Several drug molecules have shown low bioavailability and pharmacokinetic profile due to
metabolism by enzymes, excretion by the renal system, or due to other physiochemical properties of
drug molecules. These problems have resulted in the loss of efficacy and the gain of side effects associated
with drug molecules. PEGylation is one of the strategies to overcome these pharmacokinetic issues
and has been successful in the clinic. Cell-penetrating Peptides (CPPs) help to deliver molecules across
biological membranes and could be used to deliver cargo selectively to the intracellular site or to the
drug target. Hence CPPs could be used to improve the efficacy and selectivity of the drug. However, due
to the peptidic nature of CPPs, they have a low pharmacokinetic profile. Using PEGylation and CPPs
together as a component of a drug delivery system, the and efficacy of drug molecules could be improved.
The other important pharmacokinetic properties such as short half-life, solubility, stability, absorption,
metabolism, and elimination could be also improved. Here in this review, we summarized PEGylated
CPPs or PEGylation based formulations for CPPs used in a drug delivery system for several
biomedical applications until August 2019.