Self-Assembly of Zein-Based Microcarrier System for Colon-Targeted Oral Drug Delivery,Industrial & Engineering Chemistry Research

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Self-Assembly of Zein-Based Microcarrier System for Colon-Targeted Oral Drug Delivery
Industrial & Engineering Chemistry Research ( IF 3.8 ) Pub Date : 2018-09-18 , DOI: 10.1021/acs.iecr.8b02092
Hongdi Wang _{1,

2} , Xiaotong Zhang ₁ , Wei Zhu ₂ , Yanbin Jiang ₂ , Zhibing Zhang ₁

Affiliation

The advances in pharmaceutical technology allow for the development of various region-selective delivery systems for oral administration to optimize local and systemic therapy. In this paper, micronization associated with a polymorph modification approach was proposed for improving the solubility of hydrophobic drugs for developing a Zein-based colon-targeted delivery system. A microcarrier based on self-assembled structures of Zein was fabricated via a built-in ultrasonic dialysis process, which displayed high payload of a model drug, indomethacin (Indo), with its optimal crystal form. The possible self-assembly mechanism of Zein/Indo forming porous structure in the ultrasonic dialysis process was attributed to the results of intra- and/or intermolecular interactions between Zein and Indo. The designed microspheres, Zein-Indo@PDA, with a surface coating of polydopamine (PDA) not only rendered them enhanced stability and mechanical resistance but also hindered the premature drug release at undesired sites. This innovative formulation design may offer better chances of colon-targeted release.

中文翻译：

基于玉米蛋白的微载体系统的自组装，用于结肠靶向口服药物递送

制药技术的进步允许开发用于口服给药的各种区域选择性递送系统，以优化局部和全身治疗。在本文中，提出了与多晶型物修饰方法相关的微粉化方法，以提高疏水性药物的溶解度，从而开发出基于玉米醇溶蛋白的结肠靶向递送系统。通过内置的超声渗析工艺制造了基于玉米醇溶蛋白自组装结构的微载体，该载体显示出模型药物吲哚美辛（Indo）的高有效负载量，并具有最佳的晶型。Zein / Indo在超声波渗析过程中形成多孔结构的可能的自组装机制归因于Zein与Indo之间的分子内和/或分子间相互作用。设计的微球Zein-Indo @ PDA，聚多巴胺（PDA）的表面涂层不仅使它们具有更高的稳定性和机械耐受性，而且还阻碍了药物在不良部位的过早释放。这种创新的配方设计可以为结肠靶向释放提供更好的机会。

更新日期：2018-09-18

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