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Self-assembled micelles based on gambogenic acid-phospholipid complex for sustained-release drug delivery.
Journal of Microencapsulation ( IF 3.0 ) Pub Date : 2019-09-04 , DOI: 10.1080/02652048.2019.1656294
Beilei Wang 1 , Weiye Cheng 1 , Caiyun Zhang 1 , Youmei Bao 2 , Liqiong Zha 1 , Jiajia Qian 1 , Lufeng Hong 1 , Weidong Chen 1
Affiliation  

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 (AUC0→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.



中文翻译:

基于甘菊酸-磷脂复合物的自组装胶束,用于缓释药物递送。

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。

更新日期:2019-09-04
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