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Preparation and characterization of dithiocarbazate Schiff base–loaded poly(lactic acid) nanoparticles and analytical validation for drug quantification
Colloid and Polymer Science ( IF 2.4 ) Pub Date : 2019-10-31 , DOI: 10.1007/s00396-019-04572-9
Thacilla Ingrid de Menezes , Rebeca de Oliveira Costa , Rute Nazaré Fernandes Sanches , Denise de Oliveira Silva , Rodrigo Luis Silva Ribeiro Santos

Dithiocarbazate Schiff bases have been reported as a class of compounds that exhibit a wide range of pharmacological activities against neglected diseases such as malaria, trypanosomiasis, and tuberculosis. This work reports the encapsulation of the 1-(S-benzyldithiocarbazate)-3-methyl-5-phenyl-pyrazole (DTC) into biodegradable polymeric nanoparticles (NPs) of poly(lactic acid) (PLA) aiming potential drug delivery application. The DTC-loaded PLA-NPs were prepared by the single-nanoemulsification method using the poly(vinyl alcohol) (PVA) as a surfactant. The nanostructured system was characterized mainly by dynamic light scattering (DLS), electrophoretic light scattering (ELS), and transmission electron microscopy (TEM). The NPs show good colloidal stability exhibiting mean hydrodynamic diameter 157 ± 5 nm and zeta potential − 36 ± 3 mV. The encapsulation efficiency and drug loading were 52 ± 14% and 4.8 ± 1.5%, respectively. The quantifications of DTC and residual PVA in the NPs were performed by UV-Vis absorption spectroscopy. The analytical methods were validated according to regulatory agencies. Both quantification analytical curves showed good precision, in repeatability (intra-day) and intermediate (inter-day), and also good accuracy with low values of detection and quantification. The new nanostructured system, DTC-loaded PLA-NPs, shows advantages to improve stability and to overcome water solubility problems of the dithiocarbazate Schiff bases aiming potential drug delivery applications. Graphical abstract . .

中文翻译:

二硫代氨基甲酸酯席夫碱负载聚乳酸纳米颗粒的制备和表征以及药物定量的分析验证

据报道,二硫代氨基甲酸席夫碱是一类对被忽视的疾病(如疟疾、锥虫病和结核病)表现出广泛药理活性的化合物。这项工作报告了将 1-(S-苄基二硫代氨基甲酸酯)-3-甲基-5-苯基-吡唑 (DTC) 封装到聚乳酸 (PLA) 的可生物降解聚合物纳米粒子 (NPs) 中,旨在潜在的药物递送应用。使用聚乙烯醇 (PVA) 作为表面活性剂,通过单纳米乳化法制备负载 DTC 的 PLA-NPs。纳米结构系统的特征主要是动态光散射 (DLS)、电泳光散射 (ELS) 和透射电子显微镜 (TEM)。纳米颗粒显示出良好的胶体稳定性,平均流体动力学直径为 157 ± 5 nm,zeta 电位为 - 36 ± 3 mV。包封率和载药量分别为 52±14% 和 4.8±1.5%。纳米颗粒中 DTC 和残留 PVA 的定量是通过紫外-可见吸收光谱法进行的。根据监管机构对分析方法进行了验证。两条定量分析曲线在重复性(日内)和中间(日间)方面均显示出良好的精密度,并且在检测和定量值较低的情况下也具有良好的准确度。新的纳米结构系统,负载 DTC 的 PLA-NPs,显示出提高稳定性和克服二硫代氨基甲酸酯席夫碱的水溶性问题的优势,旨在潜在的药物递送应用。图形概要 。. 纳米颗粒中 DTC 和残留 PVA 的定量是通过紫外-可见吸收光谱法进行的。根据监管机构对分析方法进行了验证。两条定量分析曲线在重复性(日内)和中间(日间)方面均显示出良好的精密度,并且在检测和定量值较低的情况下也具有良好的准确度。新的纳米结构系统,负载 DTC 的 PLA-NPs,显示出提高稳定性和克服二硫代氨基甲酸酯席夫碱的水溶性问题的优势,旨在潜在的药物递送应用。图形概要 。. 纳米颗粒中 DTC 和残留 PVA 的定量是通过紫外-可见吸收光谱法进行的。根据监管机构对分析方法进行了验证。两条定量分析曲线在重复性(日内)和中间(日间)方面均显示出良好的精密度,并且在检测和定量值较低的情况下也具有良好的准确度。新的纳米结构系统,负载 DTC 的 PLA-NPs,显示出提高稳定性和克服二硫代氨基甲酸酯席夫碱的水溶性问题的优势,旨在潜在的药物递送应用。图形概要 。. 并且在低检测和定量值的情况下也具有良好的准确性。新的纳米结构系统,负载 DTC 的 PLA-NPs,显示出提高稳定性和克服二硫代氨基甲酸酯席夫碱的水溶性问题的优势,旨在潜在的药物递送应用。图形概要 。. 并且在低检测和定量值的情况下也具有良好的准确性。新的纳米结构系统,负载 DTC 的 PLA-NPs,显示出提高稳定性和克服二硫代氨基甲酸酯席夫碱的水溶性问题的优势,旨在潜在的药物递送应用。图形概要 。.
更新日期:2019-10-31
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