With advancing science and technology, new futuristic technologies have been upcoming that are having a greater impact on the pharmaceutical and biomedical fields. Many lipids and polymer of natural and synthetic origin have spread horizons enabling to reach in fabricating delivery systems for unmet medical needs. In this modern biomedicine era, we must outline and scrutiny the roles of these biomaterials and the modern technologies that are shaping up the advancing medicines. The real challenges in modulating, fine-tuning the biomaterials for their bioactive properties are vital for assessing the in-vivo performance of the developed systems. Therefore, the present review discusses the detailed analysis of the current research reported in the technologies of utilizing the lipids, polymers, and their role in delivering the drugs, genes, and designing advanced implantable medical devices. The scrutiny also focuses on key optimization tools, analytical methods, formulation, and biomedical techniques helpful in developing the solutions that can be administered different routes in different therapeutic indications.