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PEGylated Chitosan Nanoparticles Encapsulating Ascorbic Acid and Oxaliplatin Exhibit Dramatic Apoptotic Effects against Breast Cancer Cells
: This study aims to design a pH-responsive dual-loaded nanosystem based on PEGylated chitosan nanoparticles loaded with ascorbic acid (AA) and oxaliplatin (OX) for the effective treatment of breast cancer. In this regard, non-PEGylated and PEGylated chitosan nanoparticles (CS NPs) loaded with ei...
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| Autoren: | , , , , , , |
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| Format: | Artikel |
| Sprache: | Englisch |
| Veröffentlicht: |
Philipps-Universität Marburg
2022
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| Schlagworte: | |
| Online Zugang: | PDF-Volltext |
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| Zusammenfassung: | : This study aims to design a pH-responsive dual-loaded nanosystem based on PEGylated
chitosan nanoparticles loaded with ascorbic acid (AA) and oxaliplatin (OX) for the effective treatment
of breast cancer. In this regard, non-PEGylated and PEGylated chitosan nanoparticles (CS NPs) loaded
with either ascorbic acid (AA), oxaliplatin (OX), or dual-loaded with AA-OX were fabricated using the
ionotropic gelation method. The hydrodynamic diameters of the fabricated AA/CS NPs, OX/CS NPs,
and AA-OX/CS NPs were 157.20 ± 2.40, 188.10 ± 9.70, and 261.10 ± 9.19 nm, respectively. While the
hydrodynamic diameters of the designed AA/PEG-CS NPs, OX/PEG-CS NPs, and AA-OX/PEG-CS
NPs were 152.20 ± 2.40, 156.60 ± 4.82, and 176.00 ± 4.21 nm, respectively. The ζ-potential of the
prepared nanoparticles demonstrated high positive surface charges of +22.02 ± 1.50, +22.58 ± 1.85
and +40.4 ± 2.71 mV for AA/CS NPs, OX/CS NPs, and AA-OX/CS NPs, respectively. The ζ-potential
of the PEGylated CS NPs was reduced owing to the shielding of the positive charges by the PEG
chains. Additionally, all the prepared nanoparticles exhibited high entrapment efficiencies (EE%) and
spherical-shaped morphology. The chemical features of the prepared nanoparticles were investigated
using Fourier transform infrared (FTIR) spectroscopy. Release studies showed the capability of the
prepared non-PEGylated and PEGylated chitosan NPs to release their cargo in the acidic environment
of cancer tissue (pH 5.5). Furthermore, the AA/CS NPs, AA/PEG-CS NPs, OX/CS NPs, OX/PEG-CS
NPs, AA-OX/CS NPs and AA-OX/PEG-CS NPs exhibited remarkable cytotoxic activities against
breast adenocarcinoma (MCF-7) cells with IC50 values of 44.87 ± 11.49, 23.3 ± 3.73, 23.88 ± 6.29,
17.98 ± 3.99, 18.69 ± 2.22, and 7.5 ± 0.69 µg/mL, respectively; as compared to free AA and OX
(IC50 of 150.80 ± 26.50 and 147.70 ± 63.91 µg/mL, respectively). Additionally, treatment of MCF-7
cells with IC50 concentrations of AA, AA/CS NPs, AA/PEG-CS NPs, OX, OX/CS NPs, OX/PEG-CS
NPs, AA-OX/CS NPs or AA-OX/PEG-CS NPs increased the percentages of early apoptotic cells
to 5.28%, 9.53%, 11.20%, 5.27%, 13.80%, 8.43%, 2.32%, and 10.10%, respectively, and increased the
percentages of late apoptotic cells to 0.98%, 0.37%, 2.41%, 2.06%, 0.97%, 9.66%, 56%, and 81.50%,
respectively. These results clearly indicate that PEGylation enhances the apoptotic effect of AA
and OX alone, in addition to potentiating the apoptotic effect of AA and OX when combined on
MCF-7 cells. In conclusion, PEGylated chitosan nanoparticles encapsulating AA, OX, or AA and OX
represent an effective formula for induction of apoptosis in MCF-7 cells. |
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| Beschreibung: | Gefördert durch den Open-Access-Publikationsfonds der UB Marburg. |
| Umfang: | 18 Seiten |
| DOI: | 10.3390/pharmaceutics14020407 |