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Polymers 2018, 10(9), 953; https://doi.org/10.3390/polym10090953

Inhibition of Tumor Growth via Systemic siRNA Delivery Using Reducible Bile Acid-Conjugated Polyethylenimine

School of Pharmacy, Sungkyunkwan University, Suwon 16419, Korea
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Received: 1 August 2018 / Revised: 15 August 2018 / Accepted: 18 August 2018 / Published: 27 August 2018
(This article belongs to the Special Issue Polymeric Micro/Nanoparticles for Bio-Medical Applications)
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Abstract

RNA 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
Keywords: small interfering RNA; deoxycholic acid; stabilized polyplex; disulfide crosslinking; systemic gene therapy small interfering RNA; deoxycholic acid; stabilized polyplex; disulfide crosslinking; systemic gene therapy
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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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.

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