Synthesis and therapeutic effect of styrene-maleic acid copolymer-conjugated pirarubicin.
Bottom Line: The SMA-THP conjugate also formed micelles and showed albumin binding capacity in aqueous solution, which suggested that this conjugate behaved as a macromolecule during blood circulation.Consequently, SMA-THP conjugate showed significantly prolonged circulation time compared to free THP and high tumor-targeting efficiency by the enhanced permeability and retention (EPR) effect.These findings suggest the potential of SMA-THP conjugate as a highly favorable candidate for anticancer nanomedicine with good stability and tumor-targeting properties in vivo.
Affiliation: Institute for Drug Delivery Science, Sojo University, Kumamoto, Japan; Faculty of Pharmaceutical Sciences, Sojo University, Kumamoto, Japan.Show MeSH
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Mentions: As shown in Figure3(a), SMA-THP conjugate showed dose-dependent cytotoxicity against HeLa cells with an IC50 of 22 μM. In contrast, free THP showed much potent cytotoxicity (IC50, 0.17 μM). Similar results were observed in colon 26 cells: the IC50 of free THP was 0.02 μM, compared to SMA-THP of 12.6 μM (Fig.3b). In both cell lines, cytotoxicity of SMA-THP conjugate was less than 1/100 compared with that of free THP.
Affiliation: Institute for Drug Delivery Science, Sojo University, Kumamoto, Japan; Faculty of Pharmaceutical Sciences, Sojo University, Kumamoto, Japan.