Structural Modification of Nanomicelles through Phosphatidylcholine: The Enhanced Drug-Loading Capacity and Anticancer Activity of Celecoxib-Casein Nanoparticles for the Intravenous Delivery of Celecoxib
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.2. Preparation and Structural Modification of Casein Nanoparticles
2.3. Celecoxib Loading of PC-Casein Nanoparticles
2.4. Stability Study of PC-CX-Casein Nanoparticles
2.5. Preparation of CX-β-Casein Nanoparticles
2.6. Characterization of Casein Nanoparticle Dispersions
2.7. Cell Culture
2.8. Cell Viability Assay
2.9. In Vitro Cell Uptake Studies
2.10. Determination of Drug Concentration-Time Curve
2.11. Tumor Inhibition Experiments In Vivo
2.12. Statistical Analysis
3. Results and Discussion
3.1. Structural Modification of Casein Nanoparticles by PC
3.2. The Stability of PC-CX-Casein Nanoparticles
3.3. Resuspension of the Nanoparticles after Lyophilization
3.4. Inhibition on Tumor Cells In Vitro
3.5. In Vitro Cell Uptake of CX
3.6. Pharmacokinetics of NP Formulations with Different Stability
3.7. The Inhibition Effect of CX-PC-casein-NPs on Tumor Growth
4. Conclusions
Author Contributions
Funding
Conflicts of Interest
References
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Nanoparticles. | Mean Diameter (nm) | Polydispersity Index (PDI) | Zeta Potential (mV) | CX in Dispersion (mg/mL) |
---|---|---|---|---|
Fresh nanoparticle dispersion | ||||
CX-casein nanoparticles | 254.4 ± 5.4 | 0.340 ± 0.29 | −44.57 ± 2.11 | 7.3 |
CX-PC-casein-NPs | 192.6 ± 4.3 | 0.175 ± 0.09 | −37.21 ± 1.47 | 8.5 |
Reconstructed nanoparticle dispersion from the corresponding lyophilized powder | ||||
CX-casein nanoparticles | /a | / | / | / |
CX-PC-casein-NPs | 202.4 ± 2.9 | 0.188 ± 0.18 | -36.87 ± 1.77 | 8.4 |
Parameter | Formulation | |
---|---|---|
CX-β-casein-NPs | CX-PC-casein-NPs | |
AUC(0-24) (μg/L h) | 11882.6 ± 1545.6 | 34574.3 ± 7844.9 |
t1/2 (h) | 2.91 ± 0.40 | 4.51 ± 0.37 |
Cmax (μg/L) | 9974.2 ± 2426.3 | 6165.8 ± 1063.5 |
Tmax (h) | 0.5 ± 0 | 1.6 ± 0.5 |
CL (L/h/kg) | 0.42 ± 0.06 | 0.15 ± 0.04 |
Vd (L/kg) | 3.1 ± 1.78 | 0.97 ± 0.29 |
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Xv, L.; Qian, X.; Wang, Y.; Yu, C.; Qin, D.; Zhang, Y.; Jin, P.; Du, Q. Structural Modification of Nanomicelles through Phosphatidylcholine: The Enhanced Drug-Loading Capacity and Anticancer Activity of Celecoxib-Casein Nanoparticles for the Intravenous Delivery of Celecoxib. Nanomaterials 2020, 10, 451. https://doi.org/10.3390/nano10030451
Xv L, Qian X, Wang Y, Yu C, Qin D, Zhang Y, Jin P, Du Q. Structural Modification of Nanomicelles through Phosphatidylcholine: The Enhanced Drug-Loading Capacity and Anticancer Activity of Celecoxib-Casein Nanoparticles for the Intravenous Delivery of Celecoxib. Nanomaterials. 2020; 10(3):451. https://doi.org/10.3390/nano10030451
Chicago/Turabian StyleXv, Liuli, Xinxin Qian, Yan Wang, Chenghuan Yu, Dingkui Qin, Yahui Zhang, Peng Jin, and Qizhen Du. 2020. "Structural Modification of Nanomicelles through Phosphatidylcholine: The Enhanced Drug-Loading Capacity and Anticancer Activity of Celecoxib-Casein Nanoparticles for the Intravenous Delivery of Celecoxib" Nanomaterials 10, no. 3: 451. https://doi.org/10.3390/nano10030451