Evaluation of the Antitumour and Antiproliferative Effect of Xanthohumol-Loaded PLGA Nanoparticles on Melanoma

Abstract

Cutaneous melanoma is the deadliest type of skin cancer and current treatment is still inadequate, with low patient survival rates. The polyphenol xanthohumol has been shown to inhibit tumourigenesis and metastasization, however its physicochemical properties restrict its application. In this work, we developed PLGA nanoparticles encapsulating xanthohumol and tested its antiproliferative, antitumour, and migration effect on B16F10, malignant cutaneous melanoma, and RAW 264.7, macrophagic, mouse cell lines. PLGA nanoparticles had a size of 312 ± 41 nm and a PdI of 0.259, while achieving a xanthohumol loading of about 90%. The viability study showed similar cytoxicity between the xanthohumol and xanthohumol-loaded PLGA nanoparticles at 48 h with the IC50 established at 10 µM. Similar antimigration effects were observed for free and the encapsulated xanthohumol. It was also observed that the M1 antitumor phenotype was stimulated on macrophages. The ultimate anti-melanoma effect emerges from an association between the viability, migration and macrophagic phenotype modulation. These results display the remarkable antitumour effect of the xanthohumol-loaded PLGA nanoparticles and are the first advance towards the application of a nanoformulation to deliver xanthohumol to reduce adverse effects by currently employed chemotherapeutics.

Targeting STAT3 and NF-κB Signaling Pathways in Cancer Prevention and Treatment: The Role of Chalcones

“…An example of such modifications is the developed poly-lactic-co-glycolic acid (PLGA) nanoparticles encapsulating xanthohumol and tested for antiproliferative, anticancer, and migratory effects on malignant skin melanoma cells (B16F10) and mouse macrophages (RAW 264.7). The obtained results confirm the anticancer effect of PLGA nanoparticles loaded with xanthohumol and represent the first signs of progress towards the use of a nanoformulation delivering xanthohumol to reduce the side effects of currently used chemotherapeutics [ 116 ].…”

Anticancer Potential of Natural Chalcones: In Vitro and In Vivo Evidence

“…Although there are limited data about the bioavailability of XH, it is generally accepted that XH has low bioavailability in humans and animals [ 332 ]. The study by Fonseca et al [ 333 ] was focused on the comparison of the antiproliferative effect of XH and XH encapsulated in poly lactic-co-glycolic acid (PLGA) nanoparticles in the B16F10 melanoma cell line. The results showed similar activity of both XH and encapsulated XH on cell viability and migration and demonstrated the suitability of this nano-carrier for XH delivery.…”