ArticleMolecular pharmaceutics2017
Design and Solidification of Fast-Releasing Clofazimine Nanoparticles for Treatment of Cryptosporidiosis.
Article in Molecular pharmaceutics, 2017. 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, 68 citations in OpenAlex.
- Quality-by-Design Development of a Clofazimine-Pyrazinamide Dermal Emulsion and Its Diffusion Behavior in Strat-MPharmaceuticals (Basel, Switzerland) · 2026Article
- RP-DAD-HPLC Method for Quantitative Analysis of Clofazimine and Pyrazinamide for Inclusion in Fixed-Dose Combination Topical Drug Delivery System.Methods and protocols · 2026Article
- Unraveling Lyophilization and Redispersion Effects on Miktoarm Polymer-Based Nanoformulations.International journal of molecular sciences · 2025Article
- Fabrication and optimization of itraconazole-loaded zein-based nanoparticles in coated capsules as a promising colon-targeting approach pursuing opportunistic fungal infections.Drug delivery and translational research · 2023Article
- Flash NanoPrecipitation as an Agrochemical Nanocarrier Formulation Platform: Phloem Uptake and Translocation after Foliar Administration.ACS agricultural science & technology · 2023Article
- Development of a HPLC Method for Analysis of a Combination of Clofazimine, Isoniazid, Pyrazinamide, and Rifampicin Incorporated into a Dermal Self-Double-Emulsifying Drug Delivery System.Methods and protocols · 2023Article
- In vitro and in vivo evaluation of dual Clofazimine and Verapamil loaded PLGA nanoparticles.Indian journal of clinical biochemistry : IJCB · 2023Article
- Formulation and Scale-up of Delamanid Nanoparticles via Emulsification for Oral Tuberculosis Treatment.Molecular pharmaceutics · 2023Article
- Improving the Antimycobacterial Drug Clofazimine through Formation of Organic Salts by Combination with Fluoroquinolones.International journal of molecular sciences · 2023Article
- Formulation of pH-Responsive Methacrylate-Based Polyelectrolyte-Stabilized Nanoparticles for Applications in Drug Delivery.ACS applied nano materials · 2022Article
- Small-volumeInternational journal of pharmaceutics: X · 2022Article
- Adapting Clofazimine for Treatment of Cutaneous Tuberculosis by Using Self-Double-Emulsifying Drug Delivery Systems.Antibiotics (Basel, Switzerland) · 2022Review
- Pharmacokinetics and Pharmacodynamics of Clofazimine for Treatment of Cryptosporidiosis.Antimicrobial agents and chemotherapy · 2022Article
- An Overview of Mucosa-Associated Protozoa: Challenges in Chemotherapy and Future Perspectives.Frontiers in cellular and infection microbiology · 2022Review
- Clofazimine-Loaded Mucoadhesive Nanoparticles Prepared by Flash Nanoprecipitation for Strategic Intestinal Delivery.Pharmaceutical research · 2021Article
- Polymeric and Lipid Nanoparticles: Which Applications in Pediatrics?Pharmaceutics · 2021Review
- Rifabutin-Loaded Nanostructured Lipid Carriers as a Tool in Oral Anti-Mycobacterial Treatment of Crohn's Disease.Nanomaterials (Basel, Switzerland) · 2020Article
- Nanoparticles for antiparasitic drug delivery.Drug delivery · 2019Review
- Translational formulation of nanoparticle therapeutics from laboratory discovery to clinical scale.Journal of translational medicine · 2019Article
- Solid-State Behavior and Solubilization of Flash Nanoprecipitated Clofazimine Particles during the Dispersion and Digestion of Milk-Based Formulations.Molecular pharmaceutics · 2019Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Clofazimine, a lipophilic (log P = 7.66) riminophenazine antibiotic approved by the US Food and Drug Administration (FDA) with a good safety record, was recently identified as a lead hit for cryptosporidiosis through a high-throughput phenotypic screen. Cryptosporidiosis requires fast-acting treatment as it leads to severe symptoms which, if untreated, result in morbidity for infants and small children. Consequently, a fast-releasing oral formulation of clofazimine in a water-dispersible form for pediatric administration is highly desirable. In this work, clofazimine nanoparticles were prepared with three surface stabilizers, hypromellose acetate succinate (HPMCAS), lecithin, and zein, using the flash nanoprecipitation (FNP) process. Drug encapsulation efficiencies of over 92% were achieved. Lyophilization and spray-drying were applied and optimized to produce redispersible nanoparticle powders. The release kinetics of these clofazimine nanoparticle powders in biorelevant media were measured and compared with those of crystalline clofazimine and the currently marketed formulation Lamprene. Remarkably improved dissolution rates and clofazimine supersaturation levels up to 90 times equilibrium solubility were observed with all clofazimine nanoparticles tested. Differential scanning calorimetry indicated a reduction of crystallinity of clofazimine in nanoparticles. These results strongly suggest that the new clofazimine nanoparticles prepared with affordable materials in this low-cost nanoparticle formulation process can be used as viable cryptosporidiosis therapeutics.
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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.