ABSTRACT
Micellar system, a self-assembling nanoconstruct of amphiphilic copolymers with a core-shell structure, has received growing scientific attention as an efficient carrier of therapeutics in recent years owing to its solubilization, biocompatibility, high stability, selective targeting, P-glycoprotein inhibition, and altered drug internalization route and subcellular localization properties. This chapter summarizes the micellar systems tested orally for improving drug absorption either by increasing drug membrane permeability and/or by inhibiting drug efflux transporters, bioadhesive micelles which lengthen the residence time in the gastrointestinal tract and promote drug permeation, and pH-sensitive micelles which ensure therapeutic release at its absorption site. This chapter focuses also on the recent developments related to targeted delivery of anticancer therapeutics to tumor sites using micellar approaches via passive and active mechanisms. Furthermore, it elaborates on “smart” multifunctional micelles designed for enhanced biological performance by modification of copolymers to contain chemistries that can sense a specific biological environment. This chapter also
enumerates the strategies developed to enhance in vivo stability of micelles and performances of micelles tested via pulmonary, nasal, and rectal route. Finally, the clinical toxicity of micelles and strategies to improve clinical translation of micelles or other nanomedicines are pinpointed.
