The remarkable multimodal functionalities of magnetic nanoparticles, conferred by their size and morphology, are very important in resolving challenges slowing the progression of nanobiotechnology. The rapid and revolutionary expansion of magnetic nanoparticles in nanobiotechnology, especially in nanomedicine and therapeutics, demands an overview of the current state of the art for synthesizing and characterizing magnetic nanoparticles. In this review, we explain the synthesis routes for tailoring the size, morphology, composition, and magnetic properties of the magnetic nanoparticles. The pros and cons of the most popularly used characterization techniques for determining the aforementioned parameters, with particular focus on nanomedicine and biosensing applications, are discussed. Moreover, we provide numerous biomedical applications and highlight their challenges and requirements that must be met using the magnetic nanoparticles to achieve the most effective outcomes. Finally, we conclude this review by providing an insight towards resolving the persisting challenges and the future directions. This review should be an excellent source of information for beginners in this field who are looking for a groundbreaking start but they have been overwhelmed by the volume of literature.