A Supramolecular Nanovehicle Featuring a pH/Enzyme Co-Response for Targeted Delivery of the Antitumor Compound.

Abstract

Triptolide (TPL) has gained much attention as an antitumor compound with potential applications. However, TPL suffers from low bioavailability, severe toxic side effects, and limited targeted uptake by tumor cells, thus restricting the conversion of its clinical application. Here, a supramolecular nanovehicle, named TSCD/MCC NPs, featuring pH/AChE co-response was designed and prepared for loading, delivery, and targeted release of TPL. The cumulative release rate of TPL from TPL@TSCD/MCC NPs reached ∼90 % within 60 h at pH 5.0 and AChE co-stimulation. Bhaskar model is used to study TPL release procedure. In cell experiments, TPL@TSCD/MCC NPs showed high toxicity to the four tumor cells lines A549, HL-60, MCF-7, and SW480, and favorable biosafety to normal cells BEAS-2B. Furthermore, TPL@TSCD/MCC NPs containing relatively small amounts of TPL presented similar apoptosis rates to those of intrinsic TPL. We anticipate that TPL@TSCD/MCC NPs may facilitate the conversion of TPL into clinical applications through further studies.