To improve orthopedic implant fixation and reduce post-operative complications, osteogenic molecules are delivered locally by immobilizing them on the surface of implants, which will modulate the biology of cell attachment and differentiation on the implant surface. Estradiol, a natural steroid hormone, maintains bone metabolism by decreasing bone resorption. It either directly or indirectly affects osteoclasts. In this work, estradiol was immobilized on a titanium surface by polydopamine adlayer. Immobilization of estradiol was confirmed by X-ray electron spectroscopy (XPS), immunofluorescence staining and enzyme-linked immunosorbent assay (ELISA). Estradiol-modified substrates enhanced alkaline phosphatases activity (ALP) and calcium deposition of osteoblasts. However, these substrates did not decrease tartrate-resistant acid phosphatase (TRAP) activity and actin ring formation of the osteoclast. The scanning electron microscopic (SEM) images of estradiol-modified substrates showed the formation of estradiol crystals, which decreased the potency of immobilized estradiol. Despite having a successful immobilization of estradiol via the polydopamine technique, the bioavailability and potency of coated estradiol is reduced due to crystallization, suggesting that this is not a suitable system for localized estradiol delivery as tested in vitro here. Consequently, other suitable platforms have to be explored for immobilizing estradiol that will prevent crystal formation while preserving the biological activity.
Keywords: estradiol; implants; osteoblasts and osteoclasts; osteoporosis; polydopamine.