The passage of therapeutic molecules across the Blood-Brain Barrier (BBB) is a profound
challenge for the management of the Central Nervous System (CNS)-related diseases. The ineffectual
nature of traditional treatments for CNS disorders led to the abundant endeavor of researchers for the
design the effective approaches in order to bypass BBB during recent decades. Cell-Penetrating Peptides
(CPPs) were found to be one of the promising strategies to manage CNS disorders. CPPs are short peptide
sequences with translocation capacity across the biomembrane. With special regard to their two key
advantages like superior permeability as well as low cytotoxicity, these peptide sequences represent an
appropriate solution to promote therapeutic/theranostic delivery into the CNS. This scenario highlights
CPPs with specific emphasis on their applicability as a novel theranostic delivery system into the brain.
Keywords: Cell-penetrating peptide, blood-brain barrier, theranostics, central nervous system, drug delivery, translocation.
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