The existence of blood-brain barrier (BBB) represents the most formidable challenge for drug delivery to the
central nervous system (CNS). Modern breakthrough in biology offers multiple choices for overcoming this barrier but
yields modest outcomes for clinical application due to various problems such as safety concerns, insufficient delivery efficiency
and poor penetration. Cell penetrating peptides (CPPs) possessing powerful transmembrane capacity have been
shown to be effective transport vectors for bioactive molecules and an attractive alternative to traditional active targeting
approaches. However, the non-specificity of CPPs has hindered them from targeting a desired site of action. Promisingly,
design of novel CPP-mediated nanoparticulate delivery systems with specific targeting property may extricate CPPs from
the dilemma. In this review, both the traditional and novel applications of CPPs-based strategies for CNS drug delivery
will be discussed.
Keywords: Blood-brain barrier, cell penetrating peptides, central nervous system, drug delivery.
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