P-Sulfocalix[6]arene as Nanocarrier for Controlled Delivery of Doxorubicin.

Authors :: Ostos FJ
Lebrón JA
Moyá ML
López-López M
Sánchez A
Clavero A
García-Calderón CB
Rosado IV
López-Cornejo P
Source :: Chemistry, an Asian journal [Chem Asian J] 2017 Mar 16; Vol. 12 (6), pp. 679-689. Date of Electronic Publication: 2017 Feb 28.
Publication Year :: 2017
Abstract: Given the high toxicity of the anthracycline antibiotic doxorubicin (DOX), it is relevant to search for nanocarriers that decrease the side effects of the drug and are able to transport it towards a therapeutic target Here, the encapsulation of DOX by p-sulfocalix[6]arene (calix) has been studied. The interaction of DOX with the macrocycle, as well as with DNA, has been investigated and the equilibrium constant for each binding process estimated. The results showed that the binding constant of DOX to DNA, K <subscript>DNA</subscript> , is three orders of magnitude higher than that to calix, K <subscript>calix</subscript> . The ability of calixarenes to encapsulate DOX molecules, as well as the capability of the DOX molecules included into the inner cavity of the macrocycle to bind with DNA have been examined. Cytotoxicity measurements were done in different cancer and normal cell lines to probe the decrease in the toxicity of the encapsulated DOX. The low toxicity of calixarenes has also been demonstrated for different cell lines.<br /> (© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)