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首页> 美国卫生研究院文献>Antioxidants >Preparation and Evaluation of Resveratrol-Loaded Composite Nanoparticles Using a Supercritical Fluid Technology for Enhanced Oral and Skin Delivery
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Preparation and Evaluation of Resveratrol-Loaded Composite Nanoparticles Using a Supercritical Fluid Technology for Enhanced Oral and Skin Delivery

机译：使用超临界流体技术制备和评估负载白藜芦醇的复合纳米颗粒以增强口服和皮肤输送能力

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We created composite nanoparticles containing hydrophilic additives using a supercritical antisolvent (SAS) process to increase the solubility and dissolution properties of -resveratrol for application in oral and skin delivery. Physicochemical properties of -resveratrol-loaded composite nanoparticles were characterized. In addition, an in vitro dissolution–permeation study, an in vivo pharmacokinetic study in rats, and an ex vivo skin permeation study in rats were performed. The mean particle size of all the composite nanoparticles produced was less than 300 nm. Compared to micronized -resveratrol, the -resveratrol/hydroxylpropylmethyl cellulose (HPMC)/poloxamer 407 (1:4:1) nanoparticles with the highest flux (0.792 μg/min/cm ) exhibited rapid absorption and showed significantly higher exposure 4 h after oral administration. Good correlations were observed between in vitro flux and in vivo pharmacokinetic data. The increased solubility and flux of -resveratrol generated by the HPMC/surfactant nanoparticles increased the driving force on the gastrointestinal epithelial membrane and rat skin, resulting in enhanced oral and skin delivery of -resveratrol. HPMC/surfactant nanoparticles produced by an SAS process are, thus, a promising formulation method for -resveratrol for healthcare products (owing to their enhanced absorption via oral administration) and for skin application with cosmetic products.
机译：我们使用超临界抗溶剂（SAS）工艺创建了包含亲水性添加剂的复合纳米颗粒，以提高-白藜芦醇的溶解度和溶解特性，可用于口服和皮肤输送。表征了负载白藜芦醇的复合纳米颗粒的理化性质。此外，还进行了体外溶出-渗透研究，大鼠体内药代动力学研究以及大鼠体内离体皮肤渗透研究。产生的所有复合纳米颗粒的平均粒度小于300nm。与微粉化的白藜芦醇相比，具有最高通量（0.792μg/ min / cm）的-白藜芦醇/羟丙基甲基纤维素（HPMC）/泊洛沙姆407（1：4：1）纳米颗粒表现出快速吸收，并且口服后4 h暴露量显着更高管理。在体外通量和体内药代动力学数据之间观察到良好的相关性。 HPMC /表面活性剂纳米颗粒产生的白藜芦醇的溶解度和通量增加，增加了对胃肠道上皮膜和大鼠皮肤的驱动力，从而增强了口服和皮肤对白藜芦醇的输送。因此，通过SAS方法生产的HPMC /表面活性剂纳米颗粒是用于白藜芦醇的有前途的制剂方法，该白藜芦醇用于保健产品（由于它们通过口服给药增强的吸收）以及用于皮肤与化妆品一起使用。

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