Inhibition of Tumor Growth via Systemic siRNA Delivery Using Reducible Bile Acid-Conjugated Polyethylenimine
AbstractRNA interference (RNAi), mediated by small interfering RNA (siRNA), has been considered as a potential therapeutic agent for cancer owing to its ability to suppress target genes in a sequence-specific manner. In this study, a conjugate of the low molecular weight (MW) polyethylenimine (PEI) (MW 1800) and deoxycholic acid (DA) was further modified with 4-fluorothiophenol (FTP) (TP-DA-PEI) to achieve systemic siRNA delivery. The thiophenol group would be involved with disulfide bonds between the polymer chains and siRNA modified with free thiols (thiol-siRNA) to form and π–π interactions between the pendent aromatic groups and coprostane ring of the bile acid. The TP-DA-PEI conjugates could generate stable nanoparticles with thiol-siRNA. The TP-DA-PEI conjugate not only achieved enhanced intracellular uptake, serum stability, and transfection efficiency, but also showed high accumulation of TP-DA-PEI/thiol-siRNA polyplexes and significant tumor growth inhibition effect in tumor-bearing mice after systemic administration. View Full-Text
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Yin, Y.; Lee, J.E.; Kim, N.W.; Lee, J.H.; Lim, S.Y.; Kim, E.S.; Park, J.W.; Lee, M.S.; Jeong, J.H. Inhibition of Tumor Growth via Systemic siRNA Delivery Using Reducible Bile Acid-Conjugated Polyethylenimine. Polymers 2018, 10, 953.
Yin Y, Lee JE, Kim NW, Lee JH, Lim SY, Kim ES, Park JW, Lee MS, Jeong JH. Inhibition of Tumor Growth via Systemic siRNA Delivery Using Reducible Bile Acid-Conjugated Polyethylenimine. Polymers. 2018; 10(9):953.Chicago/Turabian Style
Yin, Yue; Lee, Jung E.; Kim, Nak W.; Lee, Jong H.; Lim, Su Y.; Kim, E S.; Park, Ji W.; Lee, Min S.; Jeong, Ji H. 2018. "Inhibition of Tumor Growth via Systemic siRNA Delivery Using Reducible Bile Acid-Conjugated Polyethylenimine." Polymers 10, no. 9: 953.
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