pH-responsive prodrug nanoparticles based on xylan-curcumin conjugate for the efficient delivery of curcumin in cancer therapy

• Published in: Carbohydrate polymers Vol. 188; pp. 252 - 259
• Main Authors: Sauraj, Kumar, S. Uday, Kumar, Vinay, Priyadarshi, Ruchir, Gopinath, P., Negi, Yuvraj Singh
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 15.05.2018
• Subjects: Cell cytotoxicity; Cell Line, Tumor; Cell Survival - drug effects; Curcumin; Curcumin - chemistry; Curcumin - pharmacology; Drug-release; Hemocompatibility; HT29 Cells; Humans; Hydrogen-Ion Concentration; Nanoparticles - chemistry; Prodrug NPs; Prodrugs - chemistry; Prodrugs - pharmacology; Xylan; Xylans - chemistry; Xylan; Prodrug NPs; Curcumin; Drug-release; Cell cytotoxicity; Hemocompatibility
• ISSN: 0144-8617; 1879-1344
• DOI: 10.1016/j.carbpol.2018.02.006

•pH-responsive xyl-cur prodrug NPs were prepared by dialysis membrane method.•Xyl-cur prodrug NPs showed pH-responsive drug released behavior.•Xyl-cur prodrug NPs are biocompatible and safe for intravenous administration.•Xyl-cur prodrug NPs demonstrated higher cytotoxic activity than free curcumin. In the present study, novel pH-responsive prodrug nanoparticles based on xylan-curcumin (xyl-cur) conjugate were developed to enhance the therapeutic efficacy of curcumin in cancer therapy. The synthesis of xyl-cur conjugate (prodrug) was confirmed by FT-IR, 1H NMR, UV–vis and fluorescence spectroscopy. The xyl-cur prodrug was subsequently self-assembled in to nanoparticles (xyl-cur prodrug NPs) in an aqueous medium with the average particle size 253 nm and the zeta potential of −18.76 mV. The xyl-cur prodrug NPs were highly pH-sensitive in nature and most of the drug was released at lower pH. The interaction of the xyl-cur prodrug NPs with blood components was tested by hemolysis study. The cytotoxic activity of the xyl-cur prodrug NPs against human colon cancer cells (HT-29, HCT-15) demonstrated that the prodrug NPs exhibits greater cytotoxic effect than curcumin. Therefore, these results reveal that xyl-cur prodrug NPs could be a promising candidate for improving the intracellular delivery of curcumin in cancer therapy.