Cancer, a complex series of diseased conditions, contributes to a significant
health problem and is a leading cause of mortalities across the world. Lately, with the advent
of improved diagnostics and imaging techniques, and newer advanced oral chemotherapeutics;
millions of cancer affected people can lengthen their life span. Despite all
the challenges associated with an active chemotherapeutic molecule like microenvironment
and the intestinal barrier of the gastrointestinal tract (GIT) etc., the oral delivery remains
the most acceptable route of drug administration. In this regard, nanotechnology
has played a significant role in the counteracting the challenges encountered with newly
developed molecules and aiding in improving their bioavailability and targetability to the
tumour site, while administering through the oral route. Several literature instances document
the usage of nanostructured drug delivery systems such as lipid-based, polymerbased
or metallic nanomaterials to improve the efficacy of chemotherapy. Besides, sitespecific
targeted surface-modified drug delivery system designed to deliver the active
molecule has opened up to the newer avenues of nanotechnology. However, the issue of
potential toxicity allied with nanotechnology cannot be compromised and thus, needs
specific ethical regulations and guidelines. The various in vitro models have been developed
to evaluate the in vitro toxicity profile which can be further correlated with the invivo
model. Thus, this review provides a summarized account of the various aspects related
to the role of nanotechnology in cancer therapy and various related issues thereof;
that must be triumphed over to apprehend its full promise.