Self-assembled micelles based on gambogenic acid-phospholipid complex for sustained-release drug delivery

Abstract

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.

Keywords:

• GNA
• GNA-PLC
• GNA-PLC micelles
• self-assembly
• in vitro release
• pharmacokinetic

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

The authors all acknowledge the funding support from the National Natural Science Foundation of China [51303006, 81703805], the Provincial Natural Science Foundation of Anhui Province [KJ2018ZD031, 1408085MH196] and the University excellent top-notch personnel training fund of Anhui Province [gxfx2017050].