A wide variety of nanomedicine has been designed for cancer therapy. Herein, we describe the synthesis and evaluation of a hypoxia-responsive copolymer for siRNA delivery (Perche et al., Angew Chem Int Ed Engl 53:3362–3366, 2014). The synthesis is achieved using established coupling chemistry and accessible purification procedures. A polyelectrolyte-lipid conjugate (polyethyleneimine 1.8 kDa-dioleylphosphatidylinositol, PEI-PE) and polyethylene glycol 2000 (PEG) were assembled via the hypoxiasensitive azobenzene (Azo) unit to obtain the PEG-Azo-PEI-DOPE copolymer. This copolymer can condense siRNA and shows hypoxia-induced cellular internalization and reporter gene downregulation in vitro and tumor accumulation in vivo after parenteral administration (Perche et al., Angew Chem Int Ed Engl 53:3362–3366, 2014). We also detail procedures to evaluate hypoxia-targeted polymers both in monolayer cultures, cancer cell spheroids and in tumor xenografts murine models.
CITATION STYLE
Perche, F., Biswas, S., Patel, N. R., & Torchilin, V. P. (2016). Hypoxia-responsive copolymer for siRNA delivery. In Methods in Molecular Biology (Vol. 1372, pp. 139–162). Humana Press Inc. https://doi.org/10.1007/978-1-4939-3148-4_12
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