article · Pharmaceuticals
Hesperidin is a therapeutic flavonoid with demonstrated antioxidant and antitumor potential, but its practical application is restricted by poor solubility and low bioavailability. To overcome these limitations, chitosan and hesperidin nanoparticles were synthesised using an ionic gelation technique. Chitosan, a naturally occurring biopolymer derived from crustaceans, was utilised for its mucoadhesive properties to enhance compound absorption. The synthesised nanoparticles were evaluated using physical characterisation, antioxidant radical scavenging assays, and anticancer assessments against MDA-MB-231 cells. Compared to chitosan and hesperidin administered individually, the combined nanoparticles demonstrated superior radical scavenging capacity. In cell culture tests, the formulation proved significantly more effective at suppressing cancer cell viability, triggering early cell cycle arrest, and promoting apoptosis. Overall, the chitosan carrier produces a highly soluble system that substantially enhances the biological activity of hesperidin.
Many promising plant-derived compounds fail as medicines because the body struggles to absorb them. By enclosing the poorly soluble flavonoid hesperidin inside a crustacean-derived biopolymer, this delivery system substantially enhances its solubility and potency. This approach offers a cleaner, more efficient mechanism to deliver natural antioxidant and antitumor treatments, potentially leading to more potent formulations against aggressive cancer cells.
This delivery method could enable improved therapeutic formulations for oncology drug developers and nutraceutical companies working with poorly soluble flavonoids. The abstract indicates early-stage laboratory research limited to material characterisation and in vitro testing on MDA-MB-231 cancer cells. It remains distant from commercialisation, requiring extensive in vivo testing, stability assessments, and formal clinical trials before real-world deployment as a medical treatment.
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One flavonoid glycoside with demonstrated therapeutic potential for several illnesses, including cancer, is hesperidin. However, because of its limited bioavailability and solubility, it is only marginally absorbed, necessitating a delivery mechanism to reach the intended therapeutic target. Additionally, the cytoskeleton of crustaceans yields chitosan, a naturally occurring biopolymer with mucoadhesive properties that has been used to improve the absorption of advantageous chemical substances like flavonoids. Chitosan/hesperidin nanoparticles (Hes-Nanoparticles) were made using the ion gelation technique. The synthesis of Hes-Nanoparticles was confirmed by several characterization methods, including the swelling test, zeta potential, particle size, FTIR, XRD, TEM, and SEM. DPPH and ABTS were used to demonstrate radical scavenging activity in antioxidant assays of chitosan, hesperidin, and the synthesized Hes-Nanoparticles. In addition, by a viability assay against MDA-MB-231, the anticancer efficacies of chitosan, hesperidin, and the synthesized Hes-Nanoparticles were assessed. Furthermore, annexin-V/PI double staining and the cycle of cell analysis were determined by flow cytometry. The results displayed that Hes-Nanoparticles have higher antioxidant activity than chitosan and hesperidin alone. Also, it has been demonstrated that Hes-Nanoparticles are more effective in early cell cycle arrest, suppressing the viability of cancer cells, and increasing cell apoptosis than chitosan and hesperidin alone. In conclusion, Hes-Nanoparticles demonstrated more antioxidant and antitumor activities than chitosan and hesperidin alone. Moreover, it has been established that Hes-Nanoparticles, in a highly soluble form, increase activity in contrast to the poorly soluble form of hesperidin alone.
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DOI: 10.3390/ph17080999
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