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Osteotropic Nanoscale Drug Delivery System via a Single Aspartic Acid as the Bone-Targeting Moiety

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Osteotropic nanoparticle-based drug delivery systems have been investigated as potential therapies for various skeletal diseases. These delivery systems are usually formulated by functionalizing the nanoparticle surfaces with bone-targeting ligands. Antibodies, proteins or peptide sequences have shown promise as bone-targeting ligands; however, methods utilizing these targeting ligands suffer from many limitations including high production cost, protein or peptide instability, and unwanted immune response. These limitations can be minimized by using the osteotropic small molecule approach because of the stability, ease of conjugation with polymeric nanoparticles, and low cost of small molecules. We, and others, have previously demonstrated that poly-aspartic acid sequencelinked biodegradable polymeric nanoparticles can interact specifically with mineralized tissue in vitro, ex vivo, and in vivo. The hypothesis of this study is that single aspartic acid-linked nanoparticles can effectively interact with bone tissue specifically. In this study, we sought to identify the minimal aspartic acid residues stretch necessary for efficient HA binding. We further sought to design a novel osteotropic nanoparticle-based drug delivery system using a single aspartic acid small molecule as the bone-targeting moiety.

Keywords: Musculoskeletal Tissue; Nanomedicine; Small Molecules; Targeted Drug Delivery; Targeting Ligands

Document Type: Research Article

Affiliations: 1: Institute for Regenerative Engineering, University of Connecticut Health Center, School of Medicine, Farmington, CT 06030, United States 2: Department of Biomedical Engineering, University of Wisconsin-Madison, Madison, WI 53705, United States

Publication date: March 1, 2017

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  • Journal for Nanoscience and Nanotechnology (JNN) is an international and multidisciplinary peer-reviewed journal with a wide-ranging coverage, consolidating research activities in all areas of nanoscience and nanotechnology into a single and unique reference source. JNN is the first cross-disciplinary journal to publish original full research articles, rapid communications of important new scientific and technological findings, timely state-of-the-art reviews with author's photo and short biography, and current research news encompassing the fundamental and applied research in all disciplines of science, engineering and medicine.
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