In the present research, we have investigated a drug delivery system based on the pH‐responsive behaviors of zein colloidal nanoparticles coated with sodium caseinate (SC) and poly ethylene imine (PEI). These systematically designed nanoparticles were used as nanocarriers for encapsulation of ellipticine (EPT), as an anticancer drug. SC and PEI coatings were applied through electrostatic adsorption, leading to the increased size and improved polydispersity index of nanoparticles as well as sustained release of drug. Physicochemical characteristics such as hydrodynamic diameter, size distribution, zeta potential and morphology of nanoparticles prepared using different formulations and conditions were also determined. Based on the results, EPT was encapsulated into the prepared nanoparticles with a high drug loading capacity (5.06%) and encapsulation efficiency (94.8%) under optimal conditions. in vitro experiments demonstrated that the release of EPT from zein‐based nanoparticles was pH sensitive. When the pH level decreased from 7.4 to 5.5, the rate of drug release was considerably enhanced. The mechanism of pH‐responsive complexation in the drug encapsulation and release processes was extensively investigated. The pH‐dependent electrostatic interactions and drug state were hypothesized to affect the release profiles. Compared to the EPT‐loaded zein/PEI nanoparticles, the EPT‐loaded zein/SC nanoparticles exhibited a better drug sustained‐release profile, with a smaller initial burst release and longer release period. According to the results of in vitro cytotoxicity experiments, drug‐free nanoparticles were associated with a negligible cytotoxicity, whereas the EPT‐loaded nanoparticles displayed a high toxicity for the cancer cell line, A549. Our findings indicate that these pH‐sensitive protein‐based nanoparticles can be used as novel nanotherapeutic tools and potential antineoplastic drug carriers for cancer chemotherapy with controlled release.

中文翻译：

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刺激响应的玉米醇溶蛋白纳米颗粒作为玫瑰树碱的潜在载体：合成，释放和体外递送

在本研究中，我们基于酪蛋白酸钠（SC）和聚乙烯亚胺（PEI）包覆的玉米醇溶蛋白胶体纳米颗粒的pH响应行为研究了一种药物递送系统。这些系统设计的纳米粒子被用作玫瑰树碱（EPT）封装的纳米载体，作为一种抗癌药物。SC和PEI涂层通过静电吸附进行涂覆，从而导致纳米颗粒的尺寸增加，多分散指数提高以及药物的持续释放。还确定了使用不同配方和条件制备的纳米颗粒的理化特性，例如流体动力学直径，尺寸分布，ζ电位和形态。根据结果​​，将EPT封装到制备的具有高载药量的纳米颗粒中（5。最佳条件下的封装效率（06％）和封装效率（94.8％）。体外实验表明，玉米醇溶蛋白基纳米粒中EPT的释放对pH敏感。当pH值从7.4降低到5.5时，药物释放速率大大提高。pH响应络合在药物封装和释放过程中的机制已得到广泛研究。假设pH依赖的静电相互作用和药物状态会影响释放曲线。与EPT加载的玉米醇溶蛋白/ PEI纳米颗粒相比，EPT加载的玉米醇溶蛋白/ SC纳米颗粒表现出更好的药物缓释特性，初始爆发释放较小，释放时间更长。根据体外细胞毒性实验的结果，不含药物的纳米颗粒与可忽略的细胞毒性有关，负载EPT的纳米颗粒对癌细胞系A549表现出高毒性。我们的发现表明，这些基于pH敏感蛋白的纳米颗粒可以用作新型纳米治疗工具和潜在的抗肿瘤药物载体，用于控释的癌症化疗。