Journal
POLYMER CHEMISTRY
Volume 7, Issue 23, Pages 3857-3863Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6py00427j
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Funding
- National Basic Research Program of China [2015CB755500]
- National Natural Science Foundation of China [51225305, U1401242, 51373203, 21174166, 31530023, U1501243]
- Natural Science Foundation of the Guangdong Province [2014A030312018]
- Hong Kong SAR Region [2016A050503026]
- Guangdong Innovative and Entrepreneurial Research Team Program [2013S086]
- Guangdong Province
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A pH-sensitive ternary block copolymer comprising poly(ethylene glycol) methyl ether methacrylate (PEGMA), and pH-sensitive segments poly(2-(dimethylamino) ethylmethacrylate) (PDMA) and poly(2( diisopropyl amino) ethyl methacrylate) (PDPA) (mal-PEGMA-b-PDPA-b-PDMA, PMDM) was synthesized. The copolymer effectively complexed with siRNA at pH 5.0 to form a polyplex which showed decreased positive charge along with the increase of pH value due to deprotonation of the PDPA block. The nearly non-charged polyplex at pH 7.4 exhibited enhanced stability and inertness in serum-containing media, which is favorable for a prolonged circulation time and reduced cytotoxicity. The pH-sensitivity of PDMA and PDPA also enhanced the lysosomal escape of polyplexes after endocytosis. Moreover, modification of the tumor-penetrating peptide iRGD endowed the polyplexes with effective intratumoral delivery and high transfection efficiency. A study using the luciferase expression assay achieved highly effective target gene silencing both in vitro and in vivo, which revealed the potential of our iRGD-modified and pH-sensitive siRNA polyplex as a promising siRNA delivery system in cancer treatment.
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