Chemotherapy remains the most commonly used approach in cancer treatment despite the severe side effects caused by harsh drugs. Bio-drugs, on the other hand, offer enhanced selectivity and efficacy, and hence considered as a promising alternative for chemotherapy in a number of cancer types. However, a major drawback of bio-drugs is that they often suffer from poor bioavailability and compromised PK/PD properties due to relatively large molecular weight. In designing the next generation cancer treatment, extensive effort has been made to find novel therapeutic agents as well as delivery tools. One way to circumvent the limitations associated with chemotherapy is to combine a functional vesicle with the drug for targeted delivery and controlled release. A good example is liposome – the most common type of lipid nanoparticle that is biodegradable, biocompatible, and offers a useful tool of drug delivery, particularly for the highly toxic drugs. Nowadays, an increasing number of liposomes are extensively used for drug delivery to cancer cells. The next generation of drug delivery liposome will focus more on tumor recognition, including true molecular targeting, immunoliposomes.