Abstract
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.
Highlights
Fisetin (3,7,3,4 -tetrahydroxyflavone, FST) (Figure 1) is a naturally occurring flavonol, which is widely distributed in common daily vegetables and fruits, such as strawberry, apple, persimmon, onion, and cucumber
This study proposed an efficient nanoparticle-based system to improve the biopharmaceutical properties of FST for oral delivery
A straightforward interfacial deposition method was employed to prepare the FST–NP, and the preparative parameters were optimized by the RSM based on CCD to achieve appropriate characteristics, including particle size, polydispersity index (PDI), EE, and zeta potential
Summary
Fisetin (3,7,3 ,4 -tetrahydroxyflavone, FST) (Figure 1) is a naturally occurring flavonol, which is widely distributed in common daily vegetables and fruits, such as strawberry, apple, persimmon, onion, and cucumber. A growing number of studies have suggested that FST possesses health-promoting potentials to alleviate several oxidative stress-associated diseases, such as metabolic syndrome and neuron degeneration. Since FST could inhibit the peroxidation of 5-lipoxygenase, increase the glutathione level, reduce the inflammatory response, FST could prevent the incidence of arteriosclerosis and neuron damage [4,5,6,7]. Several in vitro and in vivo studies have reported the neuron-protective effects of FST. Zheng et al [8] proved that FST could inhibit the activation of microglia, which would produce proinflammatory cytokines and ROS, thereby reduce the neurotoxicity with the BV−2 cell model. Maher et al [9] utilize a dual in vivo model, Drosophila and R6/2 mouse model, to demonstrate that FST has the potential to treat Huntington’s disease through the inhibition of the ERK pathway.
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