Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.2. Preparation of BSA/ALG Nanoparticles
2.3. Characterization of Nanoparticles
2.3.1. Composition of BSA/AlG Nanoparticles
2.3.2. Thermogravimetric Analysis (TGA)
2.3.3. Determination of Folate-Conjugated to BSA/ALG Nanoparticles
2.3.4. Morphology, Size and Z-Potential of Nanoparticles
2.3.5. Preparation of PTX–Folate-Conjugated Nanoparticles
2.3.6. Estimation of PTX Content
2.3.7. In Vitro Drug Release Studies
2.3.8. Cell Culture Studies
Cellular Uptake of Nanoparticles
Fluorescence Microscopy
Cell Viability
2.4. Statistical Analysis
3. Results
3.1. Preparation of BSA/ALG Nanoparticles
3.1.1. Composition of Nanoparticles
3.1.2. Thermogravimetric Analysis (TGA)
3.1.3. Determination of Folate Conjugated to Nanoparticles
3.2. Characterization of Folate-Conjugated BSA/ALG Nanoparticles
3.2.1. Morphology, Size and Z-Potential of Nanoparticles
3.2.2. Estimation of PTX Content in Folate-Conjugate Nanoparticles
3.2.3. PTX Release from Folate-Conjugated Nanoparticles (Nps–Fol)
3.3. In Vitro Evaluation of Folate-Conjugated Nanoparticles in Tumour Cell Lines
3.3.1. Cellular Uptake of Nanoparticles
3.3.2. Cell Viability
4. Discussion
4.1. Composition, Characterization and PTX Release from Folate-Conjugated Nanoparticles
4.2. In Vitro Evaluation of Folate-Conjugated Nanoparticles in Tumor Cell Lines
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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Nanoparticles | Composition of Blend (w/w Ratio) | BSA Incorporated into Nanoparticles (%) | ALG Incorporated into Nanoparticles (%) | BSA/ALG Ratio in Nanoparticles |
---|---|---|---|---|
30BSA/70ALG | 2BSA:1ALG | 52 ± 4 | 65 ± 5 | 1/1 |
40BSA/60ALG | 3BSA:1ALG | 13 ± 4 | 50 ± 2 | 0.25/1 |
50BSA/50ALG | 5BSA:1ALG | 25 ± 3 | 54 ± 4 | 0.5/1 |
Nanoparticles | Mean Size (nm) | Polydispersity Index | Zeta Potential (mV) |
---|---|---|---|
30BSA/70ALG | 182 ± 82 | 1.4 ± 0.7 | −0.12 ± 0.04 a |
30BSA/70ALG–Fol | 189 ± 81 | 1.7 ± 0.3 | −69.3 ± 0.8 a |
PTX-loaded 30BSA/70ALG–Fol | 290 ± 126 | 1.8 ± 0.4 | −67.3 ± 0.8 a |
50BSA/50ALG | 169 ± 28 | 1.5 ± 0.3 | −0.43 ± 0.06 b |
50BSA/50ALG–Fol | 268 ± 102 | 1.4 ± 0.3 | −66.2± 0.6 bc |
PTX-loaded 50BSA/50ALG–Fol | 296 ± 57 | 1.2 ± 0.4 | −94.1± 0.4 bc |
Drug Content in Nps–Fol | ||
---|---|---|
Nanoparticles | By Extraction with Ethanol (µg PTX/mg Np) | By Tryptic Hydrolysis of the Nanoparticles (µg PTX/mg Np) |
50BSA/50ALG–Fol | 3.56 ± 0.13 a | 3.28 ± 0.24 b |
30BSA/70ALG–Fol | 2.63 ± 0.19 a | 2.42 ± 0.36 b |
Nanoparticles | Release Rate of PTX from Nanoparticle–Fol | |
---|---|---|
First Stage: 0–4 h | Second Stage: 5–27 h | |
50BSA/50ALG–Fol | 0.63 µg PTX/h per mg of Nps–Fol (r2 0.973) | 0.019 µg PTX/h per mg of Nps–Fol (r2 0.935) |
30BSA/70ALG–Fol | 0.43 µg PTX/h per mg of Nps–Fol (r2 0.823) | 0.008 µg PTX/h per mg of Nps–Fol (r2 0.877) |
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Martínez-Relimpio, A.M.; Benito, M.; Pérez-Izquierdo, E.; Teijón, C.; Olmo, R.M.; Blanco, M.D. Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization. Polymers 2021, 13, 2083. https://doi.org/10.3390/polym13132083
Martínez-Relimpio AM, Benito M, Pérez-Izquierdo E, Teijón C, Olmo RM, Blanco MD. Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization. Polymers. 2021; 13(13):2083. https://doi.org/10.3390/polym13132083
Chicago/Turabian StyleMartínez-Relimpio, Ana María, Marta Benito, Elena Pérez-Izquierdo, César Teijón, Rosa María Olmo, and María Dolores Blanco. 2021. "Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization" Polymers 13, no. 13: 2083. https://doi.org/10.3390/polym13132083