Modern drug deliveryDrug delivery systems now require biopolymersBiopolymers due to their adjustable, biodegradable, and biocompatible characteristics. This chapter examines their function in different drug delivery strategies, with a focus on developments in three-dimensional (3D) and four-dimensional (4D) biopolymeric structures. In addition to a summary of the many drug kinetic modelsDrug kinetic model that control treatment efficacy, important facets of drug loading and release mechanisms are covered. Stimulus-responsive biopolymersBiopolymers that allow for targeted and regulated drug release are given particular consideration. The chapter also discusses the preclinical and clinical uses of formulas based on biopolymers, especially in gene delivery and cancer treatment. Additionally, the safety profiles of these nanoformulations are evaluated by looking at their cytotoxicCytotoxic, genotoxicGenotoxic, and apoptotic effectsApoptotic effects. The importance of biopolymer-based carriers in next-generation therapeutic approaches is emphasized by the discussion of their potential for accurate and effective drug targeting.