ArticleAntimicrobial agents and chemotherapy2008
Intracellular time course, pharmacokinetics, and biodistribution of isoniazid and rifabutin following pulmonary delivery of inhalable microparticles to mice.
Article in Antimicrobial agents and chemotherapy, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 94 citations in OpenAlex.
- Review
- Novel regimens for treatment ofbioRxiv : the preprint server for biology · 2026Article
- Advancing Tuberculosis Chemotherapy: Targeted Nanomedicines for the Mycobacterium TB Granuloma.Small (Weinheim an der Bergstrasse, Germany) · 2025Review
- Ceftriaxone Efficacy for Mycobacterium avium Complex Lung Disease in the Hollow Fiber and Translation to Sustained Sputum Culture Conversion in Patients.The Journal of infectious diseases · 2024Article
- Antibiotic-Derived Radiotracers for Positron Emission Tomography: Nuclear or "Unclear" Infection Imaging?Angewandte Chemie (International ed. in English) · 2022Review
- Studies of the Specific Activity of Aerosolized Isoniazid against Tuberculosis in a Mouse Model.Antibiotics (Basel, Switzerland) · 2022Article
- Targeting Intracellular Mycobacteria Using Nanosized Niosomes Loaded with Antibacterial Agents.Nanomaterials (Basel, Switzerland) · 2021Article
- Pharmaceutical strategies to extend pulmonary exposure of inhaled medicines.Acta pharmaceutica Sinica. B · 2021Review
- Inhalable solid lipid nanoparticles for intracellular tuberculosis infection therapy: macrophage-targeting and pH-sensitive properties.Drug delivery and translational research · 2021Article
- Novel Assay Platform to Evaluate Intracellular Killing ofFrontiers in immunology · 2021Article
- Mannose receptor targeted bioadhesive chitosan nanoparticles of clofazimine for effective therapy of tuberculosis.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2020Article
- Modulating lung immune cells by pulmonary delivery of antigen-specific nanoparticles to treat autoimmune disease.Science advances · 2020Article
- In Vivo Biodistribution of Respirable Solid Lipid Nanoparticles Surface-Decorated with a Mannose-Based Surfactant: A Promising Tool for Pulmonary Tuberculosis Treatment?Nanomaterials (Basel, Switzerland) · 2020Article
- An Inhalable Theranostic System for Local Tuberculosis Treatment Containing an Isoniazid Loaded Metal Organic Framework Fe-MIL-101-NH2-From Raw MOF to Drug Delivery System.Pharmaceutics · 2019Article
- Functionalization of PLGA Nanoparticles with 1,3-β-glucan Enhances the Intracellular Pharmacokinetics of Rifampicin in Macrophages.Pharmaceutical research · 2018Article
- The Effects of First-Line Anti-Tuberculosis Drugs on the Actions of Vitamin D in Human Macrophages.Journal of clinical & translational endocrinology · 2016Article
- Targeted pulmonary delivery of inducers of host macrophage autophagy as a potential host-directed chemotherapy of tuberculosis.Advanced drug delivery reviews · 2016Review
- Systems Pharmacology Approach Toward the Design of Inhaled Formulations of Rifampicin and Isoniazid for Treatment of Tuberculosis.CPT: pharmacometrics & systems pharmacology · 2015Article
- A rifapentine-containing inhaled triple antibiotic formulation for rapid treatment of tubercular infection.Pharmaceutical research · 2014Article
- Buparvaquone loaded solid lipid nanoparticles for targeted delivery in theleriosis.Journal of pharmacy & bioallied sciences · 2014Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Intracellular concentrations of isoniazid and rifabutin resulting from administration of inhalable microparticles of these drugs to phorbol-differentiated THP-1 cells and the pharmacokinetics and biodistribution of these drugs upon inhalation of microparticles or intravenous administration of free drugs to mice were investigated. In cultured cells, both microparticles and dissolved drugs established peak concentrations of isoniazid ( approximately 1.4 and 1.1 microg/10(6) cells) and rifabutin ( approximately 2 microg/ml and approximately 1.4 microg/10(6) cells) within 10 min. Microparticles maintained the intracellular concentration of isoniazid for 24 h and rifabutin for 96 h, whereas dissolved drugs did not. The following pharmacokinetic parameters were calculated using WinNonlin from samples obtained after inhalation using an in-house apparatus (figures in parentheses refer to parameters obtained after intravenous administration of an equivalent amount, i.e., 100 microg of either drug, to parallel groups): isoniazid, serum half-life (t(1/2)) = 18.63 +/- 5.89 h (3.91 +/- 1.06 h), maximum concentration in serum (C(max)) = 2.37 +/- 0.23 microg x ml(-1) (3.24 +/- 0.57 microg x ml(-1)), area under the concentration-time curve from 0 to 24 h (AUC(0-24)) = 55.34 +/- 13.72 microg/ml(-1) h(-1) (16.64 +/- 1.80 microg/ml(-1) h(-1)), and clearance (CL) = 63.90 +/- 13.32 ml x h(-1) (4.43 +/- 1.85 ml x h(-1)); rifabutin, t(1/2) = 119.49 +/- 29.62 h (20.18 +/- 4.02 h), C(max) = 1.59 +/- 0.01 microg x ml(-1) (3.47 +/- 0.33 microg x ml(-1)), AUC(0-96) = 109.35 +/- 14.78 microg/ml(-1) h(-1) (90.82 +/- 7.46 microg/ml(-1) h(-1)), and CL = 11.68 +/- 7.00 ml x h(-1) (1.03 +/- 0.11 ml.h(-1)). Drug targeting to the lungs in general and alveolar macrophages in particular was observed. It was concluded that inhaled microparticles can reduce dose frequency and improve the pharmacologic index of the drug combination.
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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.