Objective: To improve the water solubility and enhance the oral bioavailability of gambogenic acid (GNA).

Methods: GNA-phospholipid complex (GNA-PLC) micelles were successfully prepared by anti-solvent method.

Results: The encapsulation efficiency of GNA-PLC micelles can reach 99.33 % (w/w). The average particle size of the GNA-PLC micelles was 291.23 nm which was approximate agreed with the transmission electron microscopy (TEM). In vitro release profile showed the GNA-PLC and GNA-PLC micelles have significant sustained-release of GNA compared with crude GNA. Pharmacokinetic parameters indicated that the area under concentration–time curve (AUC_0→t) of GNA in cases of GNA-PLC and GNA-PLC micelles are 2.04- and 3.92-fold higher than crude GNA, respectively.

Conclusions: The better water solubility and higher bioavailability of GNA in GNA-PLC micelles with significant sustained-release of GNA endow the nanoparticle with great potential in GNA delivery system.

目的：提高甘草酸（GNA）的水溶性并提高其口服生物利用度。

方法：采用反溶剂法成功制备了GNA-磷脂复合物（GNA-PLC）胶束。

结果： GNA-PLC胶束的包封率可达到99.33％（w / w）。GNA-PLC胶束的平均粒径为291.23 nm，与透射电子显微镜（TEM）近似一致。体外释放曲线表明，与粗制GNA相比，GNA-PLC和GNA-PLC胶束具有显着的GNA持续释放。药代动力学参数表明，在GNA-PLC和GNA-PLC胶束的情况下，GNA的浓度-时间曲线下面积（AUC _0→t）分别比粗GNA高2.04倍和3.92倍。

结论：在GNA-PLC胶束中，GNA具有较好的水溶性和较高的生物利用度，且GNA的持续释放能力强，这使纳米粒子在GNA传递系统中具有巨大潜力。