Crosslinked Fibroin Nanoparticles: Investigations on Biostability, Cytotoxicity, and Cellular Internalization
Recently, crosslinked fibroin nanoparticles (FNP) using the crosslinker 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) or the polymer poly(ethylenimine) (PEI) have been developed and showed potentials as novel drug delivery systems. Thus, this study further investigated the biolo...
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| Format: | Article |
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MDPI AG
2020-04-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/13/5/86 |
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| author | Duy Toan Pham Nuttawut Saelim Raphaël Cornu Arnaud Béduneau Waree Tiyaboonchai |
| author_facet | Duy Toan Pham Nuttawut Saelim Raphaël Cornu Arnaud Béduneau Waree Tiyaboonchai |
| author_sort | Duy Toan Pham |
| collection | DOAJ |
| description | Recently, crosslinked fibroin nanoparticles (FNP) using the crosslinker 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) or the polymer poly(ethylenimine) (PEI) have been developed and showed potentials as novel drug delivery systems. Thus, this study further investigated the biological properties of these crosslinked FNP by labeling them with fluorescein isothiocyanate (FITC) for in vitro studies. All formulations possessed a mean particle size of approximately 300 nm and a tunable zeta potential (−20 to + 30 mV) dependent on the amount/type of crosslinkers. The FITC-bound FNP showed no significant difference in physical properties compared to the blank FNP. They possessed a binding efficacy of 3.3% <i>w</i>/<i>w</i>, and no FITC was released in sink condition up to 8 h. All formulations were colloidal stable in the sheep whole blood. The degradation rate of these FNP in blood could be controlled depending on their crosslink degree. Moreover, no potential toxicity in erythrocytes, Caco-2, HepG2, and 9L cells was noted for all formulations at particle concentrations of < 1 mg/mL. Finally, all FNP were internalized into the Caco-2 cells after 3 h incubation. The uptake rate of the positively charged particles was significantly higher than the negatively charged ones. In summary, the crosslinked FNP were safe and showed high potentials as versatile systems for biomedical applications. |
| first_indexed | 2024-03-10T20:07:59Z |
| format | Article |
| id | doaj.art-efdb71a1d50f46d6baa7ce22888c95c8 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T20:07:59Z |
| publishDate | 2020-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-efdb71a1d50f46d6baa7ce22888c95c82023-11-19T23:11:11ZengMDPI AGPharmaceuticals1424-82472020-04-011358610.3390/ph13050086Crosslinked Fibroin Nanoparticles: Investigations on Biostability, Cytotoxicity, and Cellular InternalizationDuy Toan Pham0Nuttawut Saelim1Raphaël Cornu2Arnaud Béduneau3Waree Tiyaboonchai4Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok 65000, ThailandFaculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok 65000, ThailandPEPITE EA4267, Univ. Bourgogne Franche-Comté, F-25000 Besançon, FrancePEPITE EA4267, Univ. Bourgogne Franche-Comté, F-25000 Besançon, FranceFaculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok 65000, ThailandRecently, crosslinked fibroin nanoparticles (FNP) using the crosslinker 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) or the polymer poly(ethylenimine) (PEI) have been developed and showed potentials as novel drug delivery systems. Thus, this study further investigated the biological properties of these crosslinked FNP by labeling them with fluorescein isothiocyanate (FITC) for in vitro studies. All formulations possessed a mean particle size of approximately 300 nm and a tunable zeta potential (−20 to + 30 mV) dependent on the amount/type of crosslinkers. The FITC-bound FNP showed no significant difference in physical properties compared to the blank FNP. They possessed a binding efficacy of 3.3% <i>w</i>/<i>w</i>, and no FITC was released in sink condition up to 8 h. All formulations were colloidal stable in the sheep whole blood. The degradation rate of these FNP in blood could be controlled depending on their crosslink degree. Moreover, no potential toxicity in erythrocytes, Caco-2, HepG2, and 9L cells was noted for all formulations at particle concentrations of < 1 mg/mL. Finally, all FNP were internalized into the Caco-2 cells after 3 h incubation. The uptake rate of the positively charged particles was significantly higher than the negatively charged ones. In summary, the crosslinked FNP were safe and showed high potentials as versatile systems for biomedical applications.https://www.mdpi.com/1424-8247/13/5/86fibroinnanoparticlescrosslinkcellular uptakebiostability |
| spellingShingle | Duy Toan Pham Nuttawut Saelim Raphaël Cornu Arnaud Béduneau Waree Tiyaboonchai Crosslinked Fibroin Nanoparticles: Investigations on Biostability, Cytotoxicity, and Cellular Internalization Pharmaceuticals fibroin nanoparticles crosslink cellular uptake biostability |
| title | Crosslinked Fibroin Nanoparticles: Investigations on Biostability, Cytotoxicity, and Cellular Internalization |
| title_full | Crosslinked Fibroin Nanoparticles: Investigations on Biostability, Cytotoxicity, and Cellular Internalization |
| title_fullStr | Crosslinked Fibroin Nanoparticles: Investigations on Biostability, Cytotoxicity, and Cellular Internalization |
| title_full_unstemmed | Crosslinked Fibroin Nanoparticles: Investigations on Biostability, Cytotoxicity, and Cellular Internalization |
| title_short | Crosslinked Fibroin Nanoparticles: Investigations on Biostability, Cytotoxicity, and Cellular Internalization |
| title_sort | crosslinked fibroin nanoparticles investigations on biostability cytotoxicity and cellular internalization |
| topic | fibroin nanoparticles crosslink cellular uptake biostability |
| url | https://www.mdpi.com/1424-8247/13/5/86 |
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