General)
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title	pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer
ctrlnum	(DE-627)DOAJ061556378 (DE-599)DOAJ4bdfa964c95744eea285336c8d5f18f4
title_full	pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer
author_sort	Hao DL
journal	International Journal of Nanomedicine
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author_browse	Hao DL Xie R De GJ Yi H Zang C Yang MY Liu L Ma H Cai WY Zhao QH Sui F Chen YJ
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author-letter	Hao DL
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title_sort	ph-responsive artesunate polymer prodrugs with enhanced ablation effect on rodent xenograft colon cancer
callnumber	R5-920
title_auth	pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer
abstract	Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun Chen Tel/ Fax +86-10-84036059Email qhzhaoicmm.ac.cn; yjchen@icmm.ac.cnPurpose: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model.Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core.Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%+- 1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor.Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.Keywords: artesunate, micelles, pH responsive, polymer prodrug, poly(2-ethyl-2-oxazoline), poly(β-amino ester)
abstractGer	Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun Chen Tel/ Fax +86-10-84036059Email qhzhaoicmm.ac.cn; yjchen@icmm.ac.cnPurpose: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model.Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core.Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%+- 1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor.Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.Keywords: artesunate, micelles, pH responsive, polymer prodrug, poly(2-ethyl-2-oxazoline), poly(β-amino ester)
abstract_unstemmed	Dan-Li Hao, Ran Xie, Ge-Jing De, Hong Yi, Chen Zang, Mi-Yi Yang, Li Liu, Hai Ma, Wei-Yan Cai, Qing-He Zhao, Feng Sui, Yan-Jun Chen Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People’s Republic of ChinaCorrespondence: Qing-He Zhao; Yan-Jun Chen Tel/ Fax +86-10-84036059Email qhzhaoicmm.ac.cn; yjchen@icmm.ac.cnPurpose: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(β-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model.Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core.Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%+- 1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor.Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.Keywords: artesunate, micelles, pH responsive, polymer prodrug, poly(2-ethyl-2-oxazoline), poly(β-amino ester)
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title_short	pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer
url	https://doaj.org/article/4bdfa964c95744eea285336c8d5f18f4 https://www.dovepress.com/ph-responsive-artesunate-polymer-prodrugs-with-enhanced-ablation-effec-peer-reviewed-article-IJN https://doaj.org/toc/1178-2013
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author2	Xie R De GJ Yi H Zang C Yang MY Liu L Ma H Cai WY Zhao QH Sui F Chen YJ
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