Despite the fact that protein and peptide therapeutics are widely employed in the treatment of various
diseases, their delivery is posing an unembellished challenge to the scientists. It was discovered that delivery of
these therapeutic systems through oral route is easy with high patient compliance. However, proteolytic degradation
and absorption through the mucosal epithelium are the barriers in this route. These issues can be minimized
by the use of enzyme inhibitors, absorption enhancers, different carrier systems or either by direct modification.
In the process of investigation, it was found that transdermal route is not posing any challenges of enzymatic
degradation, but, still absorption is the limitation as the outer layer of skin acts as a barrier. To suppress the effect
of the barrier and increase the rate of the absorption, various advanced technologies were developed, namely,
microneedle technology, iontophoresis, electroporation, sonophoresis and biochemical enhancement. Indeed,
even these molecules are targeted to the cells with the use of cell-penetrating peptides. In this review, delivery of
the peptide and protein therapeutics using oral, transdermal and other routes is discussed in detail.