ArticleMolecular pharmaceutics2011
Molecular imaging of intracellular drug-membrane aggregate formation.
Article in Molecular pharmaceutics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
What it found
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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.
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.
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Who cites it
34 citing papers in PubMed, 60 citations in OpenAlex.
- Facilitated Transport of EGFR Inhibitors Plays an Important Role in Their Cellular Uptake.Analytical chemistry · 2024Article
- Database screening as a strategy to identify endogenous candidate metabolites to probe and assess mitochondrial drug toxicity.Scientific reports · 2023Article
- Quantitative Raman chemical imaging of intracellular drug-membrane aggregates and small molecule drug precipitates in cytoplasmic organelles.Advanced drug delivery reviews · 2023Review
- Distinguishing the Concentration- vs. Bioaccumulation-Dependent Immunological and Metabolic Effects of Clofazimine.Pharmaceutics · 2023Article
- Clofazimine-Mediated, Age-Related Changes in Skeletal Muscle Mitochondrial Metabolites.Metabolites · 2023Article
- Quantitative chemometric phenotyping of three-dimensional liver organoids by Raman spectral imaging.Cell reports methods · 2023Article
- Clofazimine for the treatment of tuberculosis.Frontiers in pharmacology · 2023Review
- Respirable Clofazimine Particles Produced by Air Jet Milling Technique Are Efficacious in Treatment of BALB/c Mice with Chronic Mycobacterium tuberculosis Infection.Antimicrobial agents and chemotherapy · 2022Article
- The Effect of Tuberculosis Antimicrobials on the Immunometabolic Profiles of Primary Human Macrophages Stimulated withInternational journal of molecular sciences · 2021Article
- Host-Directed FDA-Approved Drugs with Antiviral Activity against SARS-CoV-2 Identified by Hierarchical In Silico/In Vitro Screening Methods.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Review
- Clofazimine is a broad-spectrum coronavirus inhibitor that antagonizes SARS-CoV-2 replication in primary human cell culture and hamsters.Research square · 2020Article
- Clofazimine Reduces the Survival ofACS infectious diseases · 2020Article
- Revealing Drug Self-Associations into Nano-Entities.ACS omega · 2019Article
- Photoacoustic imaging of clofazimine hydrochloride nanoparticle accumulation in cancerous vs normal prostates.PloS one · 2019Article
- Synthesis and Characterization of a Biomimetic Formulation of Clofazimine Hydrochloride Microcrystals for Parenteral Administration.Pharmaceutics · 2018Article
- The Physicochemical Basis of Clofazimine-Induced Skin Pigmentation.The Journal of investigative dermatology · 2018Article
- Reverse Engineering the Intracellular Self-Assembly of a Functional Mechanopharmaceutical Device.Scientific reports · 2018Article
- Macrophage-Mediated Clofazimine Sequestration Is Accompanied by a Shift in Host Energy Metabolism.Journal of pharmaceutical sciences · 2017Article
- New insights into the intracellular distribution pattern of cationic amphiphilic drugs.Scientific reports · 2017Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Clofazimine is a lipophilic antibiotic with an extremely long pharmacokinetic half-life associated with the appearance of crystal-like drug inclusions, in vivo. Here, we studied how clofazimine accumulates inside cells in the presence of supersaturating, extracellular concentrations of the drug (in the range of physiological drug concentrations). Based on a combination of molecular imaging, biochemical analysis and electron microscopy techniques, clofazimine mass increased inside cells in vitro, over a period of several days, with discrete clofazimine inclusions forming in the cytoplasm. These inclusions grew in size, number and density, as long as the drug-containing medium was replenished. With Raman confocal microscopy, clofazimine's spectral signature in these inclusions resembled that of amorphous clofazimine precipitates and was unlike that of clofazimine crystals. Additional experiments revealed that clofazimine first accumulated in mitochondria, with ensuing changes in mitochondrial structure and function. In turn, the degenerating organelles coalesced, fused with each other and condensed to form prominent drug-membrane aggregates (dubbed autophagosome-like drug inclusions or "aldis"). Like clofazimine, it is possible that intracellular drug-membrane aggregate formation is a common phenomenon underlying the reported phenotypic effects of many other small molecule drugs.
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Registered trials
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.