Cell-penetrating peptides (CPPs) have emerged as a promising strategy for enhancing the membrane permeability of bioactive molecules, particularly in the treatment of central nervous system diseases. CPPs possess the ability to deliver a diverse array of bioactive molecules into cells using either covalent or non-covalent approaches, with a preference for non-covalent methods to preserve the biological activity of the transported molecules. By effectively traversing various physiological barriers, CPPs have exhibited significant potential in preclinical and clinical drug development. The discovery of CPPs represents a valuable solution to the challenge of limited membrane permeability of bioactive molecules and will continue to exert a crucial influence on the field of biomedical science.