A method of loading extracellular vesicles (EV, MV) or exosomes with a small molecule drug comprises delivery of the small molecule drug conjugated to a cellular metabolite to an exosome source cell, allowing the metabolic uptake of the conjugate and the subsequent packaging and release of exosomes comprising the small molecules drug conjugate. Preferably the link between drug and metabolite is cleavable to release the drug. The invention further concerns the drug conjugate loaded extracellular vesicles, methods of drug delivery and pharmaceutical compositions comprising the extracellular vesicles. The loading of exosomes from PBMCs with cytosine arabinoside and with NSAID (isobutylphenylpropanoic acid) conjugated to a phospholipid or to vitamin B7 or B9 are exemplified.
