高载药量和厚朴酚纳米粒的制备及其抗肿瘤作用研究

Preparation of honokiol nanoparticles with high drug-loading and their premilinary antitumor efficacy

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.