School of Pharmacy, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
Drug Development and Value Creation Research Center, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
Molecules. 2021 May 19;26(10):3031. doi: 10.3390/molecules26103031.
This study aimed to design an effective nanoparticle-based carrier for the oral delivery of fisetin (FST) with improved biopharmaceutical properties. FST-loaded nanoparticles were prepared with polyvinyl alcohol (PVA) and poly(lactic-co-glycolic acid) (PLGA) by the interfacial deposition method. A central composite design of two independent variables, the concentration of PVA and the amount of PLGA, was applied for the optimization of the preparative parameter. The responses, including average particle size, polydispersity index, encapsulation efficiency, and zeta potential, were assessed. The optimized formulation possessed a mean particle size of 187.9 nm, the polydispersity index of 0.121, encapsulation efficiency of 79.3%, and zeta potential of -29.2 mV. The morphological observation demonstrated a globular shape for particles. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that the encapsulated FST was presented as the amorphous state. The dissolution test indicated a 3.06-fold increase for the accumulating concentrations, and the everted gut sac test showed a 4.9-fold gain for permeability at the duodenum region. In conclusion, the optimized FST-loaded nanoparticle formulation in this work can be developed as an efficient oral delivery system of FST to improve its biopharmaceutic properties.
本研究旨在设计一种有效的基于纳米粒子的载体，用于改善生物制药特性的 fisetin（FST）的口服递送。采用界面沉积法，用聚乙烯醇（PVA）和聚乳酸-共-羟基乙酸（PLGA）制备 FST 负载的纳米粒子。应用两独立变量（PVA 的浓度和 PLGA 的量）的中心复合设计，对制备参数进行优化。评估响应，包括平均粒径、多分散指数、包封效率和 Zeta 电位。优化的配方具有平均粒径为 187.9nm、多分散指数为 0.121、包封效率为 79.3%和 Zeta 电位为-29.2mV。形态观察表明颗粒呈球形。差示扫描量热法和粉末 X 射线衍射研究证实，包封的 FST 呈无定形态。溶出试验表明累积浓度增加了 3.06 倍，外翻肠囊试验表明十二指肠区域的透过性增加了 4.9 倍。总之，本研究中优化的 FST 负载纳米粒子配方可开发为 FST 的有效口服递送系统，以改善其生物制药特性。
