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Abstract
Chalcones (1,3-diaryl-2-propen-1-ones) are naturally occurring polyphenols with known anticancer activity against a variety of tumor cell lines, including osteosarcoma (OS). In this paper, we present the preparation and characterization of spheres (~2 mm) from polyvinyl alcohol (PVA) containing a combination of 4′-Amino-1-Naphthyl-Chalcone (D14) and doxorubicin, to act as a new polymeric dual-drug anticancer delivery. D14 is a potent inhibitor of osteosarcoma progression and, when combined with doxorubicin, presents a synergetic effect; hence, physically crosslinked PVA spheres loaded with D14 and doxorubicin were prepared using liquid nitrogen and six freeze–thawing cycles. Physical-chemical characterization using a scanning electron microscope (SEM), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) presented that the drugs were incorporated into the spheres via weak interactions between the drugs and the polymeric chains, resulting in overall good drug stability. The cytotoxicity activity of the PVA spheres co-encapsulating both drugs was tested against the U2OS human osteosarcoma cell line by 3- (4,5-dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide (MTT) assay, and compared to the spheres carrying either D14 or doxorubicin alone. The co-delivery showed a cytotoxic effect 2.6-fold greater than doxorubicin alone, revealing a significant synergistic effect with a coefficient of drug interaction (CDI) of 0.49. The obtained results suggest this developed PVA sphere as a potential dual-drug delivery system that could be used for the prominent synergistic anticancer activity of co-delivering D14 and doxorubicin, providing a new potential strategy for improved osteosarcoma treatment.
Highlights
Chalcones are phytocompounds found abundantly in nature and are precursors of different types of flavonoids, such as flavonols, catechins, isoflavones, and others
We characterized the antimetastatic activity of D14 against osteosarcoma cell lines, which presented reduced cell migration and invasion, while promoting p53 protein expression and a decrease in matrix metalloproteinases [6]
We developed polyvinyl alcohol (PVA) spheres containing doxo and D14 as co-delivery, aiming at increasing the effectiveness of doxo treatment against osteosarcoma cells
Summary
Chalcones are phytocompounds found abundantly in nature and are precursors of different types of flavonoids, such as flavonols, catechins, isoflavones, and others. Can upregulate the p53 expression that inhibits migration and invasion of osteosarcoma cancer cells [6], corresponding to fundamental processes for metastasis development and progression. In addition to their isolated effects, chalcones have synergistic effects when associated with classical antitumor drugs, such as doxorubicin (doxo), etoposide and cisplatin [7,8,9]. Despite this proven anticancer property, usage of these compounds in the therapeutic field is limited. Drug delivery systems (DDS) have been suggested in order to encapsulate these compounds into carriers that improve drug solubility, bioavailability, and its crucial therapeutic efficiency [12,13,14]
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