Preparation and preliminary pharmacokinetics study of GNA‐loaded zein nanoparticles.

Objectives: Gambogenic acid (GNA), one of the main active ingredients isolated from Garcinia cambogia, has shown diverse antitumour activities. However, short biological half‐life and low oral bioavailability severely limit its clinical application. Here, we developed GNA‐loaded zein nanoparticles (GNA‐ZN‐NPs) based on phospholipid complex and zein nanoparticles to prolong the circulation time and enhance oral bioavailability of GNA. Methods: The physicochemical properties of GNA‐ZN‐NP were characterized in details. The in vitro release profile, in vivo pharmacokinetic experiments and tissue distribution of GNA‐ZN‐NPs were also evaluated. Key findings: The particle size, PDI and encapsulation efficiency of GNA‐ZN‐NPs were 102.90 nm, 0.027 and 76.35 ± 0.64%, respectively. The results of SEM, FTIR, DSC and XRD demonstrated that GNA‐ZN‐NPs were prepared successfully. The in vitro dissolution of GNA‐ZN‐NPs exhibited controlled release compared with raw GNA solution. The pharmacokinetic study showed that the AUC of GNA‐ZN‐NPs was significantly increased, and the t1/2 and MRT values of GNA‐ZN‐NPs were 3.21‐fold and 2.19‐fold higher than that of GNA solution. Tissue distribution results illustrated that GNA‐ZN‐NPs showed hepatic‐targeting properties. Conclusion: GNA‐ZN‐NPs significantly enhanced the oral bioavailability and prolonged half‐life of GNA, providing a promising oral drug delivery system to improve in vivo pharmacokinetic behaviour of GNA. [ABSTRACT FROM AUTHOR]