Polymeric nanocarriers have an increasingly growing potential for clinical applications. The current and future expectation from a polymeric nanocarrier is to exhibit both diagnostic and therapeutic functions. Living organisms are very complex systems and have many challenges for a carrier system such as biocompatibility, biodistribution, side-effects, biological barriers. Therefore, a designed polymeric nanocarrier should possess multifunctional properties to overcome these obstacles towards its target site. However, currently there are few polymeric systems that can be used for both therapy and imaging in clinic studies. In the literature, there are many studies for developing new generation polymeric nanocarriers to obtain future smart and multifunctional nanomedicine. In this review, we discuss the new generation and promising polymeric nanocarriers, which exhibit active targeting, triggered release of contents, and imaging capability for in vivo studies.