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Development of gold(III) thiosemicarbazonate complex–loaded PLGA nanoparticles: characterization and sustained release studies
Journal of Nanoparticle Research ( IF 2.5 ) Pub Date : 2020-11-03 , DOI: 10.1007/s11051-020-05064-6
Raphael T. C. Silva , Luciana F. Dalmolin , Jéferson A. Moreto , Carolina G. Oliveira , Antonio E. H. Machado , Renata F. V. Lopez , Pedro I. S. Maia

The gold(III) complex [AuCl(L1)] has been reported as a lead candidate for Chagas’ disease (CD) treatment. However, in order to be effective, the drug must first reach the target tissue and then be delivered in therapeutic amounts. In this context, nanoparticles (NPs) of poly(lactic-co-glycolic acid) (PLGA) have been developed to be used as delivery systems for [AuCl(L1)]. The [AuCl(L1)]-PLGA-NPs were prepared via the emulsification and solvent evaporation technique and displayed encapsulation efficiency around 90% with the size range of 275 ± 5 nm, polydispersity index (PDI) around 0.115, and a higher value of zeta potential (− 6.51 ± 0.47 mV) compared to blank NPs (without gold complex), which agree with the formation of a cationic species in solution, as indicated by computational calculations. Additionally, high-resolution images obtained by SEM showed the [AuCl(L1)]-PLGA-NPs spherical shape with average sizes close to those analyzed by the DLS technique. Stability studies for the [AuCl(L1)]-PLGA-NPs pointed out that no significant changes in relation to size and PDI occur over almost 2 months of storage at 8 °C. The release of the complex from NPs was about 10% in 24 h, followed by a slow release. By means of the Korsmeyer-Peppas model, it was possible to identify the release mechanism as being through diffusion and relaxation of the polymeric matrix. Overall, it has been shown that the PLGA-NPs are promising carriers for delivery of [AuCl(L1)] and are recommended to be investigated as formulations for parasite treatment in vivo experiments.



中文翻译:

巯基氨基甲酸金(III)负载的PLGA纳米粒子的开发:表征和持续释放研究

据报道,金(III)络合物[AuCl(L 1)]是查加斯病(CD)治疗的主要候选药物。然而,为了有效,药物必须首先到达靶组织,然后以治疗量递送。在这种情况下,已经开发了聚乳酸-乙醇酸共聚物(PLGA)的纳米颗粒(NPs)作为[AuCl(L 1)]的输送系统。[AuCl(L 1)]-PLGA-NPs是通过乳化和溶剂蒸发技术制备的,封装效率约为90%,尺寸范围为275±5 nm,多分散指数(PDI)约为0.115,ζ电位值较高(-6.51与空白NPs(不含金配合物)相比,其精度为±0.47 mV),这与溶液中阳离子物质的形成相符,如计算结果所示。此外,通过SEM获得的高分辨率图像显示[AuCl(L 1)]-PLGA-NPs球形,其平均大小接近DLS技术分析的大小。[AuCl(L 1)]-PLGA-NPs指出,在8°C下储存近2个月,尺寸和PDI均无明显变化。在24小时内,复合物从NP中的释放约为10%,然后缓慢释放。通过Korsmeyer-Peppas模型,可以确定释放机理是通过聚合物基质的扩散和松弛。总体而言,已显示PLGA-NP是用于[AuCl(L 1)]传递的有希望的载体,并建议作为体内实验中用于寄生虫治疗的制剂进行研究。

更新日期:2020-11-04
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