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Acerola exosome-like nanovesicles to systemically deliver nucleic acid medicine via oral administration


ABSTRACT: Extracellular vesicles derived from mammalian cells could be useful carriers for drug delivery systems (DDSs); however, with regard to clinical application, there are several issues to be overcome. Acerola (Malpighia emarginata DC.) is a popular health food. In this study, the feasibility of orally administered nucleic acid drug delivery by acerola exosome-like nanoparticles (AELNs) was examined. AELNs were recovered from acerola juice using an affinity column instead of ultracentrifugation. MicroRNA (miRNA) was sufficiently encapsulated in AELNs by 30-min incubation on ice and was protected against RNase, strong acid, and base treatments. The administration of an AELN/miRNA mixture in cells achieved downregulation of the miRNA’s target gene, and this mixture showed cytoplasmic localization. AELNs orally delivered small RNA to the digestive system in vivo. The target gene-suppressing effect in the small intestine and liver peaked 1 day after administration, indicating potential for use as an oral DDS for nucleic acid in the digestive system. Graphical abstract Encapsulation of nucleic acids in acerola exosome-like nanovesicles (AELNs) had protective effects against RNase, acid, and base treatments. Kuroda and colleagues demonstrated that oral administration of AELNs enabled the functions of nucleic acids to be exerted in the digestive tract, and it is expected to become a new method for loading nucleic acids.

SUBMITTER: Umezu T 

PROVIDER: S-EPMC8010214 | biostudies-literature |

REPOSITORIES: biostudies-literature

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