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Aquasomes are a novel type of self-assembling, nanoparticulate carriers that provide unique benefits for the targeted delivery of bioactive substances like proteins, peptides, hormones, antigens, and genes. These spherical particles, which measure between 60 and 300 nm in diameter, and a bioactive molecule that is adsorbed onto the surface. The formation of aquasomes is influenced by non-covalent and ionic interactions, resulting in a stable and effective structure for delivering drugs. The solid core contributes to the particle's structural integrity and stability, while the carbohydrate layer serves as a protective barrier against dehydration, thereby maintaining the activity of sensitive biomolecules. Aquasomes have demonstrated significant effectiveness in delivering therapeutic agents such as insulin, hemoglobin, and enzymes like serratiopeptidase, as well as other biologically active substances, with applications in both small- molecule and biologic drug delivery. This review examines the principles that govern aquasome, the difficulties involved in preserving the conformational integrity and biochemical activity of immobilized molecules, and how these principles converge to create an effective drug delivery system. Furthermore, the review underscores the wide-ranging applications of aquasomes across different pharmaceutical sectors, highlighting their potential as a versatile and stable platform for the targeted delivery of therapeutic agents. Future outlooks and ongoing challenges in the advancement of aquasomes for clinical applications are also explored.