Over recent years advancement in nanoparticles drug delivery is widely expected to change the landscape of pharmaceutical and biotechnology industries for the foreseeable future. Nanoparticles are solid colloidal matrix-like particles made of polymers or lipids. Generally administered by the intravenous route like liposome's, they have been developed for the targeted delivery of therapeutic or imaging agents. Nanomaterials have emerged as a promising strategy in delivering therapeutic molecules effectively to diseased sites. Furthermore, most nonmaterial surfaces can be decorated with targeting ligands, enhancing their ability to home to diseased tissues through multivalent interactions with tissue-specific receptors. Thus, targeted therapy provides a means to circumvent the toxicities and lack of treatment response of conventional systemic chemotherapy. Targeted liposome's, micelles, carbon nanotubes and dendrimers incorporated with therapeutic molecules have displayed impressive anticancer effects in animal studies, and these nanomaterials are considered to be close to clinical translation due to their biocompatibility. These carriers are designed in such a way that they are independent in the environments and selective at the pharmacological site. In addition, these nanomaterials have the capability to reverse multidrug resistance a major problem in chemotherapy. Finally, tumor-homing nanosystems that amplify tumor homing can also improve the delivery of compounds to tumors, providing imaging and therapeutic options that were previously unavailable.