This review highlights recent advancements in combining metal–organic frameworks (MOFs) with carbohydrate chemistry to create biocompatible systems for biomedical applications. MOFs offer unique properties like biodegradability, low toxicity, and high surface area, enabling functionalization with biological ligands and the loading of active cargos, from small drugs to biomacromolecules. Recent research focuses on leveraging carbohydrate chemistry to functionalize and modify MOF structures, aiming for efficient and naturally inspired designs. The review discusses the field’s progress over the past five years, addressing both its potential and challenges, including sustainability and real-world applicability.