School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, Road Araraquara-Jaú, Km 01, 14801-902, Araraquara, São Paulo, Brazil.
Federal Institute of Mato Grosso (IFMT), Cuiabá Campus, Bela Vista, Juliano Costa Marques Avenue, 78050-560, Cuiabá, Mato Grosso, Brazil.
Carbohydr Polym. 2021 Feb 15;254:117444. doi: 10.1016/j.carbpol.2020.117444. Epub 2020 Nov 26.
Nanostructured polyelectrolyte complexes (nano PECs) based on biopolymers are an important technological strategy to target drugs to the action and/or absorption site in a more effective way. In this work, computational studies were performed to predict the ionization, spatial arrangement and interaction energies of chitosan (CS), hyaluronic acid (HA), and hypromellose phthalate (HP), for the design of nano PEC carriers for methotrexate (MTX). The optimal pH range (5.0-5.5) for preparing nano PECs was selected by experimental and computational methodologies, favoring the polymers interactions. CS, HA, HP and MTX addition order was also rationalized, maximizing their interactions and MTX entrapment. Spherical nano-sized particles (256-575 nm, by dynamic light scattering measurement) with positive surface charge (+25.5 to +29.2 mV) were successfully prepared. The MTX association efficiency ranged from 20 to 32 %. XRD analyses evidenced the formation of a new material with an organized structure, in relation to raw polymers.
基于生物聚合物的纳米聚电解质复合物(nano PEC)是一种将药物靶向作用和/或吸收部位的重要技术策略,以更有效的方式。在这项工作中,进行了计算研究,以预测壳聚糖(CS)、透明质酸(HA)和邻苯二甲酸羟丙基甲基纤维素(HP)的电离、空间排列和相互作用能,用于设计甲氨蝶呤(MTX)的 nano PEC 载体。通过实验和计算方法选择了制备 nano PEC 的最佳 pH 范围(5.0-5.5),有利于聚合物相互作用。还合理化了 CS、HA、HP 和 MTX 的添加顺序,最大限度地提高了它们的相互作用和 MTX 包封率。成功制备了具有正表面电荷(+25.5 至+29.2 mV)的球形纳米级颗粒(通过动态光散射测量为 256-575nm)。MTX 结合效率范围为 20 至 32%。XRD 分析表明,与原始聚合物相比,形成了具有有序结构的新材料。