GITAM School of Pharmacy, GITAM Deemed to be University, Rudraram, Hyderabad, Telangana, India.
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
Carbohydr Polym. 2023 Nov 1;319:121177. doi: 10.1016/j.carbpol.2023.121177. Epub 2023 Jul 6.
The current study aimed to overcome the poor solubility and colon-specific delivery of curcumin (CUR) by formulating a curcumin nanosuspension (CUR-NS) using the antisolvent precipitation method. Freeze-dried CUR-NS was encapsulated into microbeads (CUR-NS-MB) by the ionotropic gelation method using zinc chloride (as a cross-linking agent) with the help of rate-controlling polymers, pectin, and chitosan. Furthermore, cellulose acetate phthalate (CAP) is incorporated as an enteric polymer to protect against acidic medium degradation. Particle size, surface morphology, interaction studies, and entrapment studies were performed to optimize CUR-NSs. Nanosuspensions stabilized with hydroxypropyl methylcellulose (HPMC E-15; 1 % w/v) showed an average particle size of 193.5 ± 4.31 nm and a polydispersity index (PDI) of 0.261 ± 0.020. The optimized microbeads (CUR-NS-MB) showed 89.45 ± 3.11 % entrapment efficiency with a drug loading of 14.54 ± 1.02 %. The optimized formulation (CUR-NS-MB) showed colon-specific in vitro drug release bypassing acid pH degradation. In animal studies, a 2.5-fold increase in C and a 4.4-fold increase in AUC were observed with CUR-NS-MB, which was more significant than that of plain CUR. Therefore, the developed CUR-NS-MB has the potential to be used as a colon-specific delivery system.
本研究旨在通过反溶剂沉淀法制备姜黄素（CUR）纳米混悬剂（CUR-NS）来克服 CUR 溶解度差和结肠特异性递送的问题。采用离子凝胶法，在控制释放聚合物果胶和壳聚糖的帮助下，将冷冻干燥的 CUR-NS 包封到微球（CUR-NS-MB）中。此外，还将邻苯二甲酸醋酸纤维素（CAP）作为肠溶聚合物加入，以防止在酸性介质中降解。进行了粒径、表面形态、相互作用研究和包封研究，以优化 CUR-NS。用羟丙基甲基纤维素（HPMC E-15；1%w/v）稳定的纳米混悬剂的平均粒径为 193.5±4.31nm，多分散指数（PDI）为 0.261±0.020。优化的微球（CUR-NS-MB）的包封效率为 89.45±3.11%，载药量为 14.54±1.02%。优化的制剂（CUR-NS-MB）在体外具有结肠特异性释药作用，可绕过酸性 pH 降解。在动物研究中，CUR-NS-MB 使 C 增加了 2.5 倍，AUC 增加了 4.4 倍，明显优于普通 CUR。因此，开发的 CUR-NS-MB 有可能作为一种结肠特异性递送系统。
