Carbon nanotubes (CNTs) have been identified as one of the most advanced and versatile nanovectors, theranostics, and futuristic drug delivery tools for highly effective delivery of genes, drugs, and biomolecules, as well as for use in bioimaging and as biosensors. CNTs have drawn tremendous attention and interest from researchers worldwide in the past two decades owing to a number of unique characteristics including well defined physicochemical properties, large surface area, in addition to exclusive electrical and optical properties. Numerous recent literature related to the design and applications of CNTs were studied and summarized accordingly. Special emphasis was given for the applications of CNTs in drug targeting. Specific targeting of anticancer drugs such as cisplatin, doxorubicin, taxol, gemcitabine, and methotrexate, and delivery of small interfering RNA, micro-RNA, as well as plasmid DNA have been successfully assisted using CNTs. All the major applications of CNTs were summarized in detail with possible toxicity concerns associated with them. As far as their toxicity is concerned, it was noticed that the functionalized CNTs pose little toxicity and do not have immunogenic effects. In conclusion, CNTs showed great potential in developing a new generation of carriers for various drugs and related biomolecules. The application of CNTs ranges from physics to chemistry and now they are expanding their roles in the therapeutic drug delivery in the modern healthcare system. With applications in every imaginable route of administration, CNTs bring therapeutic benefits to society. The pharmaceutical, biopharmaceutical, pharmacokinetic, pharmacodynamic, and clinical efficacy of CNTs is explored in detail in this review.
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