Cancer stem cells (CSCs) are a small subpopulation of cells within tumors that retain the properties of self-renewal and tumorigenicity in vivo. Although CSCs have been reported in multiple cancers, the regulation of CSCs has not been described at the molecular level. miRNAs are endogenous small noncoding RNAs that post-transcriptionally regulate the expression of their target genes via RNA interference and are involved in almost all cellular processes. Since aberrant miRNA expression occurs in CSCs, such dysregulated miRNAs may be promising therapeutic targets. In this review, we summarize the current knowledge regarding miRNAs that regulate CSC properties and discuss an in vivo delivery system for synthetic miRNA mimics and miRNA inhibitors for the development of innovative miRNA therapy against CSCs.