The pH‐responsive nanoparticles are a promising drug‐carrier because they always showed sensitivity and specificity to the pH changes caused by the surrounding environment. Most of the therapeutic drugs are generally absorbed in the stomach and small intestine due to the pH‐responsive nanoparticles always release the cargos at acidic media, making them difficult to reach the lower part of the large intestine, as well as inhibiting the therapeutic effects. Herein, an alkaline media‐sensitive supramolecular nanoparticle, regarded as SACD/PEI NPs, is prepared. SACD/PEI NPs exhibit assemble/disassemble state by changing the pH, which is used to encapsulate the anti‐colon drug CSL. CSL@SACD/PEI NPs showed a high release rate of 86.1% for the encapsulated CSL at pH = 8.5 (mimic the colon micro‐environment), while keeping stable at pH = 1.2 (mimic the gastric acid micro‐environment). Meanwhile, CSL@SACD/PEI NPs exhibited low hemolysis, indicating they possess good biocompatibility. In cell experiments, CSL@SACD/PEI NPs had a similar inhibitory effect on colon tumor cell SW480 and showed low cytotoxicity to normal cells compared with free CSL. Furthermore, both free CSL and CSL@SACD/PEI NPs showed excellent apoptosis effects on tumor cell SMMC‐7721. We hope that CSL@SACD/PEI NPs could be the valuable base‐answered drug delivery candidate, and have potential application for colon tumor therapy.
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.
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