Anticancer activity and pharmacokinetics of TanshinoneⅡA derivative supramolecular hydrogels

In this work, we studied the synthesis, characterization, anticancer effect and pharmacokinetics of supramolecular hydrogels composed of 2-naphthalene acetic acid-Gly-Arg-Gly-Asp-Phe-Phe-Gly poly-peptide (Nap-peptide) and TanshinoneⅡA (TsⅡA) derivative (Ts-OH) which had excellent selectivity for inhibiting growth of cancer cells. The Nap-Ts hydrogels exhibited long, narrow and flexible nanofibers entangling each other to form three-dimensional networks, which further self-assembling into nanoparticles with diameters from 200 to 300 nm. The hydrogels drug delivery was suitable for the sustained release, which exhibited both diffusion and relaxation release mechanisms. Compared to TsⅡA, the Ts-OH, Nap-Ts hydrogels exhibited higher anticancer effect to SCG7901 cells, MCF-7 cells, HepG2 cells and MDA-MB-231 cells in vitro. The pharmacokinetic behaviours of Nap-Ts hydrogels were evaluated in rats. The Nap-Ts hydrogels possessed better biocompatibility , sustain drug release and anticancer effect than TsⅡA. The results demonstrated the potential drug delivery system of TsⅡA improving the anticancer activity.