蓝萼甲素纳米脂质体的制备、表征及对三阴性乳腺癌细胞的抑制作用

Preparation and characteristics of glaucocalyxin A-loaded nanoliposomes and its inhibition of triple negative breast cancer( TNBC)

目的:制备工艺稳定的蓝萼甲素纳米脂质体并考察其对细胞的抑制作用。方法:采用薄膜分散法制备蓝萼甲素纳米脂质体、马尔文粒径仪及透射电镜对其性质进行表征、超滤离心-高效液相色谱法进行包封率及载药量的测定,并考察蓝萼甲素纳米脂质体的体外释放行为;采用cck-8法考察蓝萼甲素纳米脂质体对sum149PT细胞系及sum149PT微球体的抑制作用,通过流式细胞仪确定sum149PT细胞的凋亡时期及凋亡比例。结果:优选处方及工艺制备的蓝萼甲素纳米脂质体粒径为(83.97±0.059)nm,Zeta电位为(-12.93±0.694)m V,包封率为(79.19±1.733)%,载药量为(3.43±0.250)%,且蓝萼甲素纳米脂质体具有较明显的缓释效果,并且对sum149PT细胞系及sum149PT微球体具有较好的抑制作用。结论:优选处方制得的蓝萼甲素纳米脂质体处方可行,制备工艺稳定,具有一定的抗三阴性乳腺癌效果。

Objective： To prepare glaucocalyxin A（ GLA）-loaded nanoliposomes（ GLA-LNs） with stable preparing technology and investigate its inhibitory effect on cells. Methods： The GLA-LNs was prepared with film dispersion method; the particle size,pd I,Zeta potential,and morphology were characterized by Malvern particle size analyzer and transmission electron microscope（ TEM）; the entrapment efficiency（ EE） and drug loading（ DL） of GLA-LNs were determined by HPLC method,and the release profile was studied; the cell cytotoxicity was measured with Kit CCK-8 method on sum149 PT cell line and sum149PT-TS; flow cytometry was used to determine the apoptosis effect on sum149 PT cell lines. Results： The particle size and the zeta potential of GLA-LNs were（ 83. 97 ± 0. 059）nm and（-12. 93 ± 0. 694） m V; the results of morphology observation showed that GLA-LNs were round in shape and had uniform size; the EE and DL were（ 79. 19 ± 1. 733） % and（ 3. 43 ± 0. 250） %,respectively; GLA-LNs hadbetter sustained release effect and they were more stable; GLA-LNs showed better inhibitory effect on sum149 PT cell line and sum149PT-TS,and the apoptosis effect of GLA-LNs was better than GLA. Conclusion： The formulation and preparing process of GLA liposomes established in this study are feasible and reasonable; GLA-LNs have a better effect on triple negative breast cancer in vitro.