中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Efficient Delivery of Antitumor Drug to the Nuclei of Tumor Cells by Amphiphilic Biodegradable Poly(L-Aspartic Acid-co-Lactic Acid)/DPPE Co-Polymer Nanoparticles

文献类型:期刊论文

作者Han, SY; Liu, YX; Nie, X; Xu, Q; Jiao, F; Li, W; Zhao, YL; Wu, Y; Chen, CY; 李炜(多)
刊名SMALL
出版日期2012
卷号8期号:10页码:1596-1606
关键词biodegradable co-polymers nanoparticles controlled drug release nucleus-targeted drug delivery tumor inhibition
英文摘要The use of biodegradable polymeric nanoparticles (NPs) for controlled drug delivery has shown significant therapeutic potential. Polyaspartic acid and polylactic acid are the most intensively studied biodegradable polymers. In the present study, novel amphiphilic biodegradable co-polymer NPs, poly(L-aspartic acid-co-lactic acid) with 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) (poly(AA-co-LA)/DPPE) is synthesized and subsequently used to encapsulate an antitumor drug doxorubicin (DOX). The formulation parameters of the NPs are optimized to improve encapsulation efficiency. The resulting drug-loaded NPs possess better size homogeneity (polydispersity) and exhibit pH-responsive drug release profiles. Cellular viability assays indicate that the poly(AA-co-LA)/DPPE NPs did not induce cell death, whereas doxorubicin encapsulated NPs were cytotoxic to various types of tumor cells. In addition, the free NPs could not enter the cell nuclei after internalized in tumor cells. The DOX-loaded NPs exhibit efficient intracellular delivery in tumor cells with co-localization in lysosome and delay entering into the nucleus, which suggests a time- and pH-dependent drug release profile within cells. When applied to deliver chemotherapeutics to a mouse xenograft model of human lung adenocarcinoma, DOX-loaded NPs have a comparable antitumor activity with free DOX, and greatly reduce systemic toxicity and mortality. The delivery of cytotoxic drugs directly to the nucleus specifically within tumor cells is of great interest. These results demonstrate the feasibility of the application of the amphiphilic polyaspartic acid derivative, poly(AA-co-LA)/DPPE, as a nanocarrier for cell nuclear delivery of potent antitumor drugs.
学科主题Chemistry; Science & Technology - Other Topics; Materials Science; Physics
收录类别SCI
WOS记录号WOS:000304001000017
公开日期2016-05-03
源URL[http://ir.ihep.ac.cn/handle/311005/224156]  
专题高能物理研究所_多学科研究中心
推荐引用方式
GB/T 7714
Han, SY,Liu, YX,Nie, X,et al. Efficient Delivery of Antitumor Drug to the Nuclei of Tumor Cells by Amphiphilic Biodegradable Poly(L-Aspartic Acid-co-Lactic Acid)/DPPE Co-Polymer Nanoparticles[J]. SMALL,2012,8(10):1596-1606.
APA Han, SY.,Liu, YX.,Nie, X.,Xu, Q.,Jiao, F.,...&李炜.(2012).Efficient Delivery of Antitumor Drug to the Nuclei of Tumor Cells by Amphiphilic Biodegradable Poly(L-Aspartic Acid-co-Lactic Acid)/DPPE Co-Polymer Nanoparticles.SMALL,8(10),1596-1606.
MLA Han, SY,et al."Efficient Delivery of Antitumor Drug to the Nuclei of Tumor Cells by Amphiphilic Biodegradable Poly(L-Aspartic Acid-co-Lactic Acid)/DPPE Co-Polymer Nanoparticles".SMALL 8.10(2012):1596-1606.

入库方式: OAI收割

来源:高能物理研究所

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