Self-organized environment-sensitive inulin–doxorubicin conjugate with a selective cytotoxic effect towards cancer cells

摘要: An inulin-based random copolymer bearing high dose doxorubicin (18.45% on a weight basis), INU-EDA-P,C-DOXO, was prepared by coupling with inulin though citraconylamide bridge used as pH sensitive spacer. A further conjugation pentynoic acid via an amidic bond led to the hydrophobization of which allows acquisition self-assembling ability at low concentration (0.33 mg mL−1) combining both Π–Π stacking and London interactions. Drug release studies were carried out different demonstrating remarkable dependency, where maximum rate observed mimicking cancer tissue lysosomal environments. Besides, measuring ζ-potential variations function pH, INU-EDA-P,C-DOXO proved capable undergoing charge reversal acidic changing its physicochemical biological behavior. In vitro tests (MDA-MB 231) normal (HB-2) breast cells verify conjugate aptitude follow routes enter depending microenvironment. This finding supported quantitative up-take studies, revealed that released before entering cells, entire diffused across cell membranes without relevant modifications.