Biocompatible ionic liquid-based nanoparticles for effective skin penetration and intracellular uptake of antisense oligonucleotides

Abstract

A novel formulation (IL-NP) for the transdermal delivery of nucleic acid medicines was developed using biocompatible ionic liquid (IL). The formulation was created by mixing DNA in water with an IL in ethanol, followed by freeze-drying and dispersion in oil, producing uniformly sized particles. In vitro studies demonstrated the enhanced skin penetration of IL-NP, while mechanistic studies showed that the IL increased cell membrane fluidity to promote cellular uptake. In vivo experiments with tumor-bearing mice confirmed that transdermal administration of IL-NP achieved comparable antitumor effects as direct injection of DNA, without side effects. This formulation effectively overcomes barriers to both stratum corneum penetration and cellular uptake, providing a non-invasive alternative to injecting nucleic acid therapeutics.

Graphical abstract: Biocompatible ionic liquid-based nanoparticles for effective skin penetration and intracellular uptake of antisense oligonucleotides

Supplementary files

Article information

Article type
Paper
Submitted
30 Mar 2025
Accepted
26 Jun 2025
First published
01 Jul 2025
This article is Open Access
Creative Commons BY-NC license

RSC Pharm., 2025, Advance Article

Biocompatible ionic liquid-based nanoparticles for effective skin penetration and intracellular uptake of antisense oligonucleotides

K. Toyofuku, R. Wakabayashi, Y. Kawaguchi, N. Kamiya and M. Goto, RSC Pharm., 2025, Advance Article , DOI: 10.1039/D5PM00087D

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