Evidence map›Paper›PMID 33255979›Full record

ArticlePharmaceutics2020

Drug-Nutraceutical Co-Crystal and Salts for Making New and Improved Bi-Functional Analgesics.

Oli Abate Fulas, André Laferrière, Ghada Ayoub, Dayaker Gandrath, Cristina Mottillo, Hatem M Titi, Robin S Stein, Tomislav Friščić, Terence J Coderre

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Pharmaceutics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

  1. Review
  2. Review
  3. Review
  4. 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

9 authors.

Oli Abate FulasDepartment of Anesthesia, McGill University, 3655 Promenade Sir William Osler, Montreal, QC H3G 1Y6, Canada.
André LaferrièreDepartment of Anesthesia, McGill University, 3655 Promenade Sir William Osler, Montreal, QC H3G 1Y6, Canada.
Ghada AyoubDepartment of Chemistry, McGill University, 801 Sherbrooke Street W, Montreal, QC H3A 0B8, Canada.
Dayaker GandrathDepartment of Chemistry, McGill University, 801 Sherbrooke Street W, Montreal, QC H3A 0B8, Canada.
Cristina MottilloDepartment of Chemistry, McGill University, 801 Sherbrooke Street W, Montreal, QC H3A 0B8, Canada.ORCID 0000-0002-0291-7387
Hatem M TitiDepartment of Chemistry, McGill University, 801 Sherbrooke Street W, Montreal, QC H3A 0B8, Canada.
Robin S SteinDepartment of Chemistry, McGill University, 801 Sherbrooke Street W, Montreal, QC H3A 0B8, Canada.
Tomislav FriščićDepartment of Chemistry, McGill University, 801 Sherbrooke Street W, Montreal, QC H3A 0B8, Canada.ORCID 0000-0002-3921-7915
Terence J CoderreDepartment of Anesthesia, McGill University, 3655 Promenade Sir William Osler, Montreal, QC H3G 1Y6, Canada.

Funding

CIHR MOP-119279Louise and Alan Edwards Foundation N/ANatural Sciences and Engineering Research Council of Canada RGPIN/05605, RGPIN-2017-06467, RGPAS 507837-17
6 · The paper itself

Abstract

The discovery and development of effective analgesics is greatly lagging behind the steadily rising prevalence of chronic pain. Currently prescribed analgesics for chronic pain are lacking in efficacy mainly due to their narrowly-targeted mechanism of action. Driving neuronal hyperexcitability that underlies symptoms of chronic pain are multiple non-neuronal processes, among which are tissue hypoxia and oxidative stress. Here we demonstrate the design, synthesis, and activity of new multi-component bi-functional analgesic crystalline solids, co-crystals, and salts, based on pairing of vasodilatory anti-hypoxic drugs pentoxifylline, clonidine and linsidomine with antioxidant nutraceuticals protocatechuic acid, α-lipoic acid, and caffeic acid. After validation, chemical and structural characterization of these novel salts and co-crystals, topical formulations of the products were tested in a rat model of complex regional pain syndrome. Analgesic effects achieved with the salts and co-crystal exceeded the efficacy and/or potency of constituent compounds indicating that more effective, advanced analgesics can readily be developed by careful pairing of compounds that simultaneously target multiple neural and non-neural processes driving chronic pain.

Indexed as

antioxidantsco-crystalCRPSmechanochemistryneuropathic paintopical analgesicsvasodilators

Identifiers

PMID33255979
PMCPMC7761172

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Registered trials

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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.