<p>The global rate of mortality among women owing to breast-cancer, their socio-economic impact and toll on the family as well as the emerging chemotherapeutic resistance is alarming. Breast cancer is highly heterogeneous and a combination of various strategies like surgery with radiotherapy plus chemo-therapy, application of immunotherapy with hormone treatment; along with psychological counselling are already in practice. A large area of cancer biomedical research is set around upgradation of drug efficiency and establishment of dynamic drug delivery systems to improve tumor targetability and site-specific drug release without depleting biostability or the functionality. Camptothecin (CPT)—based antitumor drugs are known for topoisomerase I inhibitory activity and subsequent cytotoxicity as found against various types of cancers including pulmonary cancer, gastric and hepatic cancer, colorectal cancer, and breast cancer. Despite being one critical chemotherapeutic agent, low bioavailability, hydrophobicity and lack of site-specificity were some of the major concerns of CPT based anticancer treatment but in recent years, the revolutionizing research in nanotherapeutics has opened a new chapter in study of clinical chemotherapeutics. The formation of CPT based or encapsulated polymer lipid hybrid systems, nanoemulsifiers, nanorods or nanotubes; construction of nanotech oriented CPT based micellocomplexes or liposomes, synergistic tumor chemotherapy or photothermal therapy have vastly extended the scope and viability of CPT application against various breast cancer cell lines. In this review the formation and mechanism of CPT based nanotherapeutics or nanodrugs; their advance role observed against various breast-cancer cell-lines and in animal models, are critically discussed. The summarized information will serve a deep understanding in applicability and advancement of nanotechnology-dependent clinical cancer treatment focused on CPT.</p>