Encapsulation of epigallocatechin-3-gallate into albumin nanoparticles improves pharmacokinetic and bioavailability in rat model

将表没食子儿茶素没食子酸酯封装到白蛋白纳米颗粒中可改善大鼠模型中的药代动力学和生物利用度

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作者:Nithya Ramesh, Abul Kalam Azad Mandal

Abstract

In the present study, we fabricated epigallocatechin-3-gallate (EGCG) loaded albumin nanoparticles (Alb-NP-EGCG) to enhance bioavailability and improve pharmacokinetic parameters of EGCG. The physicochemical properties of the Alb-NP-EGCG were studied using scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction and in vitro release studies. Characterization of Alb-NP-EGCG indicated the formation of spherical nanoparticles with no drug and excipient interaction. Alb-NP-EGCG showed a high drug loading capacity of 92%. Further, in vitro study showed a sustained release of EGCG from Alb-NP-EGCG over a period of 48 h. Mathematical modeling and release kinetics indicated that the Alb-NP-EGCG followed zero order kinetic and EGCG was released via fickian diffusion method. In vivo bioavailability and distribution of Alb-NP-EGCG showed an enhanced plasma concentration of EGCG with 1.5 fold increase along with prolonged T 1/2 of 15.6 h in the system when compared with the free EGCG. All this study demonstrated the fabrication of EGCG loaded albumin nanoparticles which favored the slow and sustained release of EGCG with improved pharmacokinetics and bioavailability thereby prolonging the action of EGCG. Additional acute and sub-acute toxicity test of the Alb-NP-EGCG demonstrated the safety of the Alb-NP-EGCG. Therefore, the Alb-NP-EGCG could be a promising drug delivery system for EGCG.

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