载咖啡酸苯乙酯纳米颗粒构建及抗氧化性研究

Fabrication and Antioxidant Property Characterization of Caffeic Acid Phenethyl Ester-loaded Nanoparticles

摘要:

【目的】改善咖啡酸苯乙酯（ caffeic acid phenethyl ester，CAPE）在水溶液中的分散度和利用度。【方法】以反溶剂分散法构建载CAPE大麦醇溶蛋白（CAPE-HD）纳米颗粒，对其理化性能进行表征，并考察其在Caco-2细胞内的抗氧化性能。【结果】CAPE-HD纳米颗粒中各组分之间通过氢键等非共价作用相互结合，并在形成纳米颗粒后，CAPE的存在状态发生了变化。CAPE-HD纳米颗粒呈近球形颗粒，平均粒径为193.93 nm，平均PDI为0.26，平均Zeta电位为14.50 mV，并在28 d内保持稳定。纳米颗粒具有良好的包封率和载药率，以及优越的生物相容性。抗氧化试验显示，CAPE-HD纳米颗粒在DPPH自由基清除能力和Caco-2细胞内均表现出良好的抗氧化活性。【结论】该纳米体系为提高CAPE等难溶性药物的生物利用度和临床使用率提供了一个新的平台和思路。

Abstract:

[Objective]This study aims to improve the dispersion and utilization of caffeic acid phenethyl ester (CAPE) in aqueous solutions.[Method]CAPE-loaded hordein (CAPE-HD) nanoparticles were constructed via an anti-solvent precipitation method. The physicochemical properties of the nanoparticles were characterized, and the antioxidant properties of the nanoparticles within Caco-2 cells were investigated.[Result]The components within the CAPE-HD nanoparticles interacted through non-covalent bonds, such as hydrogen bonding, resulting in an altered state of CAPE upon nanoparticle formation. The CAPE-HD nanoparticles exhibited near-spherical morphology with an average particle size of 193.93 nm, an average polydispersity index (PDI) of 0.26, and average Zeta potential of 14.50 mV. These nanoparticles remained stable over 28 days and demonstrated favorable encapsulation efficiency, drug loading capacity, and biocompatibility. Antioxidant assays revealed that the CAPE-HD nanoparticles exhibited remarkable antioxidant activity, in terms of both DPPH free radical scavenging ability and within the Caco-2 cell model.[Conclusion]This nano-delivery system provides a promising platform and strategy for enhancing the bioavailability and clinical application of poorly water-soluble drugs such as CAPE.