Li Zhu Meijuan Sun -, Longyuan Wang -, Yuefen Liu -, Haijun Qu -
Department of Pharmacy, The Affiliated Hospital of Qingdao University, Qingdao, China.
Pak J Pharm Sci. 2023 May;36(3):755-764.
The curcumin niosomes were prepared and evaluated. The film dispersion method was applied, the formulation was optimized by single factor experiment and central composite design. The optimum formulation was as follows: the ratio of Span80 to cholesterol was 4.2:1, the ratio of cholesterol to curcumin was 5:1, PBS volume was 20.9 mL, hydration speed was 381 r/min, hydration time was 1.5 h, temperature was 50C. The encapsulation efficiency of curcumin niosomes was 88.5%, average particle size was 162 nm, the Zeta potential was (-28.9±2.7) mV and the shape was regular. In intro, the niosomes exhibited good delayed release characteristics, and the drug release was in accordance with Ritger-peppas model. In vivo, the mean retention time (MRT) of curcumin niosomes (6.604±0.209 h) was significantly extended than that of the curcumin suspensions (2.498±0.016 h); the AUC of niosomes (2074.989±146.690 ng·mL·h) was significantly larger than that of the suspensions (803.475±23.335 ng·mL·h), the relative bioavailability was 258.25%. The study showed a great potential of curcumin niosomes as a good formulation with improved oral absorption.
制备并评估了姜黄素脂质体。采用薄膜分散法，通过单因素实验和中心复合设计对配方进行优化。最佳配方如下：司盘80与胆固醇的比例为4.2:1，胆固醇与姜黄素的比例为5:1，磷酸盐缓冲液（PBS）体积为20.9 mL，水化速度为381转/分钟，水化时间为1.5小时，温度为50℃。姜黄素脂质体的包封率为88.5%，平均粒径为162 nm，Zeta电位为（-28.9±2.7）mV，形状规则。在体外，脂质体表现出良好的缓释特性，药物释放符合Ritger-peppas模型。在体内，姜黄素脂质体的平均滞留时间（MRT）（6.604±0.209小时）比姜黄素混悬液（2.498±0.016小时）显著延长；脂质体的曲线下面积（AUC）（2074.989±146.690 ng·mL·h）显著大于混悬液（803.475±23.335 ng·mL·h），相对生物利用度为258.25%。该研究表明姜黄素脂质体作为一种具有改善口服吸收的良好制剂具有巨大潜力。
