Various types of nanoparticles (NPs) have been used in delivering anticancer drugs to the site of action. This area has become more attractive in recent years due to optimal size and negligible undesirable side effects caused by the NPs. The focus of this review is to explore various types of NPs and their surface/chemical modifications as well as attachment of targeting ligands for tuning their properties in order to facilitate targeted delivery to the cancer sites in a rate-controlled manner. Heme compatibility, biodistribution, longer circulation time, hydrophilic lipophilic balance for high bioavailability, prevention of drug degradation and leakage are important in transporting drugs to the targeted cancer sites. The review discusses advantages of polymeric, magnetic, gold, and mesoporous silica NPs in delivering chemotherapeutic agents over the conventional dosage formulations along with their shortcomings/risks and possible solutions/alternatives.