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J Control Release. 2013 Apr 28;167(2):175-88. doi: 10.1016/j.jconrel.2013.01.032. Epub 2013 Feb 8.

Biomedical applications of bisphosphonates.

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Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, ETH Zürich, Wolfgang-Pauli-Str. 10, 8093 Zürich, Switzerland.


Since their discovery over 100 years ago, bisphosphonates have been used industrially as corrosion inhibitors and complexing agents. With the discovery of their pharmacological activity in the late 1960s, implicating their high affinity for hydroxyapatite, bisphosphonates have been employed in the treatment of bone diseases and as targeting agents for colloids and drugs. They have notably been investigated for the treatment of Paget's disease, osteoporosis, bone metastases, malignancy-associated hypercalcemia, and pediatric bone diseases. Currently, they are first-line medications for several of these diseases and are taken by millions of patients worldwide, mostly postmenopausal women. A major problem associated with their use is their low oral bioavailability. Several delivery systems have been proposed to improve their absorption and to direct them to sites other than bone tissues. Beyond their important pharmacological role, the medical applications of bisphosphonates are numerous. In addition, their metal-chelating properties have been exploited to coat and stabilize implants, nanoparticulates, and contrast agents. In this contribution, we review the pharmacological and clinical uses of bisphosphonates and highlight their novel applications in the pharmaceutical and biomedical fields.

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