In this study, the hydrophobic drug Tanshinone ⅡA (Tan ⅡA) as a therapeutic drug was loaded into naphthalene acetic acid-phenylalanine-phenylalanine-glycine hydrogel (Nap-FFG) to construct the supramolecular hydrogels. Nap-FFG hydrogel fibers crosslinked into a network-like structure by self-assembly of polypeptides and then achieved drug loading. The rheological assay of Tan ⅡA-loaded Nap-FFG hydrogel (Tan@Nap-FFG) had excellent shear resistance, allowing it to maintain gel state. Anticoagulant and anti-oxidant assay showed Tan@Nap-FFG hydrogels synergistically resisted hydrogen peroxide damage and inhibited platelet aggregation caused by ADP, which was suitable for the therapy of cardiovascular diseases. In-vitro release assays and in-vivo pharmacokinetic had demonstrated that hydrogels released drugs slowly, reduced drug toxicity , and improved pharmacokinetic behavior. In summary, Tan@Nap-FFG hydrogels was expected to be developed as a novel injection for cardiovascular therapy.
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.
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