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Updated: Jan 23, 2026

An Injectable and Drug-loaded Supramolecular Hydrogel for Local Catheter Injection into the Pig Heart
Published on: June 7, 2015
Bio-inspired drug-dominated supramolecular nanocomplex based on low molecular weight heparin for progressive tumor
1State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Stability of Biopharmaceuticals, Department of Pharmaceutics, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
Abstract:
Low molecular weight heparin (LMWH) is a natural sulfated glycosaminoglycan with the affinity to proangiogenic factors, rendering it a promising agent for tumor therapy. Inspired by DOX binding to the helix of DNA, mitochondrial damage KLA peptide derivative (mKLA) and anti-angiogenic LMWH-chrysin conjugate (LC) are constructed to simulate the double strands for doxorubicin (DOX) binding (LKD nanocomplex). Initiated and "locked" by DOX, mKLA and LC temporarily aggregate by π-π stacks, electrostatic and hydrophobic interactions in aqueous condition with self-amplified DOX loading (19.07 ± 1.08 wt%). During endosome-lysosome trafficking, DOX protonated by H+ could "unlock" the LKD nanocomplex to disassemble, which enables mKLA and DOX to damage mitochondria and nucleus DNA respectively, and LMWH could also inhibit angiogenesis. Based on the strong inhibition of tumors at all stages in vivo, we hold that LKD nanocomplex provides a new opportunity based on smart construction of carbohydrate materials for clinically advanced cancer patients.
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