Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001, India.
Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney (UTS), Ultimo, NSW 2007, Australia.
Future Med Chem. 2020 Nov;12(22):2019-2034. doi: 10.4155/fmc-2020-0083. Epub 2020 Oct 30.
In the present study boswellic acids-loaded chitosan nanoparticles were synthesized using ionic gelation technique. The influence of independent variables were studied and optimized on dependent variables using central composite design. The designed nanoparticles were observed spherical in shape with an average size of 67.5-187.2 nm and have also shown an excellent entrapment efficiency (80.06 ± 0.48). The cytotoxicity assay revealed enhanced cytotoxicity for drug-loaded nanoparticles in contrast to the free drug having an IC value of 17.29 and 29.59 μM, respectively. Flow cytometry confirmed that treatment of cells with 40 μg/ml had arrested 22.75 ± 0.3% at SubG phase of the cell cycle when compared with untreated A459 cells. The observed results justified the boswellic acids-loaded chitosan nanoparticles were effective due to greater cellular uptake, sustained intercellular drug retention and enhanced antiproliferative effect by inducing apoptosis.
在本研究中，采用离子凝胶技术合成了负载乳香酸的壳聚糖纳米粒子。使用中心复合设计研究了独立变量对依赖变量的影响，并对其进行了优化。设计的纳米粒子呈球形，平均粒径为 67.5-187.2nm，包封率也很高（80.06±0.48）。细胞毒性试验表明，与游离药物相比，载药纳米粒子具有更高的细胞毒性，其 IC 值分别为 17.29 和 29.59μM。流式细胞术证实，与未处理的 A459 细胞相比，用 40μg/ml 的药物处理细胞时，细胞周期的 SubG 期被阻滞了 22.75±0.3%。观察到的结果表明，负载乳香酸的壳聚糖纳米粒子由于具有更高的细胞摄取率、持续的细胞内药物滞留和通过诱导细胞凋亡增强的抗增殖作用而有效。
