Structural Modification of Nanomicelles through Phosphatidylcholine: The Enhanced Drug-Loading Capacity and Anticancer Activity of Celecoxib-Casein Nanoparticles for the Intravenous Delivery of Celecoxib
| Autor: | Yan Wang, Yahui Zhang, Qizhen Du, Xinxin Qian, Dingkui Qin, Peng Jin, Chenghuan Yu, Liuli Xv |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Drug
General Chemical Engineering media_common.quotation_subject Nanoparticle 02 engineering and technology Pharmacology anticancer Article lcsh:Chemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Pharmacokinetics Casein Phosphatidylcholine medicine General Materials Science media_common celecoxib Chemistry stability 021001 nanoscience & nanotechnology Paclitaxel lcsh:QD1-999 030220 oncology & carcinogenesis Celecoxib casein nanoparticles delivery 0210 nano-technology Intracellular medicine.drug |
| Zdroj: | Nanomaterials Volume 10 Issue 3 Nanomaterials, Vol 10, Iss 3, p 451 (2020) |
| ISSN: | 2079-4991 |
| DOI: | 10.3390/nano10030451 |
| Popis: | This study aims to stabilize loaded celecoxib (CX) by modifying the structure of casein nanoparticles through phosphatidylcholine. The results show that Egg yolk phosphatidylcholine PC98T (PC) significantly increased the stability of CX-PC-casein nanoparticles (NPs) (192.6 nm) from 5 min (CX-&beta casein-NPs) to 2.5 h at 37 ° C. In addition, the resuspended freeze-dried NPs (202.4 nm) remained stable for 2.5 h. Scanning electron microscopy indicated that PC may block the micropore structures in nanoparticles by ultrasonic treatment and hence improve the physicochemical stability of CX-PC-casein-NPs. The stability of the NPs was positively correlated with their inhibiting ability for human malignant melanoma A375 cells. The structural modification of CX-PC-casein-NPs resulted in an increased intracellular uptake of CX by 2.4 times than that of the unmodified ones. The pharmacokinetic study showed that the Area Under Curve (AUC) of the CX-PC-casein-NPs was 2.9-fold higher in rats than that of the original casein nanoparticles. When CX-PC-casein-NPs were intravenously administrated to mice implanted with A375 tumors (CX dose = 16 mg/kg bodyweight), the tumor inhibition rate reached 56.2%, which was comparable to that of paclitaxel (57.3%) at a dose of 4 mg/kg bodyweight. Our results confirm that the structural modification of CX-PC-casein-NPs can effectively prolong the remaining time of specific drugs, and may provide a potential strategy for cancer treatment. |
| Databáze: | OpenAIRE |
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