Targeted delivery of miRNA-204-5p by PEGylated polymer nanoparticles for colon cancer therapy.

Aim: miRNAs have been recognized for their potential in cancer therapeutics, and multiple miRNAs were suggested to affect target genes expression. To overcome limitations of free synthetic miRNAs, such as easily degraded in biofluids and limited in cellular uptake, novel miRNAs delivery systems need to be developed.

Materials & Methods: Using surface-functionalizing technique, poly(D,L-lactide-co-glycolide)/poly(L-lactide)-block-poly(ethylene glycol)-folate polymer nanoparticle (PLGA/PLA-PEG-FA) loaded with miR-204-5p (FA-NPs-miR-204) was developed. The therapeutic efficacy of FA-NPs-miR-204 was evaluated in the Luc-HT-29 xenograft tumor model in vivo.

Results: FA-NPs-miR-204 could be taken up by HT-29  and HCT-116 cells efficiently, resulting in significant inhibitory effect on cell proliferation and promotive effect on cell apoptosis. In vivo study showed that FA-NPs-miR-204 could exert tumor suppressive function in Luc-HT-29 xenograft model.

Conclusion: Our study demonstrates a convenient miRNA delivery system that targets tumor tissue and exerts tumor suppressive function, thus demonstrating a potential new therapeutic option for colon cancer.