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Nanobiotechnology plays a more and more important role in combating cancer. Ideal delivery should maximize drug accumulation at tumors while minimize the unwanted drug exposure to the normal tissues, thus executing cytotoxicity specifically in cancer cells and sparing the healthy cells. Nanotechnology-based targeting delivery has been generally believed as the most promising method to achieve this ultimate goal of pharmacotherapy. Nano drug delivery systems can improve the pharmacokinetics profiles and tumor biodistribution of the antitumor drugs, and enhance their intracellular delivery as well; in addition, the drug instability and water insolubility problems can be solved by encapsulation into nano carriers.