Preparation of Triptolide Nano Drug Delivery System and Its Antitumor Activity In- Vitro

Triptolide (as an effective antitumor drug) is limited in clinical application because of its poor solubility and absorption in-vivo. Herein, we prepared folic acid modified polymer micelles to encapsulate triptolide and enhance its biologicalavailability coupled with antitumor effect. We prepared nano-micelles of triptolide through thin lipid film hydrational method. Physical properties and in vitro release characterization of Fol-Plla-cl-Peg-Plla-cl-Tmicelles were evaluated, while bioavailability of the formulation in rats was investigated. Tumor targeting potential of micelles was determined by observing the uptake of A549 cells. In-vitro antitumor activity of micelles and free triptolide (API) was investigated with MTT assay. The prepared polymer material exhibited no cytotoxicity. The particle size distribution of Fol-Plla-cl-Peg-Plla- cl-T micelles was uniform and small, with good stability and high efficiency of entrapment. Triptolide in-vitro release from micelles demonstrated slow and continuous released for 24 h. Compared with API, the half-life of micelles was prolonged, whilst its bioavailability in-vivo was increased by about 6.35 times. More importantly, Fol-Plla-cl-Peg-Plla-cl-T micelles significantly improved the antitumor activity of triptolide and showed good tumor targeting potential. Fol-Plla-cl-Peg-Plla-cl-T micelles could improve the bioavailability and antitumor activity of triptolide, amid demonstration of good tumor targeting and high safety.

Automated summary

In this study, folic acid modified polymer micelles were prepared to encapsulate triptolide and enhance its bioavailability and antitumor activity. The micelles exhibited good in vitro release properties, stability, and tumor targeting potential. Compared with free triptolide, the micelles showed prolonged half-life and increased bioavailability in vivo. Moreover, the micelles significantly improved the antitumor activity of triptolide and demonstrated high safety.