Simple Summary Crossing biological barriers is often required for drug delivery. Cell-
penetrating peptides (CPPs) are short strands of amino acids that have been widely used as
a delivery vehicle to overcome barriers for various applications. This review aims to
emphasize the role of CPPs as permeation enhancers for targeted drug delivery
applications. We also discuss the prospect of clinical translation of CPP-functionalized drug
delivery systems in oncology. This may help facilitate the development of new types of CPPs …

Cell-Penetrating Peptides (CPPs) are short peptides consisting of< 30 amino acids. Their
ability to translocate through the cell membrane while carrying large cargo biomolecules has
been the topic of pre-clinical and clinical trials. The ability to deliver cargo complexes
through membranes yields potential for therapeutics and diagnostics for diseases such as
cancer. Upon cellular entry, some CPPs have the ability to target specific organelles. CPP-
based intracellular targeting strategies hold tremendous potential as they can improve …