A worm-like nucleic acid nanostructure for gene delivery and endosomal escape via ClC3 ion exchanger.

Xiao, Yu; Chan, Cecilia Ka Wing; Lee, Leo Kit Cheung; Shyngys, Moldir; Chiu, Yee Ting Elaine; Xue, Evelyn Y; Lui, Kathy Oi-Lan; Chan, Ho Yin Edwin et al. · Sci Adv · 2026

basic_science · Level V

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Abstract

Nanoparticle-based gene delivery can enable therapeutic applications with lower cytotoxicity than viral vectors, but its efficacy is often hampered by endosomal entrapment. We present a nucleic acid nanotechnology approach to circumvent this delivery bottleneck by adsorbing therapeutic nucleic acids (DNA, small interfering RNA, microRNA, or messenger RNA) to a gold-polydopamine nanoworm template, thereby assembling a three-dimensional worm-like nucleic acid nanostructure. Devoid of cationic groups, lipids, or mechanical stimuli, this nanostructure naturally activates the chloride voltage-gated channel 3 (ClC3) ion exchanger in endosomes given its worm-like shape; in turn, ClC3 mediates endosomal H<sup>+</sup> and Cl<sup>-</sup> accumulation and eventual membrane rupture for cytosolic release, contributing to robust endosomal escape with a correlation coefficient <0.2 between the nanostructure and endosomes. We showcase in vitro gene regulation for primary macrophage polarization and mesenchymal stromal cell differentiation, ex vivo programmable mesenchymal stromal cell-based therapy for kidney fibrosis, and in vivo hepatocyte delivery for treating liver injury. Our versatile nucleic acid nanostructure will empower safe and effective gene therapies.

Medical subject headings