一种最有吸引力的调控基因表达的方法，名为“microRNA治疗”方法，是基于对活性microRNA(miRNA)进行调控，其细胞内水平在包括癌症在内的多种疾病中发生了异常。这可以通过使用抗microRNA分子来抑制过度表达的microRNA，或者使用microRNA模拟物来恢复与目标疾病相关的低表达的microRNA来实现。研发新的高效、低毒、定向传递这类分子的载体在microRNA药物调节领域是一个关键课题。我们比较了一小组带正电的柱[4]芳烃载体与荧光抗microRNA分子（肽核酸，PNAs）、预microRNA（microRNA前体）和成熟microRNA在脑胶质瘤细胞和结肠癌细胞模型中的传递效率。传递效率通过细胞荧光测定、细胞成像试验和RT-qPCR来进行评估。柱[4]芳烃载体显示出是促进中性（PNAs）和带负电（预microRNA和成熟microRNA）分子摄取的强大工具，对转染细胞具有低毒性，并且在传递效率方面能与商业化载体竞争。这些结果对验证microRNA治疗方法在个性化治疗和精准医学中的未来应用具有重要意义。

One of the most appealing approaches for regulating gene expression, named the "microRNA therapeutic" method, is based on the regulation of the activity of microRNAs (miRNAs), the intracellular levels of which are dysregulated in many diseases, including cancer. This can be achieved by miRNA inhibition with antimiRNA molecules in the case of overexpressed microRNAs, or by using miRNA-mimics to restore downregulated microRNAs that are associated with the target disease. The development of new efficient, low-toxic, and targeted vectors of such molecules represents a key topic in the field of the pharmacological modulation of microRNAs. We compared the delivery efficiency of a small library of cationic calix[4]arene vectors complexed with fluorescent antimiRNA molecules (Peptide Nucleic Acids, PNAs), pre-miRNA (microRNA precursors), and mature microRNAs, in glioma- and colon-cancer cellular models. The transfection was assayed by cytofluorimetry, cell imaging assays, and RT-qPCR. The calix[4]arene-based vectors were shown to be powerful tools to facilitate the uptake of both neutral (PNAs) and negatively charged (pre-miRNAs and mature microRNAs) molecules showing low toxicity in transfected cells and ability to compete with commercially available vectors in terms of delivery efficiency. These results could be of great interest to validate microRNA therapeutics approaches for future application in personalized treatment and precision medicine.