Binding of Tetracyclines to Bone

Dd, Perrin

doi:10.1038/208787a0

Cited by 66 publications

(42 citation statements)

References 7 publications

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“…(3) Pure HA (Durapatite') in solid form and commercial HA in powder form were found to bind TC and its analogs quite rapidly in vitro [3]. Samples of tetracycline (TC), tetracyclinitrile (CN), isotetracycline (ISO), and cetocycline (CETO) ( Fig.…”

Section: Methodsmentioning

confidence: 99%

“…It has been suggested that TC binds to the surface of apatite by complexing at more than one site [3]. The concentration of Ca in the adsorption bath has been shown Send reprint requests to H. M. Myers at the above address.…”

mentioning

confidence: 99%

“…The adsorption of TC on HA has been considered with the use of models [3]. Edge-on orientation of TC perpendicular to the a,b plane gave a close fit (within 0.1A) of 3 oxygen atoms of the TC with 2 trigonal and 1 hexagonal Ca +2 ion of adjacent unit cells of HA.…”

mentioning

confidence: 99%

“…Although complex formation between tetracyclines and solution cations has been widely studied [13,[15][16][17][18][19][20], the relationship between these antibiotics and the Ca of HA has been given less attention [3,5,8].…”

mentioning

confidence: 99%

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IR absorption spectrophotometric analysis of the complex formed by tetracycline and synthetic hydroxyapatite

Myers

Tochon-Danguy²,

Baud³

1983

Calcif Tissue Int

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The infrared (IR) spectra of KBr pellet preparations of tetracycline (TC) complexes with hydroxyapatite (HA) indicated that the binding of the antibiotic to bone mineral can occur independently at each of two ligands. The shifts in the IR spectrum occur for the keto-enol ligand of rings B and C and for the tricarbonylmethane grouping of ring A. Analogs that lack one or the other of these groups are able to form complexes with HA in which the common portion resembles that of the parent molecule.

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Section: Methodsmentioning

confidence: 99%

mentioning

confidence: 99%

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confidence: 99%

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confidence: 99%

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IR absorption spectrophotometric analysis of the complex formed by tetracycline and synthetic hydroxyapatite

Myers

Tochon-Danguy²,

Baud³

1983

Calcif Tissue Int

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“…However, in clinical applications, many previous studies have shown that TC can be taken up by bone through a reaction that appears to occur directly between TC and hydroxyapatite Ca 10 (PO 4 ) 6 (OH) 2 , the major constituent of bone tissue. 15 Thus, TC can be a potent chemical compound for bone targeting.…”

mentioning

confidence: 99%

Tetracycline-grafted PLGA nanoparticles as bone-targeting drug delivery system

Wang¹,

Liu²,

Tao³

et al. 2015

IJN

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Purpose Nanoparticles (NPs) that target bone tissue were developed using poly(lactic-co-glycolic acid) (PLGA) copolymers and tetracycline (TC)-based bone-targeting moieties. These NPs are expected to enable the transport of drugs, such as simvastatin (SIM), for the treatment of osteoporosis. Methods The molecular structures of TC–PLGA were validated by 1 H-NMR, and the SIM-loaded NPs were prepared using the solvent emulsification method. The surface properties, cytotoxicity, cellular uptake, cell mineralization, bone targeting potential, and animal pharmacodynamics of the TC–PLGA NPs were evaluated and compared to those of PLGA NPs. Results It was confirmed that the average particle size of the NPs was approximately 220 nm. In phosphate-buffered saline (PBS, pH 7.4), the SIM-loaded NPs exhibited a cumulative release of up to 80% within 72 hours. An in vitro cell evaluation indicated that the NPs had an excellent cellular uptake capacity and showed great biocompatibility with MC3T3-E1 cells, thereby reducing the cytotoxic effects of SIM. The cell mineralization assay showed that the SIM-loaded NPs induced osteogenic differentiation and mineralized nodule formation in MC3T3-E1 cells, thereby achieving the same effect as SIM. Preliminary findings from in vitro and in vivo bone affinity assays indicated that the TC–PLGA NPs may display increased bone-targeting efficiency compared to PLGA NPs lacking a TC moiety. The use of SIM-loaded TC–PLGA NPs in treating osteoporosis was tested through animal pharmacodynamics analyses performed in ovariectomized rats, and the results suggested that the SIM-loaded TC–PLGA NPs can improve the curative effects of SIM on the recovery of bone mineral density compared to either SIM-loaded PLGA NPs or SIM alone. Conclusion Bone-targeting NPs, which were based on the conjugation of TC to PLGA copolymers, have the ability to target bone. These NPs may be developed as a delivery system for hydrophobic drugs, and they are expected to improve the curative effects of drugs, reduce the administered drug doses, and reduce side effects in other organs.

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In vitro antibacterial efficacy of tetracycline hydrochloride adsorbed onto Bio‐Oss® bone graft

et al. 2010

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Local delivery of antibiotics may provide the advantage of reducing the potential side effects associated with their systemic administration. This study assessed, in vitro, the antimicrobial efficacy of tetracycline hydrochloride (TCH) adsorbed onto Bio-Oss bone grafts against a range of pathogenic bacteria. Various levels of TCH were adsorbed onto Bio-Oss granules by immersing in TCH aqueous solutions of different initial concentrations for 48 h at room temperature. TCH release was assessed in phosphate buffered saline at 37 degrees C, and its antimicrobial efficacy, up to 96 h, was tested against two Gram-negative bacteria associated with periodontal diseases: Aggregatibacter (formerly Actinobacillus) actinomycetemcomitans, and Porphyromonas gingivalis, and one Gram-positive bacterium associated with soft-tissue and bone infections: Staphylococcus aureus. The range of TCH concentrations studied was also assessed for cytotoxicity against osteoblast-like human osteosarcoma cell lines. The amount of TCH adsorbed and released from Bio-Oss was concentration dependent. All TCH adsorbed Bio-Oss resulted in a reduction of A. actinomycetemcomitans, P. gingivalis, and S. aureus and higher concentrations were generally more effective in reducing or eliminating bacterial growth. The proliferation of HOS cells was not substantially reduced except for the maximum concentration of TCH. In addition to its osteoconductive role, TCH adsorbed Bio-Oss could also be functional in negating systemically antibiotic prophylactic treatment in the prevention of implant or biomaterial related infections.

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Binding of Tetracyclines to Bone

Cited by 66 publications

References 7 publications

IR absorption spectrophotometric analysis of the complex formed by tetracycline and synthetic hydroxyapatite

IR absorption spectrophotometric analysis of the complex formed by tetracycline and synthetic hydroxyapatite

Tetracycline-grafted PLGA nanoparticles as bone-targeting drug delivery system

In vitro antibacterial efficacy of tetracycline hydrochloride adsorbed onto Bio‐Oss® bone graft

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