One of the extensively studied subjects in nano-biotheranostic is developing a suitable drug delivery system with well-defined structures and functions. Polymeric micelles are an emerging therapeutic approach in drug delivery and targeting selective cells/tissues. The amphiphilic block co-polymer self-assembled in an aqueous hydrodynamic environment to develop a supramolecular structure of polymeric micelles yielding the hydrophobic core and hydrophilic shell. Simple, easy synthesis method, absence of organic solvent, ability to carry and enhance the solubility of the hydrophobic drug, and improved blood circulation make the polymeric micelles an attractive drug carrier in several disease therapies such as cancer, viral, gastrointestinal, ocular, and so on. The polymeric micelles have also gained importance as multiple target-specific, controlled drug release carriers due to their easy surface modification and specific stimuli-responsive property. This article instigates a brief introduction to polymeric micelles. Several types of polymeric micelles, depending on the material used and the intermolecular forces stabilizing the amphiphilic conformation in aqueous media, are discussed. Polymeric/copolymeric materials are used for the synthesis of polymeric micelles, and two important synthesis methods, direct and indirect dissolution and several characterization methods, are also reviewed. The targeting approach of polymeric micelles by active/passive mechanism and drug release in response to several stimuli like pH, thermal, reduction, and light response has been elaborated. This article also explores the application of polymeric micelles in the delivery of anticancer drugs, genes, immunotherapeutics, ocular drugs, and oral drugs to improve therapeutic efficacy and overcome major hindrances associated with conventional therapy. © The Editor(s) (if applicable) and The Author(s), under exclusive license to Springer Nature Singapore Pte Ltd. 2022.