Improving the effectiveness of anticancer bioactive compounds

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Throughout the ages, the human being has learned how to use plant extracts for different purposes. These extracts are complex mixtures of chemicals with multiple biological functions (antioxidant, antibiotic, anticancer, antifungal, antiparasitic) derived mainly from the leaves, the stems, the fruits, or the roots of medicinal plants. Modern science allowed to identify, test, synthesize, and therapeutically exploit bioactive compounds. A notable example is the isofuranodiene (IFD) molecule, isolated from plant species of the genera CommiphoraCurcumaEugenia and Smyrnium. IFD has several potential therapeutic effects, above all, multiple anticancer activities. However, its therapeutic use is hindered by its solid-state instability, low water solubility and bioavailability. Therefore, including the IFD molecule in specific nanocarriers can improve its bioavailability and thus its therapeutic performances.

Cytotoxicity of Isofuranodiene against human breast adenocarcinoma cells was markedly enhanced upon encapsulation in monoolein nanoparticles with an inverse hexagonal internal structure

In this study, carried out by Prof. Paola Astolfi and Prof. Michela Pisani (Università Politecnica delle Marche) and colleagues, lipid vectors such as monoolein nanoparticles (cubosomes and hexosomes) were employed. These nanocarriers already proved to efficiently incorporate different therapeutic agents, and sustain their controlled release thanks to their highly ordered internal structures.

The IFD-loaded nanoparticles were characterised by Small-angle X-ray Scattering (SAXS), and UV Resonant Raman (UVRR), respectively at the Austrian and Italian CERIC partner facilities in Trieste. At the same time, free IFD and IFD-loaded nanovectors were tested against human breast adenocarcinoma cells. The results of the study showed that isofuranodiene is efficiently encapsulated in the carrier nanoparticles and that their combination can better inhibit cancer cell proliferation when compared to free IFD, thus bringing this anticancer compound a step closer to the medical practice.

ORIGINAL ARTICLE:

NANOSTRUCTURED LIQUID CRYSTALLINE PARTICLES AS DELIVERY VECTORS FOR ISOFURANODIENE: CHARACTERIZATION AND IN-VITRO ANTICANCER ACTIVITY, PISANI M., QUASSINTI L., BRAMUCCI M., GALASSI R., MAGGI F., ROSSI B., DAMIN A., CARLONI P., & ASTOLFI, P. (2020),  COLLOIDS AND SURFACES B: BIOINTERFACES, 111050.