In the past years, alternative pharmaceutical formulations of anti-cancer agents have been investigated in order to improve conventional chemotherapy treatment. In conventional/current therapy oral tablet, capsule and injectable formulations are used for anti-cancer drugs delivery. These formulations associated with problems like severe toxic side effects on healthy organs, difficulties in clinical administration, drug resistance and limited access of the drug to the tumor sites suggested the need to focus on site specific controlled drug delivery systems. Novel drug delivery systems are capable of controlling the rate of drug delivery, sustaining the duration of therapeutic activity and targeting the drug to the disease tissue leading to better therapeutic effect with minimum side effects. In this review, we have explored the literature related to recent development in delivery of anti-cancer drugs identify problems in present conventional chemotherapy and detailed newer approaches and future development in the delivery of anti-cancer drugs.