Introduction: Adequate transfection efficiency is indispensable to safe and effective delivery of therapeutically active agents, particularly in cancer. Endosomal escape is regarded as a critical and determining step devoted a significant number of studies of the drug/gene delivery field.
Areas Covered: This paper critically reviews the fundamental properties of chloroquine (CQ), its pharmacokinetics, pharmacodynamics, and clinical applications and the present knowledge of CQ application as an endosomal escape enhancing agent.