The limitations of traditional drug delivery vehicles include low specificity, uncontrolled biodegradation, and are oftentimes associated with toxicity and serious off-target events. In addressing the biological relevance of an effective drug delivery system in improving the therapeutic efficacy of active ingredients, a variety of new approaches for drug administration have recently been developed. Remarkable breakthroughs following the emergence of nanotechnologies promoted metal-organic frameworks (MOFs) as viable drug delivery possibilities. They are characterised by large surface area and porosities, and hence, exceptional drug adsorption ability. Inorganic MOFs in particular offer high drug loadings and functionalisation capacity, enabling a high-efficacy drug administration route and controlled pattern of drugs’ in vivo behaviours. This research encompasses the preparation of MOFs and their relevant drug delivery for different diseases treatment in biomedical field, which are classified according to four types of diseases including cancer, Alzheimer’s disease, pulmonary diseases, and ocular diseases. A diverse of different MOFs have been designed to treat given their corresponding properties for these diseases. Experimental outcomes from each research are also analysed to evaluate the therapeutic effectiveness and biological applicability of proposed MOFs, which is expected to provide a new idea for efficient drug delivery in disease treatment.