Nanotechnology has emerged strongly as a viable option to overcome the challenge of early diagnosis and effective drug delivery, for cancer treatment. Emerging research articles have expounded the advantages of using a specific type of nanomaterial-based system called as "nanocarriers," for anti-cancer therapy. The nanocarrier system is used as a transport unit for targeted drug delivery of the therapeutic drug moiety. In order for the nanocarriers to be effective for anticancer therapy, their physicochemical parameter needs to be tuned so that bio-functionalisation can be achieved to (1) allow drugs being attached to the substrate and for their controlled release, (2) ensure the stability of the nanocarrier up to the point of delivery, and (3) clearance of the nanocarrier after the delivery. It is therefore envisaged that tailoring of the physicochemical properties of nanocarriers can greatly influence their reactivity and interaction in the biological milieu, and this is becoming an important parameter for increasing the efficacy of cancer therapy. This review emphasizes the importance of physicochemical properties of nanocarriers, and how they influence its usage as chemotherapeutic drug carriers. The goal of this review is to present a correlation between the physicochemical properties of the nanocarriers and its intended action, and how their design based on these properties can enhance their cancer combating abilities while minimizing damage to the healthy tissues. © 2017 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 105A: 2906-2928, 2017.