目的 研究一種高載藥量和厚樸酚納米粒, 評價其對小鼠肝癌H22移植瘤的生長抑制作用。方法 用牛血清白蛋白(BSA)和聚乙烯吡咯烷酮(PVP)為輔料, 采用超聲-沉淀法制備和厚樸酚納米粒。建立H22肝癌皮下小鼠腫瘤模型, 以環(huán)磷酰胺注射液(CTX)為陽性對照, 考查ip給藥后其對腫瘤的抑制作用。結(jié)果 和厚樸酚納米粒呈球形, 平均粒徑為(116.5±1.3)nm, 多分散指數(shù)(PDI)為0.116±0.001, 體外溶出較原料藥大幅度提升。在H22荷瘤小鼠體內(nèi), 和厚樸酚納米粒顯示出劑量相關(guān)的抑瘤作用, 低、中、高劑量(10、20、40 mg/kg)組抑瘤率分別為52.57%、66.33%和71.24%。結(jié)論 和厚樸酚納米粒對腫瘤有明顯的抑制作用。

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.

北京市自然科學(xué)基金項(xiàng)目(7152099);黑龍江中醫(yī)藥大學(xué)重點(diǎn)實(shí)驗(yàn)室開放課題(2013kf05)