Alginate is being explored widely for an array of medicinal and diagnostic measures by way of nanosystems fabricated for techniques along the lines of drug delivery, imaging, tissue regeneration, etc. Their biocompatibility, nontoxicity, sensitivity to pH, mucoadhesiveness, and biodegradability have invited an extensive body of work in this field. Their gelling ability facilitates the encapsulation of different molecules like drugs, proteins, and genes, through the formation of multidimensional matrices. Furthermore, the feasibility of alginates for physical and chemical modification allows appropriate synthesis of nanosystems for their application. The current review highlights delivery of therapeutic compounds via alginate nanosystems as an effective, eco-friendly alternative for expediting controlled and target-specific release.