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用于亲脂性药物的喷雾干燥聚合物微球:制剂设计、理化特性及体外释放评价

Spray-Dried Polymeric Microspheres for Lipophilic Drugs: Formulation Design, Physicochemical Characterization, and In Vitro Release Evaluation.

作者信息

Nataren-Rodríguez Felipe, Pacheco-Molina Jorge, Gracia-Vásquez Sandra Leticia, Balderas-Rentería Isaías, Ramírez-Cabrera Mónica A, Arredondo-Espinoza Eder, Santamaría Karla J, González-Barranco Patricia

机构信息

Facultad de Ciencias Químicas, Universidad Autónoma de Nuevo León, Av Universidad S/N, Cd. Universitaria, San Nicolas de los Garza 66455, Nuevo León, Mexico.

Facultad de Farmacia, Universidad de Costa Rica, Sede Rodrigo Facio, Montes de Oca, San Pedro 11501-2060, San José, Costa Rica.

出版信息

Pharmaceuticals (Basel). 2025 Jul 9;18(7):1020. doi: 10.3390/ph18071020.

Abstract

: The formulation of microspheres for lipophilic drugs using aqueous methods, such as spray drying, faces significant challenges. The main objective of this study was to evaluate the effect of the process parameters and polymer selection on the production of microspheres by spray drying for a lipophilic drug. : Lipophilic drug-loaded microspheres were developed using various polymers via the aqueous spray drying method. The effects of the factors on the yield percentage and encapsulation efficiency were analyzed. Microspheres preparation included inulin, guar gum, hydroxypropyl methylcellulose, and Eudragit S100. A 2 factorial design was performed, and the parameters were optimized. : Inlet temperature, feed flow, and polymer percentage showed a significant effect ( < 0.05) on the yield percentage of guar gum microspheres and encapsulation efficiency of the inulin microspheres. Inulin and guar gum microspheres showed the best yield percentage (75.41%) and encapsulation efficiency (100%), respectively. In addition, guar gum microspheres had the best morphology, and hydroxypropyl methylcellulose microspheres were smaller and had an irregular surface. Eudragit did not maintain its delayed release property due to limitations of the aqueous method; inulin released the drug immediately, and guar gum and hydroxypropyl methylcellulose microspheres prolonged release only by a few additional hours. : The experimental design showed that optimizing the parameters (inlet temperature, feed flow, and the type and percentage of polymer) can regulate the microsphere development process to obtain improved product yield and encapsulation efficiency results.

摘要

采用诸如喷雾干燥等水性方法制备亲脂性药物微球面临重大挑战。本研究的主要目的是评估工艺参数和聚合物选择对通过喷雾干燥制备亲脂性药物微球的影响。

通过水性喷雾干燥法使用各种聚合物制备了载亲脂性药物的微球。分析了各因素对产率百分比和包封率的影响。微球制备中使用了菊粉、瓜尔胶、羟丙基甲基纤维素和尤特奇S100。进行了二因素设计并对参数进行了优化。

入口温度、进料流速和聚合物百分比对瓜尔胶微球的产率百分比和菊粉微球的包封率有显著影响(<0.05)。菊粉和瓜尔胶微球分别表现出最佳的产率百分比(75.41%)和包封率(100%)。此外,瓜尔胶微球具有最佳的形态,羟丙基甲基纤维素微球较小且表面不规则。由于水性方法的局限性,尤特奇未能保持其缓释性能;菊粉微球立即释放药物,瓜尔胶和羟丙基甲基纤维素微球仅将释放延长了几个小时。

实验设计表明,优化参数(入口温度、进料流速以及聚合物的类型和百分比)可以调节微球的制备过程,以获得更高的产品产率和包封率结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9106/12299377/c82312b17091/pharmaceuticals-18-01020-g001.jpg

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