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一种抗氧化纳米材料对口腔片剂制剂的影响:流动性质和关键质量属性

Influence of an Antioxidant Nanomaterial on Oral Tablet Formulation: Flow Properties and Critical Quality Attributes.

作者信息

Ortiz Andrea C, Carrasco-Rojas Javiera, Peñaloza Sofía, Simirgiotis Mario J, Rubio-Quiroz Lorena, Ruiz Diego, Lagos Carlos F, Morales Javier, Arriagada Francisco

机构信息

Escuela de Química y Farmacia, Facultad de Ciencias, Universidad San Sebastián, Santiago 7510157, Chile.

Departamento de Ciencias y Tecnología Farmacéutica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago 8380494, Chile.

出版信息

Antioxidants (Basel). 2025 Jul 5;14(7):829. doi: 10.3390/antiox14070829.

Abstract

Antioxidant nanomaterials, particularly mesoporous silica nanoparticles (MSNs) functionalized with polyphenols, offer innovative solutions for protecting oxidation-sensitive components and enhancing bioavailability in pharmaceuticals or extending the shelf life of nutraceutical and food products. This study investigates the influence of MSNs functionalized with caffeic acid (MSN-CAF) on powder flow properties and their tableting performance. Aminated MSNs were synthesized via co-condensation and conjugated with caffeic acid using EDC/NHS chemistry. Antioxidant capacity was evaluated using DPPH, ABTS, ORAC, and FRAP assays. Powder blends with varying MSN-CAF concentrations (10-70%) were characterized for flow properties (angle of repose, Hausner ratio, Carr's index), tablets were produced via direct compression, and critical quality attributes (weight uniformity, hardness, friability, disintegration, nanoparticle release) were assessed. MSN-CAF exhibited reduced antioxidant capacity compared with free caffeic acid due to pore entrapment but retained significant activity. Formulation F1 (10% MSN-CAF) showed excellent flowability (angle of repose: 12°, Hausner ratio: 1.16, Carr's index: 14%), enabling robust tablet production with rapid disintegration, low friability, and complete nanoparticle release in 10 min. Additionally, the antioxidant nanomaterial demonstrated biocompatibility with the HepG2 cell line. MSN-CAF is a versatile nanoexcipient for direct compression tablets, offering potential as an active packaging agent and delivery system in the nutraceutical and food industries.

摘要

抗氧化纳米材料,特别是用多酚功能化的介孔二氧化硅纳米颗粒(MSN),为保护对氧化敏感的成分、提高药物的生物利用度或延长营养保健品和食品的保质期提供了创新解决方案。本研究考察了用咖啡酸功能化的MSN(MSN-CAF)对粉末流动性及其压片性能的影响。通过共缩合合成胺化MSN,并使用EDC/NHS化学方法与咖啡酸共轭。使用DPPH、ABTS、ORAC和FRAP测定法评估抗氧化能力。对具有不同MSN-CAF浓度(10-70%)的粉末混合物进行流动性表征(休止角、豪斯纳比、卡尔指数),通过直接压片制备片剂,并评估关键质量属性(重量均匀度、硬度、脆碎度、崩解度、纳米颗粒释放)。由于孔包封,MSN-CAF与游离咖啡酸相比抗氧化能力降低,但仍保留显著活性。配方F1(10% MSN-CAF)表现出优异的流动性(休止角:12°,豪斯纳比:1.16,卡尔指数:14%),能够生产出具有快速崩解、低脆碎度且在10分钟内纳米颗粒完全释放的坚固片剂。此外,这种抗氧化纳米材料对HepG2细胞系具有生物相容性。MSN-CAF是一种用于直接压片的通用纳米辅料,在营养保健品和食品工业中具有作为活性包装剂和递送系统的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0cba/12291767/f7adee45d877/antioxidants-14-00829-g001.jpg

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