Polymeric nanoparticles, micelles, niosomes, hydrogels and liposomes represent effective drug carriers having huge potential for medical and pharmaceutical applications. These systems remain the most important area in medicinal chemistry research. The aforementioned biomaterials can effectively encapsulate and release diverse hydrophobic/hydrophilic therapeutic molecules including drugs and prodrugs. Applications of these carrier systems extend to nucleic acids, antibodies and proteins which could be released sustainably. Since these systems fall in the nano dimension, they are capable of enhancing the therapeutic efficacy of bioactive molecules besides enabling them to accumulate preferentially at the target site. Furthermore, these systems can protect the encapsulated drug from degradation, thereby increasing the therapeutic value of the drug candidate and reducing systemic toxicity. In this review, we illustrate the preparative methods and actions of these five drug delivery systems.