Department of Chemical Engineering, National Institute of Technology, Tiruchirappalli 620 015, Tamil Nadu, India.
Department of Chemistry, National Institute of Technology, Tiruchirappalli 620 015, Tamil Nadu, India.
Eur J Pharm Sci. 2018 Apr 30;116:48-60. doi: 10.1016/j.ejps.2018.01.023. Epub 2018 Feb 3.
The aim of the present investigation is the development, optimization and characterization of curcumin-loaded hybrid nanoparticles of vanillin-chitosan coated with super paramagnetic calcium ferrite. The functionally modified vanillin-chitosan was prepared by the Schiff base reaction to enhance the hydrophobic drug encapsulation efficiency. Calcium ferrite (CFNP) nano particles were added to the vanillin modified chitosan to improve the biocompatibility. The vanillin-chitosan-CFNP, hybrid nanoparticle carrier was obtained by ionic gelation method. Characterizations of the hybrid materials were performed by XRD, FTIR, H NMR, TGA, AFM and SEM techniques to ensure the modifications on the chitosan material. Taguchi method was applied to optimize the drug (curcumin) encapsulation efficiency by varying the drug to chitosan-vanillin, CFNP to chitosan-vanillin and TPP (sodium tripolyphospate) to chitosan-vanillin ratios. The maximum encapsulation efficiency was obtained as 98.3% under the conditions of 0.1, 0.75 and 1.0 for the drug to chitosan-vanillin, CFNP to chitosan-vanillin and TPP to chitosan-vanillin ratios, respectively. The curcumin release was performed at various pH, initial drug loading concentrations and magnetic fields. The drug release mechanism was predicted by fitting the experimental kinetic data with various drug release models. The drug release profiles showed the best fit with Higuchi model under the most of conditions. The drug release mechanism followed both non-Fickian diffusion and case II transport mechanism for chitosan, however the non-Fickian diffusion mechanism was followed for the vanillin modified chitosan. The biocompatibility of the hybrid material was tested using L929 fibroblast cells. The cytotoxicity test was performed against MCF-7 breast cancer cell line to check the anticancer property of the hybrid nano carrier with the curcumin drug.
本研究旨在开发、优化和表征载姜黄素的香草醛壳聚糖混合纳米粒子，并用超顺磁性的钙铁氧体进行包覆。功能性修饰的香草醛壳聚糖是通过席夫碱反应制备的，以提高疏水性药物包封效率。将纳米钙铁氧体（CFNP）添加到香草醛改性壳聚糖中，以提高生物相容性。通过离子凝胶法得到香草醛壳聚糖-CFNP 混合纳米载体。采用 XRD、FTIR、H NMR、TGA、AFM 和 SEM 技术对混合材料进行表征，以确保壳聚糖材料的修饰。采用 Taguchi 法通过改变药物（姜黄素）与壳聚糖-香草醛、CFNP 与壳聚糖-香草醛和 TPP（三聚磷酸钠）与壳聚糖-香草醛的比例来优化药物（姜黄素）的包封效率。在药物与壳聚糖-香草醛、CFNP 与壳聚糖-香草醛和 TPP 与壳聚糖-香草醛的比例分别为 0.1、0.75 和 1.0 的条件下，获得了最大包封效率为 98.3%。在各种 pH 值、初始药物负载浓度和磁场下进行姜黄素释放。通过将实验动力学数据与各种药物释放模型拟合，预测药物释放机制。在大多数情况下，药物释放曲线与 Higuchi 模型拟合最好。在壳聚糖中，药物释放机制遵循非 Fickian 扩散和 II 型传输机制，而在香草醛修饰的壳聚糖中，遵循非 Fickian 扩散机制。通过 L929 成纤维细胞测试混合材料的生物相容性。用 MCF-7 乳腺癌细胞系进行细胞毒性试验，以检查载有姜黄素药物的混合纳米载体的抗癌性能。
