The oral route remains one of the most popular and important routes of administration that warrants the development of advanced drug delivery systems such as the polymeric nanoparticles capable of enhancing the absorption and bioavailability of the used drugs. In this work, systematic reviewing through several databases followed by a meta-analysis study were utilized in order to navigate the published studies and reach literature-based evidence about the capability of polymeric nanoparticulate systems of augmenting the absorption and the bioavailability of the orally administered drugs. The pharmacokinetic parameter; area under the curve (AUC) was utilized as the “effect” of the meta-analysis study. The meta-analysis study demonstrated the significant increase AUC as compared to the conventional formulations. Furthermore, comparing the synthetic polymeric nanoparticles versus the naturally-based counterparts, as subgroups of the meta-analysis, revealed no significant differences.