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 under armour 1364182 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 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 without adhesions.The in vitro release experiment showed tyrone bracken 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.