Evidence map›Paper›PMID 39079659›Full record

ArticleJournal of controlled release : official journal of the Controlled Release Society2024

Evaluation of Pregabalin bioadhesive multilayered microemulsion IOP-lowering eye drops.

Doaa N Maria, Mohamed M Ibrahim, Minjae J Kim, Sara N Maria, William A White, XiangDi Wang, T J Hollingsworth, Monica M Jablonski

Abstract read
In one paragraph

Article in Journal of controlled release : official journal of the Controlled Release Society, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
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

3 citing papers in PubMed.

  1. Article
  2. Article
  3. 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

8 authors.

Doaa N MariaDepartment of Ophthalmology, Hamilton Eye Institute, University of Tennessee Health Science Center, Memphis, TN 38163, United States; Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Mohamed M IbrahimDepartment of Ophthalmology, Hamilton Eye Institute, University of Tennessee Health Science Center, Memphis, TN 38163, United States; Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Minjae J KimDepartment of Ophthalmology, Hamilton Eye Institute, University of Tennessee Health Science Center, Memphis, TN 38163, United States.
Sara N MariaDepartment of Ophthalmology, Hamilton Eye Institute, University of Tennessee Health Science Center, Memphis, TN 38163, United States; Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt; Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 38163, United States.
William A WhiteDepartment of Ophthalmology, Hamilton Eye Institute, University of Tennessee Health Science Center, Memphis, TN 38163, United States.
XiangDi WangDepartment of Ophthalmology, Hamilton Eye Institute, University of Tennessee Health Science Center, Memphis, TN 38163, United States.
T J HollingsworthDepartment of Ophthalmology, Hamilton Eye Institute, University of Tennessee Health Science Center, Memphis, TN 38163, United States.
Monica M JablonskiDepartment of Ophthalmology, Hamilton Eye Institute, University of Tennessee Health Science Center, Memphis, TN 38163, United States; Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 38163, United States. Electronic address: mjablonski@uthsc.edu.

Funding

Novel Extended Release Glaucoma Therapy for Once Daily DosingR24EY029950 · NEI · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI JABLONSKI, MONICA M · 2020 to 2024
$5.3M
Mass Spectrometer for Small Molecule Drug DevelopmentS10OD016226 · OD · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI MEIBOHM, BERND · 2014 to 2014
$316k
NEI NIH HHS R24 EY029950NIH HHS S10 OD016226
6 · The paper itself

Abstract

In spite of available treatment options, glaucoma continues to be a leading cause of irreversible blindness in the world. Current glaucoma medications have multiple limitations including: lack of sustained action; requirement for multiple dosing per day, ocular irritation and limited options for drugs with different mechanisms of action. Previously, we demonstrated that pregabalin, a drug with high affinity and selectivity for CACNA2D1, lowered IOP in a dose-dependent manner. The current study was designed to evaluate pregabalin microemulsion eye drops and to estimate its efficacy in humans using in silico methods. Molecular docking studies of pregabalin against CACNA2D1 of mouse, rabbit, and human were performed. Pregabalin microemulsion eye drops were characterized using multiple in vivo studies and its stability was evaluated over one year at different storage conditions. Molecular docking analyses and QSPR of pregabalin confirmed its suitability as a new IOP-lowering medication that functions using a new mechanism of action by binding to CACNA2D1 in all species evaluated. Because of its prolonged corneal residence time and corneal penetration enhancement, a single topical application of pregabalin ME can provide an extended IOP reduction of more than day in different animal models. Repeated daily dosing for 2 months confirms the lack of any tachyphylactic effect, which is a common drawback among marketed IOP-lowering medications. In addition, pregabalin microemulsion demonstrated good physical stability for one year, and chemical stability for 3-6 months if stored below 25 °C. Collectively, these outcomes greatly support the use of pregabalin eye drops as once daily IOP-lowering therapy for glaucoma management.

Indexed as

EmulsionsIntraocular PressureMolecular Docking SimulationOphthalmic SolutionsPregabalinAdministration, OphthalmicAnimalsAntihypertensive AgentsCorneaDrug StabilityFemaleGlaucomaHumansMaleMiceRabbitsAntihypertensive AgentsEmulsionsOphthalmic SolutionsPregabalinFluorescent immunohistochemistryIn vivoMicroemulsionMolecular dockingPharmacokineticSecond order degradation kinetics

Identifiers

PMID39079659
PMCPMC11384292

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.