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Single step encapsulation process of ivermectin in biocompatible polymer using a supercritical antisolvent system process
Asia-Pacific Journal of Chemical Engineering ( IF 1.4 ) Pub Date : 2021-06-16 , DOI: 10.1002/apj.2672
Osvaldo Valarini Junior 1, 2 , Flavia Aparecida Reitz Cardoso 3 , Guilherme Botelho Meireles Souza 1 , Willyan Machado Giufrida 4 , Lucio Cardozo‐Filho 1, 5
Affiliation  

This paper reports the production of ivermectin (IVM)-encapsulated lecithin/poly (methyl methacrylate) (PMMA) nanoparticles via supercritical antisolvent system (SAS). Of a total of nine formulations, experimental condition R7 containing 10% lecithin relative to polymer (PMMA) resulted in the smallest average experimental particle diameter (dexp), more stable surface charges and high IVM encapsulation efficiency (75.9 ± 2.5%). Nanoparticles were morphologically, thermally, and conformationally characterized using scanning electron microscopy (SEM), thermogravimetric analysis/thermogravimetric derivative (TGA/DTG), and Fourier transform infrared–attenuated total reflectance (FTIR/ATR) techniques. In vitro release test showed that the drug has a controlled release of approximately 110 h. Peppas–Sahlin model (R2 = 0.99) was able to describe the diffusion of the drug correctly. Cytotoxicity analysis showed high compatibility of nanoparticles with epithelial cells, fibroblasts, and macrophages. Population balance equation was used to determine kinetic parameters from experimental data of average particle diameter. Synthesized nanoparticles showed high solution stability, good encapsulation capacity, and showed no adverse effects on cell viability, indicating their high potential as a new IVM carrier system for veterinary medicine and human applications.

中文翻译:

使用超临界抗溶剂系统工艺将伊维菌素一步包封在生物相容性聚合物中

本文报道了通过超临界抗溶剂系统 (SAS) 生产伊维菌素 (IVM) 包裹的卵磷脂/聚甲基丙烯酸甲酯 (PMMA) 纳米颗粒。在总共九种配方中,相对于聚合物 (PMMA) 含有 10% 卵磷脂的实验条件 R7 导致最小的平均实验粒径 (d exp )、更稳定的表面电荷和高 IVM 封装效率 (75.9 ± 2.5%)。使用扫描电子显微镜 (SEM)、热重分析/热重导数 (TGA/DTG) 和傅里叶变换红外衰减全反射 (FTIR/ATR) 技术对纳米颗粒进行形态学、热学和构象表征。体外释放试验表明,该药物的控释时间约为110 h。Peppas-Sahlin 模型 (R 2  = 0.99) 能够正确描述药物的扩散。细胞毒性分析表明,纳米颗粒与上皮细胞、成纤维细胞和巨噬细胞具有高度的相容性。使用群体平衡方程从平均粒径的实验数据确定动力学参数。合成的纳米粒子显示出高溶液稳定性、良好的包封能力,并且对细胞活力没有不利影响,表明它们作为兽医和人类应用的新型 IVM 载体系统具有很高的潜力。
更新日期:2021-06-16
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