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19 Results Found

  • Article
  • Open Access
Pharmaceuticals2026, 19(2), 255;https://doi.org/10.3390/ph19020255 
(registering DOI)

1 February 2026

Background/Objectives: Topical treatment of cutaneous tuberculosis (CTB) requires reliable models to evaluate dermal drug release and diffusion, particularly for fixed-dose combinations (FDCs) with contrasting physicochemical properties. Human skin r...

  • Article
  • Open Access
11 Citations
2,698 Views
18 Pages

Tuberculosis (TB) is an airborne bacterial infection caused by Mycobacterium tuberculosis (M. tb), resulting in approximately 1.3 million deaths in 2022 worldwide. Oral therapy with anti-TB drugs often fails to achieve therapeutic concentrations at t...

  • Article
  • Open Access
17 Citations
5,506 Views
14 Pages

Synthesis and Characterization of a Biomimetic Formulation of Clofazimine Hydrochloride Microcrystals for Parenteral Administration

  • Mikhail D. Murashov,
  • Jennifer Diaz-Espinosa,
  • Vernon LaLone,
  • Joel W. Y. Tan,
  • Raluca Laza,
  • Xueding Wang,
  • Kathleen A. Stringer and
  • Gus R. Rosania

Clofazimine (CFZ) is a broad spectrum antimycobacterial agent recommended by the World Health Organization as a first line treatment for leprosy and second line treatment for multidrug resistant tuberculosis. Oral administration of CFZ leads to a red...

  • Article
  • Open Access
18 Citations
3,356 Views
9 Pages

30 March 2022

Recently, as clofazimine (CFZ) showed a good therapeutic effect in treating multi-drug-resistant tuberculosis (MDR-TB), the anti-tuberculosis activity and resistance were re-focused. Here, we investigated the CFZ resistance and genetic mutations of d...

  • Article
  • Open Access
8 Citations
2,777 Views
16 Pages

This study aimed to evaluate and compare the efficacy of cyclodextrans (CIs) and cyclodextrins (CDs) in improving the water solubility of a poorly water-soluble drug, clofazimine (CFZ). Among the evaluated CIs and CDs, CI-9 exhibited the highest perc...

  • Article
  • Open Access
1 Citations
1,996 Views
13 Pages

Distinguishing the Concentration- vs. Bioaccumulation-Dependent Immunological and Metabolic Effects of Clofazimine

  • Andrew R. Willmer,
  • Jennifer Diaz-Espinosa,
  • Austin Zhou,
  • Kathleen A. Stringer and
  • Gus R. Rosania

The antimycobacterial drug clofazimine (CFZ) is used as a single agent at high doses, to suppress the exaggerated inflammation associated with leprosy. Paradoxically, increasing doses of CFZ leads to bioaccumulation of CFZ in the spleen and other org...

  • Article
  • Open Access
5 Citations
3,314 Views
15 Pages

An Adaptive Biosystems Engineering Approach towards Modeling the Soluble-to-Insoluble Phase Transition of Clofazimine

  • Andrew R. Willmer,
  • Steven Dunne,
  • Rosemary Swanson,
  • Deepak Almeida,
  • Nicole C. Ammerman,
  • Kathleen A. Stringer,
  • Edmund V. Capparelli and
  • Gus R. Rosania

Clofazimine (CFZ) is a weakly basic, small-molecule antibiotic used for the treatment of mycobacterial infections including leprosy and multidrug-resistant tuberculosis. Upon prolonged oral administration, CFZ precipitates and accumulates within macr...

  • Article
  • Open Access
3 Citations
2,700 Views
15 Pages

Effects of Different Weak Small Organic Acids on Clofazimine Solubility in Aqueous Media

  • Igor A. Topalović,
  • Olivera S. Marković,
  • Miloš P. Pešić,
  • Mufaddal H. Kathawala,
  • Martin Kuentz,
  • Alex Avdeef,
  • Abu T. M. Serajuddin and
  • Tatjana Ž. Verbić

Background/Objectives: Clofazimine (CFZ) is a Biopharmaceutics Classification System (BCS) II drug introduced in the US market in 1986 for the treatment of leprosy. However, CFZ was later withdrawn from the market due to its extremely low aqueous sol...

  • Article
  • Open Access
2,183 Views
22 Pages

Sodium, Potassium-Adenosine Triphosphatase as a Potential Target of the Anti-Tuberculosis Agents, Clofazimine and Bedaquiline

  • Khomotso Mmakola,
  • Marissa Balmith,
  • Helen Steel,
  • Mohamed Said,
  • Moliehi Potjo,
  • Mieke van der Mescht,
  • Nomsa Hlatshwayo,
  • Pieter Meyer,
  • Gregory Tintinger and
  • Moloko Cholo
  • + 1 author

4 December 2024

Multidrug-resistant tuberculosis (MDR-TB) patients are treated with a standardised, short World Health Organization (WHO) regimen which includes clofazimine (CFZ) and bedaquiline (BDQ) antibiotics. These two antibiotics lead to the development of QT...

  • Article
  • Open Access
1,173 Views
18 Pages

Design of Clofazimine-Loaded Lipid Nanoparticles Using Smart Pharmaceutical Technology Approaches

  • Helena Rouco,
  • Nicola Filippo Virzì,
  • Carolina Menéndez-Rodríguez,
  • Carmen Potel,
  • Patricia Diaz-Rodriguez and
  • Mariana Landin

Background/Objectives: Clofazimine (CFZ) is a versatile antimicrobial active against several bacterial species, although its reduced aqueous solubility and the occurrence of side effects limit its use. Nanostructured lipid carriers (NLCs) constitute...

  • Article
  • Open Access
1,577 Views
15 Pages

Assessing the Impact of Bedaquiline, Clofazimine, and Linezolid on Mycobacterial Genome Integrity

  • Dániel Molnár,
  • Éva Viola Surányi,
  • Nikoletta Gálik,
  • Judit Tóth and
  • Rita Hirmondó

15 November 2024

Tuberculosis (TB) presents significant medical challenges, largely due to the genetic diversity of Mycobacterium tuberculosis, which enhances the resilience and resistance of the pathogen to first-line treatments. In response to the global rise of dr...

  • Article
  • Open Access
4 Citations
3,351 Views
18 Pages

Quantitative Analysis of the Phase Transition Mechanism Underpinning the Systemic Self-Assembly of a Mechanopharmaceutical Device

  • Steven Dunne,
  • Andrew R. Willmer,
  • Rosemary Swanson,
  • Deepak Almeida,
  • Nicole C. Ammerman,
  • Kathleen A. Stringer,
  • Edmund V. Capparelli and
  • Gus R. Rosania

Clofazimine (CFZ) is a poorly soluble, weakly basic, small molecule antibiotic clinically used to treat leprosy and is now in clinical trials as a treatment for multidrug resistant tuberculosis and COVID-19. CFZ exhibits complex, context-dependent ph...

  • Article
  • Open Access
1 Citations
2,218 Views
12 Pages

Clofazimine-Mediated, Age-Related Changes in Skeletal Muscle Mitochondrial Metabolites

  • Jennifer Diaz-Espinosa,
  • Kathleen A. Stringer and
  • Gus R. Rosania

Mitochondrial health declines with age, and older patients can demonstrate dysfunction in mitochondrial-rich tissues, such as cardiac and skeletal muscle. Aged mitochondria may make older adults more susceptible to adverse drug reactions (ADRs). We a...

  • Article
  • Open Access
4 Citations
1,894 Views
13 Pages

Triple-Antibiotic Combination Exerts Effective Activity against Mycobacterium avium subsp. hominissuis Biofilm and Airway Infection in an In Vivo Murine Model

  • Elliot M. Offman,
  • Amy Leestemaker-Palmer,
  • Reza Fathi,
  • Bailey Keefe,
  • Aida Bibliowicz,
  • Gilead Raday and
  • Luiz E. Bermudez

Objectives: Slow-growing nontuberculous mycobacteria (NTMs) are highly prevalent and routinely cause opportunistic intracellular infectious disease in immunocompromised hosts. Methods: The activity of the triple combination of antibiotics, clarithrom...

  • Article
  • Open Access
16 Citations
3,874 Views
12 Pages

Outcomes of Inhaled Amikacin and Clofazimine-Containing Regimens for Treatment of Refractory Mycobacterium avium Complex Pulmonary Disease

  • Bo-Guen Kim,
  • Hojoong Kim,
  • O. Jung Kwon,
  • Hee Jae Huh,
  • Nam Yong Lee,
  • Sun-Young Baek,
  • Insuk Sohn and
  • Byung Woo Jhun

14 September 2020

Limited data are available regarding optimal treatment for refractory Mycobacterium avium complex-pulmonary disease (MAC-PD). We evaluated outcomes of inhaled amikacin (AMK) with clofazimine (CFZ) regimens as an add-on salvage therapy for refractory...

  • Article
  • Open Access
122 Views
23 Pages

21 January 2026

Reversed-phase high-performance liquid chromatography (RP-HPLC) remains one of the most widely applied analytical techniques in the development and quality control testing of finished pharmaceutical products. The combination of gradient chromatograph...

  • Review
  • Open Access
25 Citations
5,217 Views
15 Pages

MmpL3 Inhibition as a Promising Approach to Develop Novel Therapies against Tuberculosis: A Spotlight on SQ109, Clinical Studies, and Patents Literature

  • Mohd. Imran,
  • Mandeep Kumar Arora,
  • Anurag Chaudhary,
  • Shah Alam Khan,
  • Mehnaz Kamal,
  • Manal Mutlaq Alshammari,
  • Raghad Mohammad Alharbi,
  • Nuha Abdullah Althomali,
  • Ibrahim Mohammed Alzimam and
  • Ali A. Rabaan
  • + 5 authors

Tuberculosis (TB) is accountable for considerable global morbidity and mortality. Effective TB therapy with multiple drugs completes in about six months. The longer duration of TB therapy challenges patient compliance and contributes to treatment col...

  • Article
  • Open Access
2 Citations
2,800 Views
21 Pages

25 September 2023

Self-emulsifying drug delivery systems (SEDDSs) are lipid-based systems that are superior to other lipid-based oral drug delivery systems in terms of providing drug protection against the gastrointestinal (GI) environment, inhibition of drug efflux a...

  • Review
  • Open Access
573 Views
26 Pages

Targeted next-generation sequencing (tNGS) closes the gap between point-of-care rapid tests and phenotypic drug susceptibility testing (pDST) in drug-resistant tuberculosis (DR-TB). The 2025 World Health Organization (WHO) consolidated guidelines and...