Abstract: According to an exemplary embodiment of the present invention, a versatile delivery module based on a myristoylated polyarginine backbone can be provided to cross a blood-brain barrier (“BBB”). An incorporation of a fatty acid group can be achieved using a Schotten-Bauman reaction with quantitative yield, and a peptide can be further synthesized by conventional solid phase peptide synthesis (“SPPS”). An in vivo distribution of the delivery module into a brain over time using near-infrared (“NIR”) fluorescence imaging can be obtained. A fluorescent cargo can be detected in vivo after an intravenous injection and can be further characterized in perfused brains. A staining of an excised brain can show that the delivery module can primarily accumulate in neurons with occasional localization in astrocytes and endothelial cells. This exemplary approach can be used for the delivery of imaging probes and targeted therapeutics across the BBB.