The side effects and low bioavailability of paclitaxel (PTX) limit its clinical application. The formation of self-assembled nanomedicines without structural modification is attractive for biomedical applications. Here, we constructed a supramolecular co-assembled nanoparticles (NPs), which is formed by betulonic acid (BTA) and PTX mainly through hydrogen bond interaction and hydrophobic interaction. It not only has the characteristics of NPs but also the activity of natural small molecules (NSMs). The results of in vitro and in vivo experiments showed that BTA-PTX NPs showed excellent synergistic enhancement of anti-tumor efficacy, because BTA and PTX have different anti-tumor mechanisms. What's more, BTA-PTX NPs showed excellent biosafety and low toxicity, because BTA has impressive biological activity and biosafety. This work provides an effective and simple method to construct high efficiency and minimize side effects of NPs, which provides more possibilities for the application of NSMs in drug delivery.
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