SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur, Chennai, India.
Department of Pharmaceutical Technology, University College of Engineering, Bharathidasan Institute of Technology Campus, Anna University, Tiruchirappalli, India.
Cardiovasc Hematol Agents Med Chem. 2020;18(1):45-54. doi: 10.2174/1871525718666200203112502.
The present research work discussed the preparation of lomustine loaded with chitosan nanoparticles (LNCp) by ionic gelation method with homogenization using the design on experiments by Box-Behnken design.
The nanoparticles are evaluated by particle size, zeta potential, surface morphology, drug content, entrapment efficiency and in-vitro drug release.
The FT-IR results support that drug have no interaction with excipients, which are used in the preparation of nanoparticle. The particle size, drug content and encapsulation efficiency of the developed nanoparticles ranged from 190 to 255 nm, 80.88% to 94.02%, and 77.12 to 88.74%, respectively. The drug release rate is diffusion-controlled over 8 hours. The F-value for all of the responses shows that the models are significant. The p-value, less than 0.05 for all the responses reveals the significance of the models. Graphical optimisation is done by desirability plot and overlay plot, which contains optimal values of independent variables with the desirability of 1.
In conclusion, the results suggested that the optimised lomustine loaded chitosan nanoparticles are useful for brain targeting hence hold the potential for further research and clinical application.
本研究工作讨论了通过离子凝胶化法并用 Box-Behnken 设计的均匀化法制备载洛莫司汀的壳聚糖纳米粒（LNCp）。
通过粒径、Zeta 电位、表面形态、药物含量、包封效率和体外药物释放来评价纳米粒。
傅里叶变换红外（FT-IR）结果表明，药物与纳米粒制备中使用的赋形剂之间没有相互作用。所开发的纳米粒的粒径、药物含量和包封效率范围分别为 190 至 255nm、80.88%至 94.02%和 77.12%至 88.74%。药物释放速率在 8 小时内为扩散控制。所有响应的 F 值表明模型是显著的。所有响应的 p 值均小于 0.05，表明模型具有显著性。通过可接受性图和叠加图进行图形优化，包含具有 1 可接受性的独立变量的最优值。
总之，结果表明，优化的载洛莫司汀壳聚糖纳米粒可用于脑靶向，因此具有进一步研究和临床应用的潜力。
