Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers

Peng Fei Gu1, Hui Xu1, Bo Wen Sui2, Jing Xin Gou1, Ling Kuo Meng1, Feng Sun1, Xiu Jun Wang1, Na Qi1, Yu Zhang1, Hai Bing He1, Xing Tang11Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, 2School of Pharmaceutical Sciences, Jilin University, Changchun, People&#39;s Re...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Gu PF, Xu H, Sui BW, Gou JX, Meng LK, Sun F, Wang XJ, Qi N, Zhang Y, He HB, Tang X
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/77460b9f363b4d32b90563fa7eb4f4bf
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:77460b9f363b4d32b90563fa7eb4f4bf
record_format	dspace
spelling	oai:doaj.org-article:77460b9f363b4d32b90563fa7eb4f4bf2021-12-02T02:01:53ZPolymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers1176-91141178-2013https://doaj.org/article/77460b9f363b4d32b90563fa7eb4f4bf2012-01-01T00:00:00Zhttp://www.dovepress.com/polymeric-micelles-based-on-polyethylene-glycol-block-polyracemic-amin-a9003https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Peng Fei Gu1, Hui Xu1, Bo Wen Sui2, Jing Xin Gou1, Ling Kuo Meng1, Feng Sun1, Xiu Jun Wang1, Na Qi1, Yu Zhang1, Hai Bing He1, Xing Tang11Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, 2School of Pharmaceutical Sciences, Jilin University, Changchun, People&#39;s Republic of ChinaAbstract: In this work, racemic hybrid polypeptides poly(ethylene glycol) (PEG)-b-poly(racemic-leucine) (PRL) copolymers with different leucine residues have been synthesized and characterized. Using docetaxel as a model molecule, the high drug-loaded spherical micelles based on PEG-PRL were prepared successfully using dialysis, with a tunable particle size from 170 nm to 250 nm obtained by changing the length of the hydrophobic blocks. Facilitated drug-loading behavior (higher drug-loading ability and easier drug-loading process) of PEG-PRL compared with their corresponding levo forms (PEG-b-poly[levo leucine]) was observed and clarified for the first time. With this facilitation, the highest drug-loading content and efficiency of PEG-PRL micelles can achieve 11.2% &plusmn; 0.4% and 67.2% &plusmn; 2.4%, respectively. All drug-loaded PEG-PRL micelles exhibit a similar release behavior with a sustained release up to 72 hours. The PEG-PRL was shown to be nontoxic against MCF-7 and human umbilical vein endothelial cells up to a concentration of 100 &micro;g/mL, displaying a good biocompatibility. Also, the docetaxel-loaded PEG-PRL micelles were more toxic than the free drug against MCF-7 human breast cancer cells &ndash; both dose and time dependent. Therefore, these high docetaxel-loaded micelles based on racemic hybrid polypeptides appear to be a novel promising nanomedicine for anticancer therapy.Keywords: racemic polypeptides, micelles, conformation, high drug-loading ability, anticancer nanomedicineGu PFXu HSui BWGou JXMeng LKSun FWang XJQi NZhang YHe HBTang XDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 109-122 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Gu PF Xu H Sui BW Gou JX Meng LK Sun F Wang XJ Qi N Zhang Y He HB Tang X Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers
description	Peng Fei Gu1, Hui Xu1, Bo Wen Sui2, Jing Xin Gou1, Ling Kuo Meng1, Feng Sun1, Xiu Jun Wang1, Na Qi1, Yu Zhang1, Hai Bing He1, Xing Tang11Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, 2School of Pharmaceutical Sciences, Jilin University, Changchun, People&#39;s Republic of ChinaAbstract: In this work, racemic hybrid polypeptides poly(ethylene glycol) (PEG)-b-poly(racemic-leucine) (PRL) copolymers with different leucine residues have been synthesized and characterized. Using docetaxel as a model molecule, the high drug-loaded spherical micelles based on PEG-PRL were prepared successfully using dialysis, with a tunable particle size from 170 nm to 250 nm obtained by changing the length of the hydrophobic blocks. Facilitated drug-loading behavior (higher drug-loading ability and easier drug-loading process) of PEG-PRL compared with their corresponding levo forms (PEG-b-poly[levo leucine]) was observed and clarified for the first time. With this facilitation, the highest drug-loading content and efficiency of PEG-PRL micelles can achieve 11.2% &plusmn; 0.4% and 67.2% &plusmn; 2.4%, respectively. All drug-loaded PEG-PRL micelles exhibit a similar release behavior with a sustained release up to 72 hours. The PEG-PRL was shown to be nontoxic against MCF-7 and human umbilical vein endothelial cells up to a concentration of 100 &micro;g/mL, displaying a good biocompatibility. Also, the docetaxel-loaded PEG-PRL micelles were more toxic than the free drug against MCF-7 human breast cancer cells &ndash; both dose and time dependent. Therefore, these high docetaxel-loaded micelles based on racemic hybrid polypeptides appear to be a novel promising nanomedicine for anticancer therapy.Keywords: racemic polypeptides, micelles, conformation, high drug-loading ability, anticancer nanomedicine
format	article
author	Gu PF Xu H Sui BW Gou JX Meng LK Sun F Wang XJ Qi N Zhang Y He HB Tang X
author_facet	Gu PF Xu H Sui BW Gou JX Meng LK Sun F Wang XJ Qi N Zhang Y He HB Tang X
author_sort	Gu PF
title	Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers
title_short	Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers
title_full	Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers
title_fullStr	Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers
title_full_unstemmed	Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers
title_sort	polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/77460b9f363b4d32b90563fa7eb4f4bf
work_keys_str_mv	AT gupf polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT xuh polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT suibw polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT goujx polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT menglk polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT sunf polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT wangxj polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT qin polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT zhangy polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT hehb polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers AT tangx polymericmicellesbasedonpolyethyleneglycolblockpolyracemicaminoacidshybridpolypeptidesconformationfacilitateddrugloadingbehaviorandpotentialapplicationaseffectiveanticancerdrugcarriers
_version_	1718402785059274752

Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers

Ejemplares similares