Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical Cancer Cells
Quercetin is a natural flavonoid with high anticancer activity, especially for related-HPV cancers such as cervical cancer. However, quercetin exhibits a reduced aqueous solubility and stability, resulting in a low bioavailability that limits its therapeutic use. In this study, chitosan/sulfonyl-eth...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-03-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/3/936 |
| _version_ | 1797609484902727680 |
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| author | Miguel Ferreira Diana Gomes Miguel Neto Luís A. Passarinha Diana Costa Ângela Sousa |
| author_facet | Miguel Ferreira Diana Gomes Miguel Neto Luís A. Passarinha Diana Costa Ângela Sousa |
| author_sort | Miguel Ferreira |
| collection | DOAJ |
| description | Quercetin is a natural flavonoid with high anticancer activity, especially for related-HPV cancers such as cervical cancer. However, quercetin exhibits a reduced aqueous solubility and stability, resulting in a low bioavailability that limits its therapeutic use. In this study, chitosan/sulfonyl-ether-β-cyclodextrin (SBE-β-CD)-conjugated delivery systems have been explored in order to increase quercetin loading capacity, carriage, solubility and consequently bioavailability in cervical cancer cells. SBE-β-CD/quercetin inclusion complexes were tested as well as chitosan/SBE-β-CD/quercetin-conjugated delivery systems, using two types of chitosan differing in molecular weight. Regarding characterization studies, HMW chitosan/SBE-β-CD/quercetin formulations have demonstrated the best results, which are obtaining nanoparticle sizes of 272.07 ± 2.87 nm, a polydispersity index (PdI) of 0.287 ± 0.011, a zeta potential of +38.0 ± 1.34 mV and an encapsulation efficiency of approximately 99.9%. In vitro release studies were also performed for 5 kDa chitosan formulations, indicating a quercetin release of 9.6% and 57.53% at pH 7.4 and 5.8, respectively. IC<sub>50</sub> values on HeLa cells indicated an increased cytotoxic effect with HMW chitosan/SBE-β-CD/quercetin delivery systems (43.55 μM), suggesting a remarkable improvement of quercetin bioavailability. |
| first_indexed | 2024-03-11T06:02:00Z |
| format | Article |
| id | doaj.art-3e9b67b91f0f4b579c80f543193e7748 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T06:02:00Z |
| publishDate | 2023-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-3e9b67b91f0f4b579c80f543193e77482023-11-17T13:16:29ZengMDPI AGPharmaceutics1999-49232023-03-0115393610.3390/pharmaceutics15030936Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical Cancer CellsMiguel Ferreira0Diana Gomes1Miguel Neto2Luís A. Passarinha3Diana Costa4Ângela Sousa5CICS-UBI—Health Science Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalCICS-UBI—Health Science Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalCICS-UBI—Health Science Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalCICS-UBI—Health Science Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalCICS-UBI—Health Science Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalCICS-UBI—Health Science Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, PortugalQuercetin is a natural flavonoid with high anticancer activity, especially for related-HPV cancers such as cervical cancer. However, quercetin exhibits a reduced aqueous solubility and stability, resulting in a low bioavailability that limits its therapeutic use. In this study, chitosan/sulfonyl-ether-β-cyclodextrin (SBE-β-CD)-conjugated delivery systems have been explored in order to increase quercetin loading capacity, carriage, solubility and consequently bioavailability in cervical cancer cells. SBE-β-CD/quercetin inclusion complexes were tested as well as chitosan/SBE-β-CD/quercetin-conjugated delivery systems, using two types of chitosan differing in molecular weight. Regarding characterization studies, HMW chitosan/SBE-β-CD/quercetin formulations have demonstrated the best results, which are obtaining nanoparticle sizes of 272.07 ± 2.87 nm, a polydispersity index (PdI) of 0.287 ± 0.011, a zeta potential of +38.0 ± 1.34 mV and an encapsulation efficiency of approximately 99.9%. In vitro release studies were also performed for 5 kDa chitosan formulations, indicating a quercetin release of 9.6% and 57.53% at pH 7.4 and 5.8, respectively. IC<sub>50</sub> values on HeLa cells indicated an increased cytotoxic effect with HMW chitosan/SBE-β-CD/quercetin delivery systems (43.55 μM), suggesting a remarkable improvement of quercetin bioavailability.https://www.mdpi.com/1999-4923/15/3/936chitosancyclodextrindelivery systemsinclusion complexquercetin |
| spellingShingle | Miguel Ferreira Diana Gomes Miguel Neto Luís A. Passarinha Diana Costa Ângela Sousa Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical Cancer Cells Pharmaceutics chitosan cyclodextrin delivery systems inclusion complex quercetin |
| title | Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical Cancer Cells |
| title_full | Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical Cancer Cells |
| title_fullStr | Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical Cancer Cells |
| title_full_unstemmed | Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical Cancer Cells |
| title_short | Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical Cancer Cells |
| title_sort | development and characterization of quercetin loaded delivery systems for increasing its bioavailability in cervical cancer cells |
| topic | chitosan cyclodextrin delivery systems inclusion complex quercetin |
| url | https://www.mdpi.com/1999-4923/15/3/936 |
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