The application of
saponins has been restricted by problems such as
hemolysis, low bioavailability, and poor solubility. So it is imperative to find a strategy to deliver
saponins safely and efficiently. Here, through bottom-up technique, we design and prepare two
saponin-
cholesterol (Cho) nano-complex:
dioscin (Dio,
steroid saponin)-Cho nanofibers (NFs) and
escin Ia (EIa,
triterpene saponin)-Cho nanoparticles (NPs). It is found that the hydrophobic force and hydrogen bonding drive the two pairs of molecules to bind in different directions (the 3β-
OH of Cho face the
sugar chain of EIa and the 22α-O of Dio, respectively) and finally show spherical NPs (EIa-Cho) and fibrous NFs (Dio-Cho). The equimolar
saponin-Cho complex, Dio NFs and EIa NPs, reveal potent cytotoxicities against mouse
breast cancer cells (4T1) in vitro. In vivo results confirm the antitumor (4T1 mice model) efficacy of PEGylation Dio NFs (10 mg/kg, i.v.) with a
tumor inhibition rate of 61%, meanwhile, it does not cause extreme irritation and
pain as free Dio does to mice. Moreover, compared with the free
drug, the prepared nano-complex can significantly reduce
hemolysis and organ toxicity. Our research reduces the toxicity of
saponins while retaining their antitumor activity, providing a new strategy for the delivery of
saponins.