Polysorbate 80‐coated PLGA nanoparticles improve the permeability of acetylpuerarin and enhance its brain‐protective effects in rats
作者： Deqing Sun , Aiying Xue , Bin Zhang , Haiyan Lou , Huanying Shi
DOI: 10.1111/JPHP.12481
关键词:
摘要: Objectives Acetylpuerarin (AP) is an acetylated derivative of puerarin (PUE). The study aimed to prepare polysorbate 80-coated poly(lactic-co-glycolic acid) (PLGA) nanoparticles improve the permeability AP across blood–brain barrier (BBB) and enhance its brain-protective effects. Methods AP-loaded PLGA (AP-PLGA-NPs) were prepared using a solvent diffusion methodology. NPs characterized. pharmacokinetics, tissue distributions effects AP-PLGA-NPs evaluated in animals. Key findings AP-PLGA-NPs successfully with mean particle size 145.0 nm zeta potential −14.81 mV. in-vitro release from PLGA-NPs showed biphasic profile. was metabolized into PUE rats. AUC0−∞ values for 2.90- 2.29-fold as great those solution, respectively. relative targeting efficiency brain 2.40 2.58 PUE, ratios peak concentration 1.91 1.89 Compared crude drug, better rats. Conclusion Polysorbate can cross BBB
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