Science has been trying to deal with complex diseases, like cancer, for a long time. Indeed, the side effects of the conventional treatment methods are tremendous, in some cases irreversible. This kind of problems demands a solution. Therefore, novel drug delivery systems are devised to mitigate the negative impacts of conventional ones. Polymeric nanocarrier systems are of great importance in this newly opened field. Polymers having been vastly investigated are common in some properties, such as their being biocompatibility and biodegradability. Generally speaking, a set of properties is required to achieve optimum delivery of drugs to target organs with minimum side effects. To do so, some measures should be taken. First of all, the strategy for release should be determined, categorized into two main branches, active and passive. Next, the drug release method should be engineered. Generally, there are two main categories for drug release, exogenous and endogenous. In this review, some of the chief subcategories of any aforementioned items are discussed. In the end, we catch up on already engineered nanocarriers' administration to the human body, possible toxic effects, if any, and the routes for affecting as a toxin.