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Self-assembling bisphosphonates into nanofibers to enhance their inhibitory capacity on bone resorption

2016; Royal Society of Chemistry; Volume: 8; Issue: 20 Linguagem: Inglês

10.1039/c6nr00843g

2040-3372

Anming Tang, Yu Qian, Shuang Liu, Weijuan Wang, Bing Xu, An Qin, Gaolin Liang,

Connective tissue disorders research

Osteoporosis (OP) is an important aging-related disease and the effective prevention/treatment of this disease remains challenging. Considering the acidic microenvironment of bone resorption lacunae, herein, we rationally designed two pamidronate (Pami)-derivative and alendronate (Alen)-derivative hydrogelators Pami-D and Alen-D which self-assemble into nanofibers to form supramolecular hydrogels under acidic conditions. Cell viability assay, osteoclastogenesis, osteoclastic gene expression, and in vitro bone resorption results indicated that both Pami-D and Alen-D have better inhibitory effects on osteoclastic formation and bone resorption than Pami and Alen, respectively. We anticipate that our new drugs Pami-D and Alen-D could "smartly" self-assemble and locally concentrate the drugs at bone resorption lacunae in vivo and subsequently prevent/treat osteoporosis more efficiently.