Autophagy modulation is considered to be a promising programmed cell death

mechanism to prevent and cure a great number of disorders and diseases. The crucial step in

designing an effective therapeutic approach is to understand the correct and accurate causes of

diseases and to understand whether autophagy plays a cytoprotective or cytotoxic/cytostatic role in

the progression and prevention of disease. This knowledge will help scientists find approaches to

manipulate tumor and pathologic cells in order to enhance cellular sensitivity to therapeutics and

treat them. Although some conventional therapeutics suffer from poor solubility, bioavailability

and controlled release mechanisms, it appears that novel nanoplatforms overcome these obstacles

and have led to the design of a theranostic-controlled drug release system with high solubility and

active targeting and stimuli-responsive potentials. In this review, we discuss autophagy

modulators-related signaling pathways and some of the drug delivery strategies that have been

applied to the field of therapeutic application of autophagy modulators. Moreover, we describe

how therapeutics will target various steps of the autophagic machinery. Furthermore, nano drug

delivery platforms for autophagy targeting and co-delivery of autophagy modulators with

chemotherapeutics/siRNA, are also discussed.

Autophagy modulation is considered to be a promising programmed cell death mechanism to prevent and cure a great number of disorders and diseases. The crucial step in designing an effective therapeutic approach is to understand the correct and accurate causes of diseases and to understand whether autophagy plays a cytoprotective or cytotoxic/cytostatic role in the progression and prevention of disease. This knowledge will help scientists find approaches to manipulate tumor and pathologic cells in order to enhance cellular sensitivity to therapeutics and treat them. Although some conventional therapeutics suffer from poor solubility, bioavailability and controlled release mechanisms, it appears that novel nanoplatforms overcome these obstacles and have led to the design of a theranostic-controlled drug release system with high solubility and active targeting and stimuli-responsive potentials.