Linear polyethyleneimine-doxorubicin conjugate for pH-responsive synchronous delivery of drug and microRNA-34a

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• 作者：Hyosook Jung ; Seung An Kim ; Eunjoo Lee ; Hyejung Mok
• 关键词：doxorubicin ; microRNA ; co ; delivery system ; pH ; responsive ; linear polyethyleneimine
• 刊名：Macromolecular Research
• 出版年：2015
• 出版时间：May 2015
• 年：2015
• 卷：23
• 期：5
• 页码：449-456
• 全文大小：646 KB
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• 作者单位：Hyosook Jung (1)
  Seung An Kim (1)
  Eunjoo Lee (1)
  Hyejung Mok (1)
  
  1. Department of Bioscience and Biotechnology, Konkuk University, Seoul, 143-701, Korea
  
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Physical Chemistry
  Polymer Sciences
  Characterization and Evaluation of Materials
  Soft and Granular Matter, Complex Fluids and Microfluidics
  Nanochemistry
  Nanotec
  
• 出版者：The Polymer Society of Korea, co-published with Springer
• ISSN：2092-7673

文摘

Although stimuli-responsive co-delivery systems of chemotherapy drugs and microRNA (miRNA) can serve as a promising treatment strategy for cancer, to our best knowledge, pH-responsive nanocarriers for the codelivery of chemical drugs and microRNAs (miRNAs) have not yet been reported. In this study, we synthesized doxorubicin (DOX)-tethered linear polyethylenimine (LPEI) conjugates linked via a pH-responsive hydrazone bond (LPEI-HZ-DOX) for the synchronous delivery of DOX and miRNA-34a. The free DOX was successfully released from the LPEI-HZ-DOX conjugates at acidic pH, which provided selective toxicity against cancer cells in a pH-sensitive manner. The resulting LPEI-HZ-DOX conjugates formed nano-sized complexes with chemically modified long-chain miRNAs with a size of ?00 nm, which exhibited synergistic toxicity and anti-proliferation activity against PC-3 cancer cells. This platform of cationic conjugates with high biocompatibility could serve as a pH-sensitive in vitro system for gene and drug delivery.