Provided are a poorly water-soluble drug delivery system, a method of preparing the same, a method of delivering a poorly water-soluble drug using the same, and a pharmaceutical composition including the same as an effective component, and more particularly, a poorly water-soluble drug delivery system aiming cancer cell specific targeting, which may variously control the kind of a cancer cell targeting material capable of specifically reacting to an antigen overexpressed in a cancer cell, thereby binding to the surface of the poorly water-soluble drug delivery system, and variously control the kind of a poorly water-soluble drug encapsulated therein depending on the kind of cancer and a therapeutic purpose, thereby being effectively applicable to a cancer treatment method.