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Development of Bone Targeting Drugs

Department of Biological Sciences, University of Delaware, Newark, DE 19716, USA
Nemours/Alfred I. duPont Hospital for Children, Wilmington, DE 19803, USA
Institute for the Study of Inborn Errors of Metabolism, Pontificia Universidad Javeriana, Bogotá D.C. 110231, Colombia
Department of Pediatrics, Graduate School of Medicine, Gifu University, Gifu 501-1193, Japan
Department of Pediatrics, Thomas Jefferson University, Philadelphia, PA 19107, USA
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Int. J. Mol. Sci. 2017, 18(7), 1345;
Received: 21 April 2017 / Revised: 15 June 2017 / Accepted: 16 June 2017 / Published: 23 June 2017
(This article belongs to the Special Issue Advances in Bone and Cartilage Research)
The skeletal system, comprising bones, ligaments, cartilage and their connective tissues, is critical for the structure and support of the body. Diseases that affect the skeletal system can be difficult to treat, mainly because of the avascular cartilage region. Targeting drugs to the site of action can not only increase efficacy but also reduce toxicity. Bone-targeting drugs are designed with either of two general targeting moieties, aimed at the entire skeletal system or a specific cell type. Most bone-targeting drugs utilize an affinity to hydroxyapatite, a major component of the bone matrix that includes a high concentration of positively-charged Ca2+. The strategies for designing such targeting moieties can involve synthetic and/or biological components including negatively-charged amino acid peptides or bisphosphonates. Efficient delivery of bone-specific drugs provides significant impact in the treatment of skeletal related disorders including infectious diseases (osteoarthritis, osteomyelitis, etc.), osteoporosis, and metabolic skeletal dysplasia. Despite recent advances, however, both delivering the drug to its target without losing activity and avoiding adverse local effects remain a challenge. In this review, we investigate the current development of bone-targeting moieties, their efficacy and limitations, and discuss future directions for the development of these specific targeted treatments. View Full-Text
Keywords: bone targeting drugs; osteoporosis; metabolic skeletal dysplasia; bisphosphonates; nanoparticles bone targeting drugs; osteoporosis; metabolic skeletal dysplasia; bisphosphonates; nanoparticles
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MDPI and ACS Style

Stapleton, M.; Sawamoto, K.; Alméciga-Díaz, C.J.; Mackenzie, W.G.; Mason, R.W.; Orii, T.; Tomatsu, S. Development of Bone Targeting Drugs. Int. J. Mol. Sci. 2017, 18, 1345.

AMA Style

Stapleton M, Sawamoto K, Alméciga-Díaz CJ, Mackenzie WG, Mason RW, Orii T, Tomatsu S. Development of Bone Targeting Drugs. International Journal of Molecular Sciences. 2017; 18(7):1345.

Chicago/Turabian Style

Stapleton, Molly, Kazuki Sawamoto, Carlos J. Alméciga-Díaz, William G. Mackenzie, Robert W. Mason, Tadao Orii, and Shunji Tomatsu. 2017. "Development of Bone Targeting Drugs" International Journal of Molecular Sciences 18, no. 7: 1345.

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