Biopolymer nanoparticles are molecules of interest in the direction of generation of new pre-diagnostic and treatment strategies with improved efficacy and specificity. Several methods have been developed to produce biopolymer nanoparticles. These biopolymer nanoparticles had distinct properties such as size and charge according to the production method affecting their targeting and drug encapsulation abilities. The present review highlighted the progress in the development of theronostic nanoparticles. The surface of the nanoparticles may be subjected to modification and be hidden from the immune system, so that they can stay in blood circulation for a long time to achieve their intended outcome. The safety and efficacy of most of the generated nanoparticles systems were not tested in humans in details. The synthesizable nanoparticles that are generated using biodegradable and/or biocompatible building blocks have been easy to be considered as important candidates for the usage in treatment and diagnostic evaluation plan. In-depth understanding and research must be achieved for better understanding of the mechanism of theranostic nanoparticles metabolism and their excretion out of the human body. An attempt to summarize the recent research studies in the field of therapeutics and diagnostics based on the biopolymers was achieved in this review article.