AUTHOR=Xie Minghua , Wu Jia , Ji Liqaing , Jiang Xiaorui , Zhang Jin , Ge Min , Cai Xinjun 

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

JOURNAL=Frontiers in Oncology

VOLUME=9

YEAR=2019

URL=https://www.frontiersin.org/journals/oncology/articles/10.3389/fonc.2019.00978

DOI=10.3389/fonc.2019.00978

ISSN=2234-943X

ABSTRACT=<p><bold>Purpose:</bold> 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.</p><p><bold>Methods:</bold> 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.</p><p><bold>Results:</bold> 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 <italic>in vitro</italic> release experiment showed complete release of the prepared TP-SMEDDS in PBS solution in 6 h. <italic>In vivo</italic> antitumor activity showed its inhibitory effect in the xenograft model.</p><p><bold>Conclusion:</bold> The self-microemulsifying delivery system improved the oral bioavailability and the <italic>in vivo</italic> antitumor effect of TP.</p>