目的 研究一种高载药量和厚朴酚纳米粒, 评价其对小鼠肝癌H22移植瘤的生长抑制作用。方法 用牛血清白蛋白(BSA)和聚乙烯吡咯烷酮(PVP)为辅料, 采用超声-沉淀法制备和厚朴酚纳米粒。建立H22肝癌皮下小鼠肿瘤模型, 以环磷酰胺注射液(CTX)为阳性对照, 考查ip给药后其对肿瘤的抑制作用。结果 和厚朴酚纳米粒呈球形, 平均粒径为(116.5±1.3)nm, 多分散指数(PDI)为0.116±0.001, 体外溶出较原料药大幅度提升。在H22荷瘤小鼠体内, 和厚朴酚纳米粒显示出剂量相关的抑瘤作用, 低、中、高剂量(10、20、40 mg/kg)组抑瘤率分别为52.57%、66.33%和71.24%。结论 和厚朴酚纳米粒对肿瘤有明显的抑制作用。

Objective To prepare honokiol nanoparticles (HK-Nps) with high drug-loading and study their anticancer efficacy on H22 hepatoma-bearing mice. Methods High drug-loading HK-Nps were successfully prepared using ultrasonic radiation and precipitation method. Bovine serum albumin (BSA) and polyvinyl pyrrolidone (PVP) were used in combination (weight ratio 1:1) as the main adjuvant. The antitumor effect of the resultant HK-Nps (ip administration) was evaluated against H22-bearing mice at different dose using CTX as a positive control. Results The obtained HK-Nps were described as smooth surface and (116.5 ± 1.3) nm in average diameter with narrow and normal distribution (PDI value being 0.116 ± 0.001). HK-Nps had high drug-loading content of 38.6% and showed quickly and significantly enhanced dissolution in comparison with HK bulk powder. In the H22-bearing mice of tumor models, HK-Nps demonstrated a dose-dependent tumor suppression effect with inhibitory rate of 52.57%, 66.33% and 71.24% respectively at low, middle, and high dose (10, 20, and 40 mg/kg). Conclusion The resultant HK-Nps have the obvious inhibitory effect on tumor.

北京市自然科学基金项目(7152099);黑龙江中医药大学重点实验室开放课题(2013kf05)