**Abstract**

Blood-brain barrier (BBB), a unique membrane barrier formed by closely stitched brain capillary endothelial cells (BCEC) with tight cellular junctions, separates brain from the circulating blood to protect it from bloodborne pathogens. BBB greatly limits the entry of chemotherapeutics to brain, and in consequence, it is a major obstacle for treating brain tumor. Advances in designing efficient nanodrug carriers are opening new avenues for overcoming this uphill systemic challenge. This book chapter describes current understanding of nanocarriers-mediated noninvasive drug targeting to brain tumor. Design principles behind the construction of the most promising recently designed receptor and transporter selective nano-drug carriers for combating brain tumors have been highlighted.

**Keywords:** blood-brain barrier, brain tumor, nanocarrier, drug delivery, nanomedicine
