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In a conventional oral or intravascular drug delivery approach, therapeutic factors are distributed throughout the body and only a limited part of the drug reaches to tumor site. Packaging of cytotoxic agents in drug delivery systems like nanoparticles could enhance its delivery to specific targets in the tumors and could be potential candidate for therapeutics advancement. Targeted drug delivery holds the potential to overcome the present therapeutics of cancer by selective delivery of an arbitrary amount of drug at the tumor site. Loading of cytotoxic agents in drug delivery systems could enhance its delivery to specific targets based on strategy to reach the tumor site. This chapter explores the detailed of innovative methods of drug delivery, challenges of targeted drug delivery, and their implications.