A study of the delivery-targeting concept applied to antineoplasic drugs active on human osteosarcoma. I. Synthesis and biological activity in nude mice carrying human osteosarcoma xenografts of gem-bisphosphonic methotrexate analogues

In vitro and in vivo toxicity of 5-FdU-alendronate, a novel cytotoxic bone-seeking duplex drug against bone metastasis

“…The chemical linkage of the compounds is the determining factor for stability, pharmacokinetic and pharmacological properties of such bonetargeting conjugates. Several previously synthesized BPconjugates linking antitumor agents to BPs only showed modest anticancer activities [10][11][12][13].…”

Comparative biodistribution of thin‐coated iron oxide nanoparticles TCION: Effect of different bisphosphonate coatings

“…This type of molecule is used in many studies for its bone tropism [Sturtz et al, 1992] and in clinical routine for bone scintigraphy. Because of the relative stability of the nanoparticle labeling in the early times after injection (reflected by near constant 99m Tc/ 59 Fe ratios) and the important dose of particles fixed compared to other peripheral organs (muscle, skin), the fixation concerns more likely particles rather than bisphosphonate molecules chelating Tc and 59 Fe doses fixed by mineral bone after extraction of the bone marrow and compared to the activity of the complete bone.…”

Bisphosphonate conjugation for bone specific drug targeting

“…However, many also lack convincing data for conjugate function. An early study showed that BP and methotrexate linked together via a peptide bond successfully localized to bone ( Table 1 : 1) ( Hosain et al, 1996 ; Sturtz et al, 1992 ). Later, another BP-methotrexate conjugate was shown to induce apoptosis in OS cells in vitro but at a rate similar to the standard methotrexate OS treatment ( Yang et al, 2014a ).…”