The nanocrystal-loaded liposome of tanshinone IIA with high drug loading and stability towards efficient liver fibrosis reversion.

Tanshinone IIA (TSIIA) is a lipid-soluble pharmacological constituent extracted from the Salvia miltiorrhiza with anti-hepatic fibrosis properties. However, its clinical use has been limited due to its poor water solubility and oral bioavailability. In this paper, we constructed a drug delivery system consisting of a drug nanocrystal core and a liposome shell: TSIIA nanocrystals@liposome (TNC@Lipo). This combination can greatly improve the solubility and bioavailability of poorly water-soluble drugs. TNC@Lipo was prepared by ultrasonic method combined with antisolvent method. In order to obtain the optimal TNC, we optimized the formulation ratio and preparation process of TNC by single-factor experiments. The results showed that TNC@Lipo had higher drug loading (27.86 ± 1.55 %) and superior stability. And TNC@Lipo can significantly reversed CCl4-induced liver fibrosis in mice compared with free-TSIIA. In conclusion, this study provides a new approach for the clinical application of TSIIA.