Evidence map›Paper›PMID 26331790›Full record

ArticleBiomacromolecules2015

Biodistribution of Fracture-Targeted GSK3β Inhibitor-Loaded Micelles for Improved Fracture Healing.

Stewart A Low, Chris V Galliford, Jiyuan Yang, Philip S Low, Jindřich Kopeček

Open access · greenAbstract read
In one paragraph

Article in Biomacromolecules, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
1.1field-weighted citation impact, top 19% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

17 citing papers in PubMed, 27 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Review
  5. An engineered dual function peptide to repair fractured bones.Journal of controlled release : official journal of the Controlled Release Society · 2022
    Article
  6. Macrophage depletion increases target specificity of bone-targeted nanoparticles.Journal of biomedical materials research. Part A · 2022
    Article
  7. Article
  8. Biomaterials for Orthopaedic Diagnostics and Theranostics.Current opinion in biomedical engineering · 2021
    Article
  9. Review
  10. Article
  11. Article
  12. Review
  13. Review
  14. Development of controlled drug delivery systems for bone fracture-targeted therapeutic delivery: A review.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2018
    Review
  15. Article
  16. Review
  17. Indium-based and iodine-based labeling of HPMA copolymer-epirubicin conjugates: Impact of structure on the in vivo fate.Journal of controlled release : official journal of the Controlled Release Society · 2016
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

5 authors at 1 institution in 1 country.

Stewart A Low
Chris V GallifordDepartment of Chemistry, Purdue University , West Lafayette, Indiana 47907, United States.
Jiyuan Yang
Philip S LowDepartment of Chemistry, Purdue University , West Lafayette, Indiana 47907, United States.
Jindřich Kopeček
Purdue University West Lafayette · US

Funding

BONE TARGETED DELIVERY OF ANABOLIC AGENTSR01GM069847 · NIGMS · UNIVERSITY OF UTAH · PI KOPECEK, JINDRICH H. · 2004 to 2011
$2.3M
NIGMS NIH HHS R01 GM069847NIGMS NIH HHS R01 GM69847
6 · The paper itself

Abstract

Bone fractures constitute a major cause of morbidity and mortality especially in the elderly. Complications associated with osteoporosis drugs and the age of the patient slow bone turnover and render such fractures difficult to heal. Increasing the speed of fracture repair by administration of a fracture-targeted bone anabolic agent could find considerable application. Aspartic acid oligopeptides are negatively charged molecules at physiological pH that adsorb to hydroxyapatite, the mineral portion of bone. This general adsorption is the strongest where bone turnover is highest or where hydroxyapatite is freshly exposed. Importantly, both of these conditions are prominent at fracture sites. GSK3β inhibitors are potent anabolic agents that can promote tissue repair when concentrated in a damaged tissue. Unfortunately, they can also cause significant toxicity when administered systemically and are furthermore difficult to deliver due to their strong hydrophobicity. In this paper, we solve both problems by conjugating the hydrophobic GSK3β inhibitor to a hydrophilic aspartic acid octapeptide using a hydrolyzable bond, thereby generating a bone fracture-targeted water-soluble form of the drug. The resulting amphiphile is shown to assemble into micelles, extending its circulation time while maintaining its fracture-targeting abilities. For measurement of pharmacokinetics, an 125I was introduced at the location of the bromine in the GSK3β inhibitor to minimize any structural differences. Biodistribution studies demonstrate a greater than 4-fold increase in fracture accumulation over healthy bone.

Indexed as

MicellesAnimalsDrug CarriersFracture HealingGlycogen Synthase Kinase 3Glycogen Synthase Kinase 3 betaMiceProtein Kinase InhibitorsTissue DistributionTomography, Emission-Computed, Single-PhotonTomography, X-Ray ComputedDrug CarriersGlycogen Synthase Kinase 3Glycogen Synthase Kinase 3 betaGsk3b protein, mouseMicellesProtein Kinase Inhibitors

Identifiers

PMID26331790
PMCPMC4800810
OpenAlexW2436450428

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.