Nanotechnology has a potential impact in the detection, treatment, and monitoring of cancer significantly, and to revolutionize cancer nanomedicine. Nanoparticles are particles with dimensions in the 1-100 nm range, the scale at which scale materials have unique physicochemical properties including ultrasmall size, large surface-to-mass ratio, high reactivity, and unique interactions with biological systems. Advanced nanoparticulate designs as “magic bullets” postulated by Paul Ehrlich, the Founder of chemotherapy, are now under in-lab development, including with combined capabilities for targeting, imaging, and delivering multiple drugs with enhanced therapeutic index and treatment efficacy to revolutionize the current cancer therapies in the coming years. Specifically, prostate cancer develops in the prostate, a gland in the male reproductive system. As the disease progresses and becomes more aggressive, the cancerous lesions spread beyond the prostate locally to the rectum or bladder, then eventually to the bones, lymph nodes, lungs, and liver. Enhancing therapeutic efficacy is essential for successful treatment of chemoresistant cancers such as metastatic hormone-refractory prostate cancer. Current chemotherapy regimens are plagued with issues such as toxicity, low bioavailability, and lack of specificity. To combat these issues, the feasibility of using nano/microparticles to enhance the therapeutic efficacy of chemotherapeutic drug have been widely explored in these days. This chapter aims to overview nanodiamonds (NDs) for therapeutic delivery systems for delivering the cancer drugs of interest, bioimaging for the detection of cancer and targeted drugs by multifunctionalized nanocarriers. NDs are attractive for this application because of their small size, 5-50 nm, which enables them to have enhanced circulation time in the body and the relative ease of modifying their surface with a range of functional molecules. The enhancement of chemotherapy using nanodiamond particles (NDPs) is attributed to three factors viz. drug mediation/combination therapy, targeted drug delivery, and bioimaging. Fluorescent-based detection and binding kinetics in a unique biosensing platform consisting of precision-patterned subpicoliter molecularly imprinted polymer (MIP) elements with ND fluorescence from nitrogen or silicon-vacancy centers.