环巴胺固体脂质纳米粒的研究

Study on cyclopamine-loaded solid lipid nanoparticles

目的制备环巴胺固体脂质纳米粒(Cyc-SLNs),并考察其理化性质和对Hedgehog信号通路的抑制作用。方法采用薄膜超声法制备Cyc-SLNs,并考察其对B16F10黑色素瘤细胞增殖、细胞周期、凋亡和Hedgehog信号通路靶基因Gli1表达的影响。结果制得的Cyc-SLNs呈平整的球形,平均粒径、多分散指数(PDI)、Zeta电位和平均包封率分别为126.5±2.1 nm、0.198±0.007、23.5±0.7 m V、91.59%±0.37%;Cyc-SLNs对B16F10细胞增殖分裂的抑制、凋亡的促进和Gli1表达的下调均强于环巴胺。结论成功制备了抗肿瘤细胞效果强于环巴胺的固体脂质纳米粒Cyc-SLNs。

OBJECTIVE To prepare cyclopamine - loaded solid lipid nanoparticles （ Cyc - SLNs） and to investigate its quality and the inhibiting effect on Hedgehog signaling pathway. METHODS The formulation of Cyc - SLNs were prepared by film ultrasonication method. The cell proliferation inhibition rate, apoptosis rate and cell cycle inhibiting effect on B16F10 cells was evaluated. RT -PCR was performed to amplify and detect Glil expression. RESULTS The obtained Cyc - SLNs were round, smooth particles with average size of 126.5±2.1 nm,PDI of 0. 198 ± 0. 007 ,Zeta potential of 23.5 ± 0.7 mv and encapsulation efficiency of 91.59% ± 0.37%. Cye - SLNs significantly inhibited the proliferation of B16F10 cells and induced apoptosis. Glil expression was down - regulated after being treated by Cyc - SLNs. CONCLUSION Cyc - SLNs were successfully prepared, and showed enhanced anti - cancer effect.