目的 制備芒果苷納米囊泡，考察其性質(zhì)、穩(wěn)定性和大鼠藥動(dòng)學(xué)研究。方法 采用乙醇注入法制備芒果苷納米囊泡。以包封率為指標(biāo)，芒果苷質(zhì)量濃度、聚山梨酯80與膽固醇比例、囊材與藥物比例為主要影響因素，采用Box-Behnken響應(yīng)面法優(yōu)化芒果苷納米囊泡處方工藝，并制成凍干粉。透射電鏡觀察芒果苷納米囊泡微觀形態(tài)，X-射線粉末衍射考察芒果苷晶型，透析袋法考察芒果苷納米囊泡在模擬胃腸液中釋藥行為。ig大鼠芒果苷納米囊泡，繪制藥時(shí)曲線，計(jì)算吸收生物利用度。結(jié)果 芒果苷納米囊泡最佳處方為：芒果苷質(zhì)量濃度為0.51 mg/mL，聚山梨酯80與膽固醇比例為1.56∶1，囊材與藥物比例為18.73∶1。芒果苷納米囊泡的平均包封率為（82.67±1.19）%，載藥量為（4.15±0.18）%，粒徑為（318.84±26.46）nm，Zeta電位為−（31.71±1.87）mV。芒果苷納米囊泡外觀呈橢圓形，芒果苷在芒果苷納米囊泡凍干粉中轉(zhuǎn)變?yōu)闊o(wú)定形，在模擬胃腸液中累積釋放度得到明顯增加。芒果苷納米囊泡血藥濃度（C_max）和相對(duì)口服吸收生物利用度分別增加至3.54、5.30倍。結(jié)論 芒果苷納米囊泡可增加芒果苷在胃腸液中累積釋放度和穩(wěn)定性，有效促進(jìn)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.

R283

上海市科技計(jì)劃項(xiàng)目（21S21903400）