Evidence map›Paper›PMID 22888471›Full record

ArticleDrug delivery and translational research2011

Intravitreal Poly(L-lactide) Microparticles Sustain Retinal and Choroidal Delivery of TG-0054, a Hydrophilic Drug Intended for Neovascular Diseases.

Namdev B Shelke, Rajendra Kadam, Puneet Tyagi, Vidhya R Rao, Uday B Kompella

RetractedOpen access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Drug delivery and translational research, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It has been retracted, and should not be counted. Cited by 25 papers.

0numbers the graph read from it
0cells of the map it votes in
25citing papers in PubMed
3.7field-weighted citation impact, top 7% 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

25 citing papers in PubMed, 59 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Review
  6. Review
  7. Article
  8. Microsphere antioxidant and sustained erythropoietin-R76E release functions cooperate to reduce traumatic optic neuropathy.Journal of controlled release : official journal of the Controlled Release Society · 2021
    Article
  9. Review
  10. Article
  11. Intravitreal Delivery of VEGF-ACurrent eye research · 2019
    Article
  12. Article
  13. Article
  14. Article
  15. Article
  16. Corticosteroid-loaded biodegradable nanoparticles for prevention of corneal allograft rejection in rats.Journal of controlled release : official journal of the Controlled Release Society · 2015
    Article
  17. Article
  18. Article
  19. Development of a novel bioerodible dexamethasone implant for uveitis and postoperative cataract inflammation.Journal of controlled release : official journal of the Controlled Release Society · 2013
    Article
  20. Nanoparticle diffusion in, and microrheology of, the bovine vitreous ex vivo.Journal of controlled release : official journal of the Controlled Release Society · 2013
    Article
4 · The record

Corrections and comments

  • Expression of concern · 2015-12-28Concerns/Issues about Data · Falsification/Fabrication of Data · Investigation by Company/Institution · Misconduct - Official Investigation(s) and/or Finding(s) · Misconduct by Author · Unreliable Data · · R Kadam named for fabrication;
  • Expression of concern
5 · Who and what money

Authors and funding

5 authors at 1 institution in 1 country.

Namdev B ShelkeDepartment of Pharmaceutical Sciences, University of Colorado Denver, Aurora, Colorado.
Rajendra Kadam
Puneet Tyagi
Vidhya R Rao
Uday B Kompella
University of Colorado Denver · US

Funding

Transcleral Therapeutics in Diabetic RetinopathyR01EY018940 · NEI · UNIVERSITY OF COLORADO DENVER · PI KOMPELLA, UDAY B · 2010 to 2014
$2.4M
NEI NIH HHS R01 EY018940
6 · The paper itself

Abstract

While poorly soluble drugs such as corticosteroids sustain drug delivery in the vitreous humor by virtue of slow dissolution, macromolecules such as antibodies and their fragments sustain their levels due to their slow clearance. However, currently there are no approaches to sustain the delivery of well water soluble small molecule drugs in the vitreous. In this study we optimized a PLA microparticle formulation for sustained intravitreal delivery of TG-0054, a well water soluble anti-angiogenic drug that is of potential value in treating choroid neovascularization. After determining the influence of process parameters on particle size and drug loading, spherical microparticles syringeable through a 27 G needle, with a mean diameter of 7.6 μm, 10% w/w TG-0054 loading, sustained in vitro drug release for at least 6 months, and low residual organic solvent content (~ 1 ppb/mg) were prepared. Microparticles as well as drug solution were assessed for their in vivo drug delivery over 3 months following intravitreal injection in New Zealand white rabbits. Drug levels in the microparticle dosed eyes at 3 months were 43.7 ± 16.2, 243 ± 42.6, 62.8 ± 22.6 μg/g vitreous, retina, and choroid-RPE, respectively, and similar to levels at one month. Intravitreal injection of plain drug solution resulted in significantly lower amounts of drug in the dosed eye, with the levels being 0.8 ± 0.5, 2.7 ± 2.8, and 4.9± 4.2 μg/g in vitreous, retina, and choroid-RPE, respectively, at one month, with no detectable drug at three months. Although surface degradation was evident, microparticles maintained their spherical structure during the 6 months in vitro study and the 3 months in vivo study, with the vitreal particle retention at 1 and 3 months being 60% and 27%, respectively. Thus, PLA microparticles capable of sustaining retinal and choroidal delivery of TG-0054 for three to six months were developed.

Identifiers

PMID22888471
PMCPMC3416885
OpenAlexW2039200973

What OpenQuestion holds

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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.