Hydrophobically modified chitosan-based polymeric micelles (CBPMs) are formed through self-aggregation of chitosan amphiphilic derivatives. Their core-shell structure, diversity and the fact that all of their properties are adjustable through reconciling the interactions among their three main constituents: chitosan, hydrophilic segment and hydrophobic segment as well as with the outside medium through changing the ratio and chemical structure of each component's, chemical structure distinguish them from other chitosan-based drug delivery systems (DDSs) and give rise to these promising candidates for targeted delivery of lipophilic anticancer drugs. The majority of review articles conducted previously on chitosan-based DDSs have only made simple differential comparisons between such systems and the anticancer drugs that have been delivered through them. In this review article, all the basic properties of CBPMs including physicochemical, pharmaceutical and biological properties are technically detailed and discussed. The intention of this article is to outline and discuss salient features of CBPMs to contribute to the understanding of optimized strategies for the design of stable and efficient CBPMs.