Development of Triptolide Self-Microemulsifying Drug Delivery System and Its Anti-tumor Effect on Gastric Cancer Xenografts

Development of Triptolide Self-Microemulsifying Drug Delivery System and Its Anti-tumor Effect on Gastric Cancer Xenografts

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Purpose: To develop a triptolide (TP) self-microemulsifying drug delivery system and to investigate its anti-tumor effect on human gastric cancer line MGC80-3 xenografts in nude mice.Methods: The medium chain triglyceride (MCT) was selected as oil phase; polyoxyethylene castor oil (EL) was selected as surfactant, and PEG-400 was selected as cosurfactant.The mass ratio of each corky lala phase was optimized by central composite design and response surface methodology to prepare TP-SMEDDS (self-microemulsifying drug delivery system).

The quality of TP-SMEDDS was evaluated, and its inhibitory effect on tumor growth investigated in nude mice transplanted with MGC80-3 cells.Results: The final prescription process was defined as follows: MCT mass ratio: 25.3%; EL mass ratio: 49.

6%; PEG-400 mass ratio: 25.1%.The prepared TP-SMEDDS was a transparent liquid with a clear appearance (the theoretical particle size: 31.

168 nm).On transmission electron microscopy, the microemulsion particles were spherical in size and uniformly distributed ranchy doodle without adhesions.The in vitro release experiment showed complete release of the prepared TP-SMEDDS in PBS solution in 6 h.

In vivo antitumor activity showed its inhibitory effect in the xenograft model.Conclusion: The self-microemulsifying delivery system improved the oral bioavailability and the in vivo antitumor effect of TP.