Influence of an Antioxidant Nanomaterial on Oral Tablet Formulation: Flow Properties and Critical Quality Attributes
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. Th...
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| Format: | Article |
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MDPI AG
2025-07-01
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| Series: | Antioxidants |
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| Online Access: | https://www.mdpi.com/2076-3921/14/7/829 |
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| author | Andrea C. Ortiz Javiera Carrasco-Rojas Sofía Peñaloza Mario J. Simirgiotis Lorena Rubio-Quiroz Diego Ruiz Carlos F. Lagos Javier Morales Francisco Arriagada |
| author_facet | Andrea C. Ortiz Javiera Carrasco-Rojas Sofía Peñaloza Mario J. Simirgiotis Lorena Rubio-Quiroz Diego Ruiz Carlos F. Lagos Javier Morales Francisco Arriagada |
| author_sort | Andrea C. Ortiz |
| collection | DOAJ |
| description | 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<sup>●</sup>, ABTS<sup>●+</sup>, 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. |
| format | Article |
| id | doaj-art-df33607039dc4c17bb47a305a2801bb2 |
| institution | DOAJ |
| issn | 2076-3921 |
| language | English |
| publishDate | 2025-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Antioxidants |
| spelling | doaj-art-df33607039dc4c17bb47a305a2801bb22025-08-20T03:13:39ZengMDPI AGAntioxidants2076-39212025-07-0114782910.3390/antiox14070829Influence of an Antioxidant Nanomaterial on Oral Tablet Formulation: Flow Properties and Critical Quality AttributesAndrea C. Ortiz0Javiera Carrasco-Rojas1Sofía Peñaloza2Mario J. Simirgiotis3Lorena Rubio-Quiroz4Diego Ruiz5Carlos F. Lagos6Javier Morales7Francisco Arriagada8Escuela de Química y Farmacia, Facultad de Ciencias, Universidad San Sebastián, Santiago 7510157, ChileDepartamento de Ciencias y Tecnología Farmacéutica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago 8380494, ChileDepartamento de Ciencias y Tecnología Farmacéutica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago 8380494, ChileInstituto de Farmacia, Facultad de Ciencias, Universidad Austral de Chile, Campus Isla Teja, Valdivia 5090000, ChileChemical Biology & Drug Discovery Lab, Escuela de Química y Farmacia, Facultad de Ciencias, Universidad San Sebastián, Campus Los Leones, Lota 2465 Providencia, Santiago 7510157, ChileInstituto de Farmacia, Facultad de Ciencias, Universidad Austral de Chile, Campus Isla Teja, Valdivia 5090000, ChileChemical Biology & Drug Discovery Lab, Escuela de Química y Farmacia, Facultad de Ciencias, Universidad San Sebastián, Campus Los Leones, Lota 2465 Providencia, Santiago 7510157, ChileDepartamento de Ciencias y Tecnología Farmacéutica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago 8380494, ChileDepartamento de Ciencias y Tecnología Farmacéutica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago 8380494, ChileAntioxidant 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<sup>●</sup>, ABTS<sup>●+</sup>, 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.https://www.mdpi.com/2076-3921/14/7/829antioxidant nanomaterialnanoantioxidantmesoporous silica nanoparticlescaffeic acidpowder flow propertiesantioxidant tablets |
| spellingShingle | Andrea C. Ortiz Javiera Carrasco-Rojas Sofía Peñaloza Mario J. Simirgiotis Lorena Rubio-Quiroz Diego Ruiz Carlos F. Lagos Javier Morales Francisco Arriagada Influence of an Antioxidant Nanomaterial on Oral Tablet Formulation: Flow Properties and Critical Quality Attributes Antioxidants antioxidant nanomaterial nanoantioxidant mesoporous silica nanoparticles caffeic acid powder flow properties antioxidant tablets |
| title | Influence of an Antioxidant Nanomaterial on Oral Tablet Formulation: Flow Properties and Critical Quality Attributes |
| title_full | Influence of an Antioxidant Nanomaterial on Oral Tablet Formulation: Flow Properties and Critical Quality Attributes |
| title_fullStr | Influence of an Antioxidant Nanomaterial on Oral Tablet Formulation: Flow Properties and Critical Quality Attributes |
| title_full_unstemmed | Influence of an Antioxidant Nanomaterial on Oral Tablet Formulation: Flow Properties and Critical Quality Attributes |
| title_short | Influence of an Antioxidant Nanomaterial on Oral Tablet Formulation: Flow Properties and Critical Quality Attributes |
| title_sort | influence of an antioxidant nanomaterial on oral tablet formulation flow properties and critical quality attributes |
| topic | antioxidant nanomaterial nanoantioxidant mesoporous silica nanoparticles caffeic acid powder flow properties antioxidant tablets |
| url | https://www.mdpi.com/2076-3921/14/7/829 |
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