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Akademický článek

Macrophages sequester clofazimine in an intracellular liquid crystal-like supramolecular organization.

Autor: Jason Baik, Gus R Rosania

Publikováno v: PLoS ONE, Vol 7, Iss 10, p e47494 (2012)

Clofazimine is a poorly-soluble but orally-bioavailable small molecule drug that massively accumulates in macrophages when administered over prolonged periods of time. To determine whether crystal-like drug inclusions (CLDIs) that form in subcellular

Externí odkaz: https://doaj.org/article/6d048e47a30846b4a8924217e9d5c795

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An Expandable Mechanopharmaceutical Device (1): Measuring the Cargo Capacity of Macrophages in a Living Organism

Autor: Tehetina Woldemichael, Phillip Rzeczycki, Andrew R. Willmer, Mikhail D. Murashov, Rahul K. Keswani, Naír Rodríguez-Hornedo, Kathleen A. Stringer, Gus R. Rosania, Jason Baik, Gi Sang Yoon

Publikováno v: Pharmaceutical Research. 36

PURPOSE: Clofazimine (CFZ) is an FDA-approved, poorly soluble small molecule drug that precipitates as crystal-like drug inclusions (CLDIs) which accumulate in acidic cytoplasmic organelles of macrophages. In this study, we considered CLDIs as an exp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3fa7de0a70ed16ed3338c2d70fd9268f
https://doi.org/10.1007/s11095-018-2539-6

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An Expandable Mechanopharmaceutical Device (2): Drug Induced Granulomas Maximize the Cargo Sequestering Capacity of Macrophages in the Liver

Autor: Rahul K. Keswani, Gi Sang Yoon, Mikhail D. Murashov, Ingrid L. Bergin, Phillip Rzeczycki, Gus R. Rosania, Kathleen A. Stringer, Jason Baik, Sudha Sud

Publikováno v: Pharmaceutical research. 36(1)

PURPOSE: Drug-induced liver injuries (DILI) comprise a significant proportion of adverse drug reactions leading to hospitalizations and death. One frequent DILI is granulomatous inflammation from exposure to harmful metabolites that activate inflamma

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::122aa933dad4e931c072e9c0f66dc9f0
https://pubmed.ncbi.nlm.nih.gov/30406478

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Molecular Imaging of Intracellular Drug–Membrane Aggregate Formation

Autor: Jason Baik, Gus R. Rosania

Publikováno v: Molecular Pharmaceutics. 8:1742-1749

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 supersaturat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c258eece09d15d2ada128b3ff57a3fa5
https://doi.org/10.1021/mp200101b

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Chemical Analysis of Drug Biocrystals: A Role for Counterion Transport Pathways in Intracellular Drug Disposition

Autor: Chuck Hitzman, Rahul K. Keswani, Kathleen A. Stringer, Gus R. Rosania, Jason Baik, Naír Rodríguez-Hornedo, Larisa Yeomans, Allison M. Johnson, Ashtamurthy S. Pawate, Paul J. A. Kenis

In mammals, highly lipophilic small molecule chemical agents can accumulate as inclusions within resident tissue macrophages. In this context, we characterized the biodistribution, chemical composition and structure of crystal-like drug inclusions (C

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92363be562d99305eda8938f9d7575b6
https://europepmc.org/articles/PMC4568831/

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Phagocytosed Clofazimine Biocrystals Can Modulate Innate Immune Signaling by Inhibiting TNFα and Boosting IL-1RA Secretion

Autor: Jason Baik, Kathleen A. Stringer, Theodore J. Standiford, Rahul K. Keswani, Sudha Sud, Gi Sang Yoon, Gus R. Rosania

Publikováno v: Molecular pharmaceutics. 12(7)

Clofazimine (CFZ) is an FDA-approved leprostatic and anti-inflammatory drug that massively accumulates in macrophages, forming insoluble, intracellular crystal-like drug inclusions (CLDIs) during long-term oral dosing. Interestingly, when added to ce

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7e4732b494e3163799d319eeae097db
https://pubmed.ncbi.nlm.nih.gov/25909959

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Multiscale distribution and bioaccumulation analysis of clofazimine reveals a massive immune system-mediated xenobiotic sequestration response

Autor: Gerta Mane, Gus R. Rosania, Kathleen A. Stringer, Jason Baik

Publikováno v: Antimicrobial agents and chemotherapy. 57(3)

Chronic exposure to some well-absorbed but slowly eliminated xenobiotics can lead to their bioaccumulation in living organisms. Here, we studied the bioaccumulation and distribution of clofazimine, a riminophenazine antibiotic used to treat mycobacte

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da37bb0e93817a395a82c82512b24499
https://pubmed.ncbi.nlm.nih.gov/23263006

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