Remarkable advances have been achieved in modern material technology, especially in device fabrication, and these have facilitated the use of diverse materials in various applications. Carbon nanotubes (CNTs) are being successfully implemented in drug delivery, sensing, water purification, composite materials, and bone scaffolds. Thus, CNTs must meet a wide range of criteria such as surface modification, high aspect ratio, desired conductivity, high porosity and loading, non-toxicity, specificity, and selectivity, and compatibility for device fabrication. The main focus of this review is to explore the maximum applications of CNTs for human health, and we particularly focus on nanocarrier and biomedical applications. The scope of this review initially covers the basic aspects of CNTs and is also extended further to describe their synthesis strategies as well as various challenges encountered in their functionalization, dispersion, and toxicity. Our discussion also emphasizes future directions for these emerging fields of research.