通过改良反溶剂法提高大麻二酚在玉米醇溶蛋白和乳清蛋白复合纳米颗粒中的稳定性及口服生物利用度。

Enhanced Stability and Oral Bioavailability of Cannabidiol in Zein and Whey Protein Composite Nanoparticles by a Modified Anti-Solvent Approach.

作者信息

Wang Ce, Wang Jia, Sun Yonghai, Freeman Kalev, Mchenry Monique Alyssa, Wang Cuina, Guo Mingruo

机构信息

Department of Food Science, College of Food Science and Engineering, Jilin University, Changchun 130062, China.

College of Medicine, University of Vermont, Burlington, VT 05405, USA.

出版信息

Foods. 2022 Jan 27;11(3):376. doi: 10.3390/foods11030376.

Wide applications of cannabidiol (CBD) in the food and pharmaceutical industries are limited due to its low bioavailability, sensitivity to environmental pressures and low water solubility. Zein nanoparticles were stabilized by whey protein (WP) for the delivery of cannabidiol (CBD) using a modified anti-solvent approach. Particle size, surface charge, encapsulation efficiency, and re-dispersibility of nanoparticles were influenced by the zein to WP ratio. Under optimized conditions at 1:4, zein-WP nanoparticles were fabricated with CBD (200 μg/mL) and further characterized. WP absorbed on zein surface via hydrogen bond, hydrophobic forces, and electrostatic attraction. The zein-WP nanoparticles showed excellent storage stability (4 °C, dark) and effectively protected CBD degradation against heat and UV light. In vivo pharmacokinetic study demonstrated that CBD in zein-WP nanoparticles displayed 2-times and 1.75-fold enhancement in maximum concentration (C max) and the area under curve (AUC) as compared to free-form CBD. The data indicated the feasibility of developing zein-WP based nanoparticles for the encapsulation, protection, and delivery of CBD.

由于大麻二酚（CBD）的生物利用度低、对环境压力敏感且水溶性差，其在食品和制药行业的广泛应用受到限制。采用改良的反溶剂法，用乳清蛋白（WP）稳定玉米醇溶蛋白纳米颗粒以递送大麻二酚（CBD）。纳米颗粒的粒径、表面电荷、包封率和再分散性受玉米醇溶蛋白与乳清蛋白比例的影响。在1:4的优化条件下，制备了负载CBD（200μg/mL）的玉米醇溶蛋白-乳清蛋白纳米颗粒，并对其进行了进一步表征。乳清蛋白通过氢键、疏水力和静电引力吸附在玉米醇溶蛋白表面。玉米醇溶蛋白-乳清蛋白纳米颗粒表现出优异的储存稳定性（4℃，暗处），并能有效保护CBD免受热和紫外线的降解。体内药代动力学研究表明，与游离形式的CBD相比，玉米醇溶蛋白-乳清蛋白纳米颗粒中的CBD在最大浓度（Cmax）和曲线下面积（AUC）方面分别提高了2倍和1.75倍。数据表明开发基于玉米醇溶蛋白-乳清蛋白的纳米颗粒用于CBD的包封、保护和递送是可行的。