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Bioconjug Chem. 2017 Aug 16;28(8):2051-2061. doi: 10.1021/acs.bioconjchem.7b00222. Epub 2017 Jul 26.

Amphiphilic siRNA Conjugates for Co-Delivery of Nucleic Acids and Hydrophobic Drugs.

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Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, Swiss Federal Institute of Technology Zurich (ETHZ) , Vladimir-Prelog-Weg, Zurich 8093, Switzerland.
Basic Research & Innovation Division, AmorePacific Corporation R&D Unit , Yongin 446-729, Republic of Korea.
National Institute of Biomedical Imaging and Bioengineering , 9000 Rockville Pike, Bethesda, Maryland 20892, United States.
Department of Biological Science, Korea Advanced Institute of Science and Technology (KAIST) , Daejeon 305-701, Republic of Korea.
Department of Bioscience and Biotechnology, Konkuk University , Seoul 143-701, Republic of Korea.


Combination therapy of nucleic acids and chemical drugs for cancer treatment is a promising strategy to enhance the therapeutic efficacy by simultaneously regulating multiple troublesome pathways. In this study, we report on polyethylene glycol-siRNA-polycaprolactone (PEG-siRNA-PCL) micelles that encapsulate hydrophobic drugs for efficient co-delivery of siRNA and drugs to cancer cells. Amphiphilic PEG-siRNA-PCL copolymers were synthesized by annealing antisense siRNA-PCL conjugates with sense siRNA-PEG conjugates. After paclitaxel encapsulation, PEG-siRNA-PCL micelles containing antiapoptotic Bcl-2-specific siRNA were stabilized with linear polyethylenimine via electrostatic interactions. Stabilized PEG-siRNA-PCL micelles showed superior anticancer effects, assessed by caspase-3 activity analysis, apoptotic cell staining, and a cytotoxicity test, to those of paclitaxel-free PEG-siRNA-PCL micelles and unmodified siRNAs. The strong anticancer activity of paclitaxel-incorporated siRNA micelles can be attributed to the synergistic effect of Bcl-2 siRNA and paclitaxel. This work provides an efficient co-delivery platform for combination anticancer therapy with siRNA and chemotherapy.

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