Cyclic anhydrides are potent tools for bioconjugation, therefore they are broadly used in the functionalization of biomolecules and carriers. The pH-dependent stability and reactivity, as well as the physical properties, can be tuned by the structure of the cyclic anhydride used, thus their application in smart delivery systems has become very important. This review intends to cover the last updates in the use of cyclic anhydrides as pH-sensitive linkers, their differences in reactivity and the latest applications found in bioconjugation chemistry, or chemical biology and when possible, in drug delivery.