Fabrication of cationic nanomicelle from chitosan-graft-polycaprolactone as the carrier of 7-ethyl-10-hydroxy-camptothecin

doi:10.1016/j.colsurfb.2009.12.007

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	Fabrication of cationic nanomicelle from chitosan-graft-polycaprolactone as the carrier of 7-ethyl-10-hydroxy-camptothecin
	Duan, Kongrong 4; Zhang, Xiaolan 2,4; Tang, Xiaoxing 4; Yu, Jiahui 4; Liu, Shiyuan 5; Wang, Daxin 1; Li, Yaping3 ; Huang, Jin 2,4
刊名	COLLOIDS AND SURFACES B-BIOINTERFACES
	2010-04-01
卷号	76 期号:2 页码:475-482
关键词	Chitosan-graft-PCL 7-Ethyl-10-hydroxy-camptothecin Cationic polymeric nanomicelles Cytoroxicity Stability
ISSN号	0927-7765
DOI	10.1016/j.colsurfb.2009.12.007
文献子类	Article
英文摘要	In this research, amphiphilic brush-like polycations were synthesized, and used to fabricate cationic nanomicelle as the carrier of 7-ethyl-10-hydroxy-camptothecin (SN-38), in order to enhance its cellular uptake, solubility and stability in aqueous media. In particular, cationic chitosan-graft-polycaprolactone (CS-g-PCL) copolymers were synthesized with a facile one-pot manner via ring-opening polymerization of P-CL onto the hydroxyl groups of CS by using methanesulfonic acid as solvent and catalyst. The formation of CS-g-PCL nanomicelles was confirmed by fluorescence spectrophotoscopy and particle size measurements. It was found that all the nanomicelles showed spherical shapes with narrow size distributions. Their sizes ranged from 47 to 13 run, and the zeta potentials ranged from 26.7 to 50.8 mV, depending on the grafting content of PCL in CS-g-PCL, suggesting their passive targeting to tumor tissue and endocytosis potential. Water-insoluble antitumor drug. SN-38, was easily encapsulated into CS-g-PCL nanomicelles by lyophilization method. In comparison with bare CS-g-PCL nanomicelles, the corresponding SN-38-loaded nanomicelles showed increased particle sizes and a little reduced zeta potentials. With an increase Of grafting PCL content, the drug encapsulation efficiency (EE) and drug loading (DL) of the nanomicelles increased from 64.3 to 84.6% and 6.43 to 8.66%, respectively, whereas their accumulative drug release showed a tendency to decrease due to the enhanced hydrophobic interaction between hydrophobic drug and hydrophobic PCL segments in CS-g-PCL. Also, the CS-g-PCL nanomicelles effectively protected the active lactone ring of SN-38 from hydrolysis under physiological condition, due to the encapsulation of SN-38 into the hydrophobic cores in the nanomicelles. Compared with free SN-38, the SN-38-loaded nanomicelles showed essential decreased cytotoxicity against L929 cell line, and bare CS-g-PCL nanomicelles almost showed non-toxicity. These results suggested the potential utilization of the CS-g-PCL nanomicelles as the carriers of hydrophobic drugs with improving the delivery and release properties. (C) 2009 Elsevier B.V. All rights reserved.
资助项目	973 Projects of Chinese Ministry of Science and Technology[2007CB936104] ; 973 Projects of Chinese Ministry of Science and Technology[2009CB930300] ; Shanghai Municipality Commission for Special Project of Nanometer Science and Technology[0852nm03700] ; Shanghai Municipality Commission for Special Project of Nanometer Science and Technology[0952nm05300] ; Shanghai Municipality Commission for Nongovernmental International Corporation[09540709000]
WOS关键词	EPSILON-CAPROLACTONE ; ANTICANCER DRUGS ; GENE DELIVERY ; CAMPTOTHECIN ; MICELLES ; SERUM ; BIODISTRIBUTION ; NANOPARTICLES ; FORMULATION ; COPOLYMERS
WOS研究方向	Biophysics ; Chemistry ; Materials Science
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000275352800012
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278929]
专题	药物制剂研究中心
通讯作者	Yu, Jiahui
作者单位	1.Yangzhou Univ, Subei Hosp Jiangsu Prov, Yangzhou 225001, Peoples R China; 2.Wuhan Univ Technol, Coll Chem Engn, Wuhan 430070, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, Shanghai 201203, Peoples R China 4.E China Normal Univ, Inst Adv Interdisciplinary Res, Shanghai 200062, Peoples R China; 5.Changzheng Hosp, Dept Diagnost Imaging, Shanghai 200003, Peoples R China;
推荐引用方式 GB/T 7714	Duan, Kongrong,Zhang, Xiaolan,Tang, Xiaoxing,et al. Fabrication of cationic nanomicelle from chitosan-graft-polycaprolactone as the carrier of 7-ethyl-10-hydroxy-camptothecin[J]. COLLOIDS AND SURFACES B-BIOINTERFACES,2010,76(2):475-482.
APA	Duan, Kongrong.,Zhang, Xiaolan.,Tang, Xiaoxing.,Yu, Jiahui.,Liu, Shiyuan.,...&Huang, Jin.(2010).Fabrication of cationic nanomicelle from chitosan-graft-polycaprolactone as the carrier of 7-ethyl-10-hydroxy-camptothecin.COLLOIDS AND SURFACES B-BIOINTERFACES,76(2),475-482.
MLA	Duan, Kongrong,et al."Fabrication of cationic nanomicelle from chitosan-graft-polycaprolactone as the carrier of 7-ethyl-10-hydroxy-camptothecin".COLLOIDS AND SURFACES B-BIOINTERFACES 76.2(2010):475-482.