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Record W4416867113 · doi:10.1016/j.ijpharm.2025.126448

Dual activity of low-molecular-weight polymeric β-cyclodextrins against tuberculosis

2025· article· en· W4416867113 on OpenAlexfundno aff
Amine Pochet, Jesus Alfredo Godinez-Leon, Tahmida Shamsuddin, Priscille Brodin, Ruxandra Gref, Arnaud Machelart

Bibliographic record

VenueInternational Journal of Pharmaceutics · 2025
Typearticle
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicDrug Solubulity and Delivery Systems
Canadian institutionsnot available
FundersHorizon 2020Dairy Research IrelandRégion Hauts-de-FranceInstitut du Cerveau et de la Moelle EpinièreAgence Nationale de la RechercheConsejo Nacional de Ciencia y TecnologíaInnovative Medicines InitiativeUniversity of DundeeConseil National de la Recherche ScientifiqueInnovative Health InitiativeEntomological Society of CanadaFondation pour la Recherche MédicaleInstitut National de la Santé et de la Recherche MédicaleAgence Nationale de Recherches sur le Sida et les Hépatites ViralesEuropean Federation of Pharmaceutical Industries and AssociationsBill and Melinda Gates Foundation
KeywordsMycobacterium tuberculosisTuberculosisAntimicrobialDrugDrug deliveryAdverse effectAnti-Infective AgentsExtensively drug-resistant tuberculosisDrug development

Abstract

fetched live from OpenAlex

Tuberculosis remains the leading cause of death from infectious diseases. While effective therapies are available, their prolonged duration and severe adverse effects compromise patient adherence and promote antimicrobial resistance, highlighting the urgent need for innovative therapeutic approaches. We previously identified polymeric β-cyclodextrin (pβCD) as a promising drug delivery platform, possessing intrinsic antibacterial activity and serving as a carrier for the second-line drug ethionamide. Here, we investigated the biological properties of pβCD of different molecular weights. Strikingly, only the low-molecular-weight pβCD (LMW-pβCD) displayed antibacterial activity, in contrast to the high-molecular-weight one. Mechanistically, this activity was linked to the inhibition of Mycobacterium tuberculosis entry into macrophages through disruption of lipid rafts. Transcriptomic profiling further revealed that the LMW-pβCD also enhanced pro-inflammatory cytokine secretion, suggesting dual antimicrobial and immunomodulatory functions. Notably, linezolid, an important second-line anti-tuberculosis drug, was efficiently incorporated in pβCD, regardless of its molecular weight. These findings emphasize the critical importance of molecular weight in dictating pβCD bioactivity. Only LMW-pβCD combines antimicrobial and immunomodulatory activities with effective drug delivery, making it a promising candidate for the development of novel anti-tuberculosis therapies.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.001
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.106
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0010.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0010.000
Research integrity0.0000.001
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.050
GPT teacher head0.430
Teacher spread0.380 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations0
Published2025
Admission routes1
Has abstractyes

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