Green chemistry, in particular, the principle of atom economy, has defined new criteria for the efficient and sustainable production of synthetic compounds. In complex nanomaterials, the number of embedded functional entities and the energy expenditure of the assembly process represent additional compound-associated parameters that can be evaluated from an economic viewpoint. In this Perspective, we extend the principle of atom economy to the study and characterization of multifunctionality in nanocarriers, which we define as "multifunctional efficiency". This concept focuses on the design of highly active nanomaterials by maximizing integrated functional building units while minimizing inactive components. Furthermore, synthetic strategies aim to minimize the number of steps and unique reagents required to make multifunctional nanocarriers. The ultimate goal is to synthesize a nanocarrier that is highly specialized but practical and simple to make. Owing to straightforward crystal engineering, metal-organic framework (MOF) nanoparticles are an excellent example to illustrate the idea behind this concept and have the potential to emerge as next-generation drug delivery systems. Here, we highlight examples showing how the combination of the properties of MOFs ( e.g., their organic-inorganic hybrid nature, high surface area, and biodegradability) and induced systematic modifications and functionalizations of the MOF's scaffold itself lead to a nanocarrier with high multifunctional efficiency.