Triptolide, a complex triepoxide diterpene natural product, has attracted considerable interest in the medicinal society due to its multiple biological activities. However, poor water solubility, narrow therapeutic window and multi-organ toxicity have greatly hindered its clinical application. In order to improve its clinical potential, either structural modification or the development of novel targeted delivery systems for triptolide have been executed worldwide in the past decades. In this review, we systematically summarized strategies that have been utilized to develop triptolide-targeted delivery methods, including direct conjugation of triptolide to selected ligands such as sugar, short peptide, oligonucleotide, antibody and most importantly encapsulation of triptolide with well-designed nanovehicle. Thanks to the potent multiple biological activities of triptolide, either direct conjugation of triptolide to selected ligands or encapsulation of triptolide with nanocarriers could provide better anti-inflammatory or anticancer activity. Thus, these targeted delivery strategies could be taken as a starting point for future utilization of triptolide and also other NPs in experimental clinical therapy. (C) 2018 Elsevier Masson SAS. All rights reserved.