ABSTRACT

This chapter provides a discussion of the various aspects relating to use of polymeric micelles for formulation of anti-cancer drugs. It presents an information on the physico-chemical properties of micelles, micelle preparation techniques as well as drug loading and release properties of micelles. The chapter highlights the preclinical development of several polymeric micelle formulations that are under clinical trial evaluation for use as cancer therapy. It reviews the interaction between polymeric micelles and cancer cells, including cellular internalization, in vitro cytotoxicity, and chemosensitization of multi-drug resistant cancer cells. The chapter discusses the physico-chemical properties of polymeric micelles are related to their in vivo performance such as in vivo drug release, pharmacokinetics, toxicity profiles, and anti-cancer efficacy. Finally, it introduces the development of several advanced polymeric micelle systems that are capable of targeted delivery to tumors via external stimuli or active targeting mechanisms.