Paclitaxel (taxol, 1a) and docetaxel (taxotere, 1b) have established themselves as an important class of antitumor drugs currently available to the oncologist. While the great contribution of these drugs to the management of the disease and their effect on the improvement of the patient quality of life could not be overemphasized, a great deal of research has been ongoing to improve two key pharmacologic factors, antitumor activity and systemic toxicity. Both physical and chemical means have been employed towards the enhancement of antitumor activity and at the same time, lowering the inherent toxicity and side effects of these drugs. This mini-review compiles the recent reported works on the design and development of taxane delivery systems through tumor cell surface receptor-targeted delivery mechanisms such as small-molecule peptides and monoclonal antibodies, as well as those on non-targeted procedures such as liposomes, nanostructures, and natural and synthetic polymers.