Receptor-mediated uptake has been utilized for cell-specific delivery. This system takes advantage of the overexpression of a specific receptor on the surface of tumor cells for the selective uptake of anticancer cargoes. One of the most exploited receptors for this strategy is the folate receptor α. To date, many anti-cancer therapeutics have been preferentially delivered to tumor cells upon conjugation to folate. Some of the most successful examples reported in the literature are the conjugation of folate to a desacetyl vinblastine monohydrazine and to taxol derivatives. In both cases, the drug and the folate component were separated by a peptidyl spacer and a self-cleaving linker. Besides, folate conjugation was also proven to be effective in the delivery of antibodies, nanoparticles, and imaging agents. Specifically, folate conjugates were found to have enhanced selectivity towards cancer cells overexpressing folate receptor α.