目的 制備和厚樸酚脂質(zhì)體（HK-Lipsomes），探討其對小鼠乳腺癌細(xì)胞（4T1細(xì)胞）的體內(nèi)外生長抑制作用。方法 將蛋黃卵磷脂、膽固醇、mPEG2000-DSPE2000、和厚樸酚按照質(zhì)量比3：1：1：1，以注入法制備成和厚樸酚脂質(zhì)體。通過Zetasizer nano ZS測定和厚樸酚脂質(zhì)體的粒徑，透射電鏡觀察和厚樸酚脂質(zhì)體的形態(tài)。用噻唑藍(lán)（MTT）比色法評價(jià)和厚樸酚脂質(zhì)體對4T1細(xì)胞的細(xì)胞毒性。建立小鼠4T1乳腺癌腫瘤模型，以紫杉醇注射液為陽性對照，考察腹腔給藥后和厚樸酚脂質(zhì)體對腫瘤的抑制作用。結(jié)果 制備得到的和厚樸酚脂質(zhì)體的平均粒徑為（113.8±0.2）nm，多分散指數(shù)（0.209±0.005），電位為（-30.7±2.4）mV，透射電鏡觀察和厚樸酚脂質(zhì)體為球型。和厚樸酚溶液和脂質(zhì)體對4T1細(xì)胞的IC₅₀值分別為（43.74±2.38）μg/mL和（12.52±2.24）μg/mL。和厚樸酚脂質(zhì)體高（60 mg/kg）、中（40 mg/kg）、低（20 mg/kg）劑量組的抑瘤率分別為85.19%、60.95%和37.83%，呈劑量相關(guān)性。結(jié)論 實(shí)驗(yàn)使用較為簡便的制備方法成功制備粒徑較小、包封率高的和厚樸酚脂質(zhì)體。荷瘤小鼠體內(nèi)實(shí)驗(yàn)顯示抑瘤效果良好。

Objective To prepare honokiol liposomes (HK Liposomes) and explore their inhibition of breast cancer cells (4T1) in vitro and in vivo. Method The HK Liposomes were prepared by ethanol injection method using egg yolk lecithin, cholesterol, mPEG2000-DSPE2000 and honokiol (3:1:1:1, weight ratio) in formulation. The size of HK liposomes was determined by Zetasizer nano ZS. The morphology of HK Liposomes was observed by transmission electron microscope. MTT assay was used to evaluate the cytotoxic activity of HK liposomes against 4T1 murine breast cancer cell line with free HK as a control. The in vivo antitumor effect of the resultant HK Liposomes (ip administration) was evaluated on 4T1-bearing mice at different dose using PTX injection as a positive control. Results The HK liposomes were (113.8±0.209) nm in average particle size with smooth surface and spherical shape. The polydispersity index (PDI) value was (0.209±0.005) and zeta potential was (-30.7±2.4) mV. Honokiol liposomes showed significant higher cytotoxicity than free HK against 4T1 cells (IC₅₀ value 12.52 μg/mL vs 43.74 μg/mL, P<0.01). On 4T1 tumor-bearing mice models, HK liposomes demonstrated a dose-dependent tumor suppression effect with inhibitory rate being 37.83%, 60.95% and 85.19% respectively for low (20 mg/kg), middle (40 mg/kg), and high dose (60 mg/kg). Conclusion In contrast, HK liposomes were successfully prepared with high encapsulation efficiency (94%), small particle size (113.8 nm) and demonstrated enhanced in vitro and in vivo anti-tumor efficacy in comparison with free HK.