The purpose of this study was to apply the quality-by-design (QbD) approach for the development of colon-targeted curcumin-loaded polymeric microparticles (Col-CUR-MPs). The proportion of the enterosoluble polymer (Eudragit^® FS) in the polymeric matrix, curcumin concentration, and the concentration of the polymer mixture (Eudragit^® FS-polycaprolactone) were identified as potential risk factors for the quality of the final product following risk assessment. The influence of these variables on the critical quality attributes (CQAs) of Col-CUR-MPs was investigated. Therefore, a central composite face experimental design was used in order to determine the functional relationships between variables and product CQAs. The obtained regression model and contour plots were used to establish the design space. Finally, the model was validated by preparing two microparticulate formulations, one corresponding to the robust setpoint from within the design space and one outside the established design space, and calculating the percentage bias between the experimental and predicted values. The in vivo study, which was conducted on a fluorescein-loaded formulation that corresponded to the robust setpoint determined by QbD and that contained a mixture of polycaprolactone and Eudragit^® FS (60:40, w/w), confirmed the colon-targeting qualities of this formulation.

中文翻译：

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通过设计质量法研究姜黄素负载的聚合物微粒口服药物递送系统对结肠的靶向作用

这项研究的目的是将按设计质量（QbD）方法应用于结肠靶向姜黄素负载的聚合物微粒（Col-CUR-MPs）的开发。所述肠溶聚合物的比例（尤特奇^® FS）在聚合物基质中，姜黄素浓度，聚合物混合物的浓度（尤特奇^®经风险评估后，FS-聚己内酯被确定为最终产品质量的潜在风险因素。研究了这些变量对Col-CUR-MP的关键质量属性（CQA）的影响。因此，为了确定变量和产品CQA之间的功能关系，使用了中央复合面实验设计。使用获得的回归模型和等高线图来建立设计空间。最后，通过准备两种微粒配方来验证模型，其中一种配方对应于设计空间内的鲁棒设定点，另一种对应既定设计空间外的鲁棒设定点，并计算实验值与预测值之间的百分比偏差。体内研究^® FS（60:40，重量/重量），证实了这一制剂的结肠靶向的品质。