Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical Cancer Cells

Abstract

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. IC50 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.

Anti-cervical cancer mechanism of bioactive compounds from Alangium platanifolium based on the ‘compound-target-disease’ network

“…Active ingredients with a high degree in the C-T-P network were quercetin, methylprednisolone, and caudatin. Quercetin is a flavonoid widely present in natural products and has pronounced anticancer effects, especially against HPV-related cancers such as CC [ 60 ]. It has been reported to promote apoptosis in HeLa cells by inducing the tumor endoplasmic reticulum stress (ERS) pathway [ 61 ].…”

The Commonly Used Stabilizers for Phytochemical-Based Nanoparticles: Stabilization Effects, Mechanisms, and Applications

“…CS and sulfonyl-ether-β-cyclodextrin-conjugated quercetin NPs have the potential as an effective anti-cancer approach for cervical cancer cells [ 104 ]. In that study, an in vitro cell viability assay was conducted to investigate the effects of this NP delivery system on HeLa cells.…”

A Potential Effect of Circadian Rhythm in the Delivery/Therapeutic Performance of Paclitaxel–Dendrimer Nanosystems

“…To evaluate the cytotoxicity of free PTX and the G4-PTX-R8 dendrimer on HeLa, an MTT assay was performed. HeLa cells were seeded at a density of 5 × 10 3 cells/well in 96-well plates, and the day before the experiments, the culture medium was changed to DMEM-F12 supplemented with 10% FBS without antibiotics to enhance the cellular uptake [34,35].…”