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

Abstract

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.