School of Pharmacy, The University of Nottingham, Malaysia Campus, Jalan Broga, Semenyih, Malaysia.
Pharm Dev Technol. 2013 May-Jun;18(3):591-9. doi: 10.3109/10837450.2011.640688. Epub 2011 Dec 10.
In the present study, we investigate the mucoadhesive characteristics and release of the anticancer agent curcumin, contained in chitosan nanoparticles (CS-NPs). Such a system has potential therapeutic benefits in the treatment of colon cancer through prolonged retention and delivery. The CS-NPs were ionically gelled with tripolyphosphate (TPP) and registered an isoelectric pH of 6.2 (z-average diameter of 214 nm ± 1.0 nm). pH variations around the isoelectric point caused a reduction in CS-NPs electrical charge which correspondingly increased the z-average due to agglomeration. Curcumin release from CS-NPs was slowest at chitosan to TPP weight ratio of 3:1, with a significant retention (36%) at the end of 6 h. Adsorption isotherms of mucin on CS-NPs fitted both the Freundlich and Langmuir models, suggesting a monolayer-limited adsorption on heterogeneous sites with varied affinities. Encapsulated curcumin exerted an influence on the adsorption of mucin due to H-bonding as well as π-π interactions between the phenolic moieties of curcumin and mucin.
在本研究中，我们研究了载有抗癌药物姜黄素的壳聚糖纳米粒子（CS-NPs）的粘膜粘附特性和释放。通过延长保留和输送时间，这种系统在治疗结肠癌方面具有潜在的治疗益处。CS-NPs 与三聚磷酸（TPP）离子交联，等电 pH 值为 6.2（Z 均粒径为 214nm±1.0nm）。等电点周围 pH 值的变化导致 CS-NPs 电荷减少，相应地由于聚集而使 Z 均粒径增加。当壳聚糖与 TPP 的重量比为 3:1 时，CS-NPs 中姜黄素的释放最慢，在 6 小时结束时保留率显著（36%）。粘蛋白在 CS-NPs 上的吸附等温线同时符合 Freundlich 和 Langmuir 模型，表明在具有不同亲和力的异质位点上存在单层限制吸附。由于氢键以及姜黄素和粘蛋白的酚部分之间的π-π相互作用，包封的姜黄素对粘蛋白的吸附有影响。
