In this article, we discussed the expression of some ABC (e.g., P-glycoprortein, MRP and CFTR) and SLC (e.g., POT, DAT, OAT, OATP, OCT, EAAT2/GLT1 and GLUT) amino acid, metal and nucleoside transporters in the nasal mucosa. The localization and therapeutic targeting of these transporters are explored in detail. The wide array of transporters discovered so far in the nasal mucosa implies that a plethora of compounds can be delivered by targeting these transporters. The article concludes with a discussion of the potential challenges and delivery options for transporter-mediated drug targeting via the nasal route.