Microwave (MW) irradiation technology has significant benefits in various fields, namely, materials synthesis, food processing, and therapeutics. Until now, MW-assisted reactions have gathered considerable attention in synthesising drug delivery carriers. Dipolar polarisation and conduction are the fundamental mechanisms of MW irradiation. Recognising the benefits of the advantages of MW-assisted reactions, such as high yield and accelerated reaction with high purity, MW-assisted technology has the potential for synthesising drug delivery nanocarriers with improved physicochemical properties and bioavailability. This chapter will discuss the synthesis of advanced drug delivery systems, which encompasses carbon quantum dots, polylactic acid, poly(lactic-co-glycolic acid), metal-organic frameworks, and mesoporous silica nanoparticles. Additionally, this chapter provides challenges and opportunities concerning the scaling up of the synthesis of nanocarriers used in drug delivery processes, regulatory issues, and environmental toxicity. Despite the limitations, MW irradiation is an innovative approach for the formulation of novel nanocarriers. It thus opens new avenues for developing drug delivery systems in various biomedical applications.