Materials Synthesis and Characterization Laboratory, Institute of Advanced Technology (ITMA), Universiti Putra Malaysia, Serdang 43400, Selangor, Malaysia.
Laboratory for Vaccine and Immunotherapeutic, Institute of Biosciences, Universiti Putra Malaysia, Serdang 43400, Selangor, Malaysia.
Int J Mol Sci. 2019 Aug 1;20(15):3764. doi: 10.3390/ijms20153764.
One of the current developments in drug research is the controlled release formulation of drugs, which can be released in a controlled manner at a specific target in the body. Due to the diverse physical and chemical properties of various drugs, a smart drug delivery system is highly sought after. The present study aimed to develop a novel drug delivery system using magnetite nanoparticles as the core and coated with polyvinyl alcohol (PVA), a drug 5-fluorouracil (5FU) and Mg-Al-layered double hydroxide (MLDH) for the formation of FPVA-FU-MLDH nanoparticles. The existence of the coated nanoparticles was supported by various physico-chemical analyses. In addition, the drug content, kinetics, and mechanism of drug release also were studied. 5-fluorouracil (5FU) was found to be released in a controlled manner from the nanoparticles at pH = 4.8 (representing the cancerous cellular environment) and pH = 7.4 (representing the blood environment), governed by pseudo-second-order kinetics. The cytotoxicity study revealed that the anticancer delivery system of FPVA-FU-MLDH nanoparticles showed much better anticancer activity than the free drug, 5FU, against liver cancer and HepG2 cells, and at the same time, it was found to be less toxic to the normal fibroblast 3T3 cells.
药物研究的当前发展之一是药物的控制释放制剂，它可以在体内的特定靶标以受控方式释放。由于各种药物的物理和化学性质不同，因此非常需要智能药物输送系统。本研究旨在开发一种新型药物输送系统，该系统使用磁铁矿纳米粒子作为核心，并涂覆有聚乙烯醇（PVA），药物 5-氟尿嘧啶（5FU）和 Mg-Al 层状双氢氧化物（MLDH），以形成 FPVA-FU-MLDH 纳米粒子。通过各种物理化学分析支持涂覆纳米粒子的存在。此外，还研究了药物含量，药物释放动力学和机制。发现 5-氟尿嘧啶（5FU）在 pH = 4.8（代表癌细胞环境）和 pH = 7.4（代表血液环境）时从纳米粒子中以受控方式释放，遵循伪二阶动力学。细胞毒性研究表明，FPVA-FU-MLDH 纳米粒子的抗癌输送系统显示出比游离药物 5FU 更好的抗癌活性，针对肝癌和 HepG2 细胞，同时发现对正常成纤维细胞 3T3 细胞的毒性较小。
