Targeted drug delivery systems gave newer dimensions for safer and more effective use
of therapeutic drugs, thus helping in circumventing the issues of toxicity and unintended drug accumulation.
These ongoing developments in delivery systems can, in turn, bring back drugs that suffered
various limitations, Ellipticine (EPT) being a candidate. EPT derivatives witnessed entry into
clinical settings but failed to survive in clinics citing various toxic side effects. A large body of preclinical
data deliberates the potency of drug delivery systems in increasing the efficiency of
EPT/derivatives while decreasing their toxic side effects. Recent developments in drug delivery systems
provide a platform to explore EPT and its derivatives as good clinical candidates in treating
tumors. The present review deals with delivery mechanisms of EPT/EPT derivatives as antitumor
drugs, in vitro and in vivo, and evaluates the suitability of EPT-carriers in clinical settings.