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Self-Assembly of Zein-Based Microcarrier System for Colon-Targeted Oral Drug Delivery

Wang, Hongdi, Zhang, Xiaotong, Zhu, Wei, Jiang, Yanbin, Zhang, Zhibing
Industrial & engineering chemistry process design and development 2018 v.57 no.38 pp. 12689-12699
coatings, microparticles, ultrasonics, indomethacin, process design, chemical interactions, mechanical properties, hydrophobicity, zein, solubility, oral administration, dialysis
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.