The research in this book is focused on the application of the concept of polymer-drug conjugation to prepare conjugates. These conjugates acts as pro-drugs from which bioactive agents are released to predestined biological environment. The macromolecular carriers used are biodegradable, non-toxic, easily conveyed to the target cells or tissues, with different solubilizing groups to ensure rapid dissipation of the conjugate in the central circulation system. The polymer-drug connective link is to provide delayed and controlled drug release thereby ensuring restriction of drug serum concentration and reduction of organ toxicity. This book elaborates on the conjugation of 4- and 8-aminoquinolines to polymers to overcome the drug resistance associated with the currently used aminoquinolines. Presently, some antimalarial drugs have been found to be anti-carcinogenic and have ability to inhibit tumor development and as such, this book is also focused on the co-conjugation of an anticancer and an antimalarial agent on a single carrier, whereby the antimalarial is expected to serve as potentiating and resistance reducing agent.