目的 制备芒果苷纳米囊泡，考察其性质、稳定性和大鼠药动学研究。方法 采用乙醇注入法制备芒果苷纳米囊泡。以包封率为指标，芒果苷质量浓度、聚山梨酯80与胆固醇比例、囊材与药物比例为主要影响因素，采用Box-Behnken响应面法优化芒果苷纳米囊泡处方工艺，并制成冻干粉。透射电镜观察芒果苷纳米囊泡微观形态，X-射线粉末衍射考察芒果苷晶型，透析袋法考察芒果苷纳米囊泡在模拟胃肠液中释药行为。ig大鼠芒果苷纳米囊泡，绘制药时曲线，计算吸收生物利用度。结果 芒果苷纳米囊泡最佳处方为：芒果苷质量浓度为0.51 mg/mL，聚山梨酯80与胆固醇比例为1.56∶1，囊材与药物比例为18.73∶1。芒果苷纳米囊泡的平均包封率为（82.67±1.19）%，载药量为（4.15±0.18）%，粒径为（318.84±26.46）nm，Zeta电位为−（31.71±1.87）mV。芒果苷纳米囊泡外观呈椭圆形，芒果苷在芒果苷纳米囊泡冻干粉中转变为无定形，在模拟胃肠液中累积释放度得到明显增加。芒果苷纳米囊泡血药浓度（C_max）和相对口服吸收生物利用度分别增加至3.54、5.30倍。结论 芒果苷纳米囊泡可增加芒果苷在胃肠液中累积释放度和稳定性，有效促进了口服吸收。

Objective To prepare mangiferin nanovesicles (MF-NVs), and study its properties, stability, and pharmacokinetics in rats.Methods Ethanol injection method was employed to prepare MF-NVs. Envelopment rate was used as evaluation indexes, mangiferin concentration, Tween 80 to cholesterol ratio, and materials to drug ratio were acted as main factors, Box-Behnken design-response surface method was employed to optimize the prescriptions of MF-NVs, and its lyophilized powder was also prepared. Transmission electron microscope (TEM) was employed to observe the microscopic morphology of MF-NVs, X-ray powder diffraction (XRPD) was used to investigate the crystal form of mangiferin. Dialysis bag method was used to investigate its release behavior in simulated gastrointestinal fluid. After ig administration of MF-NVs for rat, drug-time curve was drawn and the oral bioavailability was calculated.Results The optimal formulation of MF-NVs: mangiferin concentration was 0.51 mg/mL, Tween 80 to cholesterol ratio was 1.56:1, materials to drug ratio was 18.73:1. Envelopment efficiency, drug loading, particle size and Zeta potential of MF-NVs were (82.67 ± 1.19)%, (4.15 ± 0.18)%, (318.84 ± 26.46) nm, and −(31.71 ± 1.87) mV, respectively. The appearance of MF-NVs was oval. Mangiferin in MF-NVs lyophilized powder was transformed into amorphous state, and cumulative release rate of mangiferin was significantly increased in simulated gastrointestinal fluid. C _max and relative oral bioavailability of MF-NVs were increased to 3.54 and 5.30 times, respectively.Conclusion MF-NVs can increase cumulative release rate of mangiferin in gastrointestinal fluid, and promote oral absorption effectively.

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上海市科技计划项目（21S21903400）