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Loading of 5-fluorouracil onto Halloysite nanotubes for targeted drug delivery using a subcritical gas antisolvent process (GAS)
The Journal of Supercritical Fluids ( IF 3.4 ) Pub Date : 2020-01-21 , DOI: 10.1016/j.supflu.2020.104756
Sekar Harikrishnan , Rossen Sedev , Chau Chun Beh , Craig Priest , Neil R. Foster

Halloysite clay nanotubes are efficient biocompatible nanocarriers for pharmaceutical products. A gas antisolvent (GAS) process employing subcritical carbon dioxide delivers a product with high loading (43 %) and free of residual solvent. An anticancer agent, 5-fluorouracil, was loaded on nanoclay particles. A quantitative distinction is made between tightly-bound (adsorbed) and loosely-bound (co-precipitated) drug. The physical stages of the dense gas process are clearly outlined. The strongly attached drug is released completely at pH = 7.4 but only up to 30 % in pH = 1.2. The release follows first-order kinetics with a characteristic time of 2 h. The mass ratio of clay nanotubes to 5-fluorouracil affects the loading with adsorbed drug as well as the ratio of loose to tightly attached drug molecules. The system Halloysite-5-fluorouracil can be implemented in drug delivery systems to achieve a desired release profile. The GAS process is a one-pot green process with a low solvent consumption and high-purity product.



中文翻译:

使用亚临界气体反溶剂工艺(GAS)将5-氟尿嘧啶加载到埃洛石纳米管上以进行靶向药物递送

埃洛石粘土纳米管是用于药物产品的有效生物相容性纳米载体。使用亚临界二氧化碳的气体反溶剂(GAS)工艺可提供高负荷(43%)且无残留溶剂的产品。将抗癌剂5-氟尿嘧啶负载在纳米粘土颗粒上。在紧密结合(吸附)和松弛结合(共沉淀)药物之间进行了定量区分。清楚地概述了浓密气体工艺的物理阶段。在pH = 7.4时,牢固附着的药物会完全释放,但在pH = 1.2时,最多释放30%。释放遵循一级动力学,特征时间为2 h。粘土纳米管与5-氟尿嘧啶的质量比影响吸附药物的负载以及松散的和紧密附着的药物分子的比率。系统Halloysite-5-fluorouracil可以在药物输送系统中实现所需的释放曲线。GAS工艺是一种一锅法绿色工艺,具有低溶剂消耗和高纯度产品的特点。

更新日期:2020-01-21
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