- |||||||||| Luzu (luliconazole) / Bausch Health, Cresemba (isavuconazonium sulfate) / Astellas, Basilea, Pfizer, Laboratoire Riva, Asahi Kasei
Preclinical, Journal: Comparison of in vitro activities of newer triazoles and classic antifungal agents against dermatophyte species isolated from Iranian University Hospitals: a multi-central study. (Pubmed Central) - Feb 27, 2023
Trichophyton mentagrophytes, Trichophyton interdigitale, and Trichophyton rubrum were the most common fungal species isolated from the patients. luliconazole, terbinafine, and isavuconazole in vitro were revealed to be the most effective antifungal agents against all dermatophyte isolates.
- |||||||||| griseofulvin / Generic mfg.
Journal: Nanoseeded Desupersaturation and Dissolution Tests for Elucidating Supersaturation Maintenance in Amorphous Solid Dispersions. (Pubmed Central) - Feb 25, 2023
This study examines the impacts of the seed size loading on the solution-mediated precipitation from griseofulvin ASDs...In the dissolution tests, only the Sol-based ASDs generated significant supersaturation, which decreased upon an increase in the nanoseed loading. This study has demonstrated the importance of using drug nanocrystals in lieu of conventional coarse crystals in desupersaturation and dissolution tests in ASD development.
- |||||||||| griseofulvin / Generic mfg.
Synthesis of spirocarbocycles utilizing an intramolecular interrupted homo Nazarov cascade cyclization (Room 201 (Indiana Convention Center)) - Feb 14, 2023 - Abstract #ACSSp2023ACS_SP_7082;
In particular, spirocarbocycles have shown potent antibacterial properties with griseofulvin being designated a WHO essential medicine...Herein, we showcase an unprecedented approach to spirocarbocycles that involves an intramolecular interrupted homo Nazarov cascade cyclization of aryl-tethered alkenyl cyclopropyl ketones. Polycyclic spirocarbocycles with variable substitution patterns and functionalities were found to be readily accessible.
- |||||||||| griseofulvin / Generic mfg.
Journal: Preparation of Free-Flowing Spray-Dried Amorphous Composites Using Neusilin. (Pubmed Central) - Jan 27, 2023
Griseofulvin (GF) is applied as a model BCS class 2 drug in ASDs...Lastly, the AC powders retained a fully amorphous state of GF after 3-month ambient storage. The overall results conveyed that the improved flowability and dissolution rate could outweigh the loss of drug loading resulted by addition of Neusilin.
- |||||||||| griseofulvin / Generic mfg.
Preclinical, Journal: Endophytic Fungus of Achyrocline satureioides: Molecular Identification, Chemical Characterization, and Cytotoxic Evaluation of its Metabolites in Human Melanoma cell line. (Pubmed Central) - Jan 19, 2023
in the production of isocoumarin orthosporin; the terpenoids nigriterpene A and 10-xylariterpenoid; the polyketide derivatives daldinin C, 7'dechloro-5'-hydroxygriseofulvin, daldinone D, Sch-642305, curtachalasin A, cytochalasin E, epoxycytochalasins Z8, Z8 isomer, and Z17...Given its ability to produce unique metabolites with promising cytotoxic effects, Biscogniauxia sp. of A. satureioides may be a reservoir of compounds with important therapeutic applications.
- |||||||||| fluconazole oral / Generic mfg., griseofulvin / Generic mfg., itraconazole / Generic mfg.
Journal: Neonatal-Onset Inflammatory Tinea Capitis by Microsporum canis Due to a Woolen Hat. (Pubmed Central) - Jan 17, 2023
Griseofulvin, itraconazole and fluconazole have been reported to be effective drugs for the treatment of children tinea capitis. Liver enzymes should be regularly monitored during the period of using antifungal agents.
- |||||||||| griseofulvin / Generic mfg.
Journal: Antifungal polyketides from the marine-derived fungus Nigrospora sp. MG36-1. (Pubmed Central) - Dec 27, 2022
Three new polyketides, a griseofulvin derivative 1, a hydroanthraquinone derivative 8 and a pyranolactone derivative 10, together with eight known compounds (2-7, 9 and 11), were isolated from the marine-derived fungus Nigrospora sp...Compound 1 showed antibacterial activity against Acinetobacter baumannii with MIC 42.5 μg/mL. Compounds 1 and 8 exhibited antifungal activity against Candida albicans with MICs 21.5 μg/mL and 17.5 μg/mL, respectively.
- |||||||||| PK/PD data, Journal: Design, Synthesis, SAR, Pharmacokinetic Prediction of New 4-Quinolones as Anti-Microbial Agents. (Pubmed Central) - Nov 22, 2022
The presence of halogen elements plays a key role in the biological activity that is clear by in vitro analysis. Target compounds exhibit moderate to significant activity near to standard marketed drugs like amoxycillin, chloramphenicol, ciprofloxacin, norfloxacin, griseofulvin, and nystatin.
- |||||||||| griseofulvin / Generic mfg.
Journal: Dose Titration of Solid Dosage Forms via FDM 3D-Printed Mini-Tablets. (Pubmed Central) - Nov 15, 2022
Griseofulvin, as a model poorly water-soluble drug, and hydroxypropyl cellulose along with Kollicoat Protect as polymers were used to prepare filaments at 1-20% drug concentrations via hot-melt extrusion (HME)...In contrast, split tablets demonstrated different release behaviors, attributed to their size and shape differences. Overall, the distinct advantages of mini-tablets to provide dose flexibility while maintaining similar release profiles was demonstrated.
- |||||||||| griseofulvin / Generic mfg.
Journal: Modeling of Particle Dissolution Behavior Using a Geometrical Phase-Field Approach. (Pubmed Central) - Nov 9, 2022
A diffusion-limited model compound, xylitol, with a high aqueous solubility and a surface reaction-limited model compound, griseofulvin, with a low aqueous solubility were chosen. The results of the simulations demonstrated that phase-field modeling is a powerful approach for predicting the dissolution behaviors of pure crystalline substances.
- |||||||||| griseofulvin / Generic mfg., paracetamol / Generic mfg.
Preclinical, Journal: Development of an In Vitro System To Emulate an In Vivo Subcutaneous Environment: Small Molecule Drug Assessment. (Pubmed Central) - Nov 9, 2022
Via conducting a DoE factor screening study using acetaminophen solution, the relationship of the output (drug release from the "SC" chamber to the "blood circulation" chamber) and the input parameters could be modeled using a variety of methods, including polynomial equations, machine learning methods, and Monte Carlo simulation-based methods...An in vitro-in vivo correlation (IVIVC) study was developed using griseofulvin suspension to explore the feasibility of applying ESCAR in formulation development and bioequivalence studies...In conclusion, ESCAR had important implications for research and development and quality control of SC drug products. Future work would be focused on further optimizing ESCAR and expanding its applications via assessing more types of molecules and formulations.
- |||||||||| griseofulvin / Generic mfg.
Review, Journal: Griseofulvin: An Updated Overview of Old and Current Knowledge. (Pubmed Central) - Oct 28, 2022
Therefore, they could be responsible for liver injury and Mallory body (MB) formation in hepatocytes of human, mouse, and rat treated with griseofulvin. Moreover, the stronger binding of griseofulvin to K18 in rodents than in human may explain the observed difference in the severity of hepatitis between rodents and human.
- |||||||||| griseofulvin / Generic mfg.
Journal: Antifungal nanosuspensions with surfactants and silver for the treatment of onychomycosis. (Pubmed Central) - Oct 15, 2022
Here in this contribution, we introduce a novel approach to enhance penetration and antifungal activity of the antifungal drug griseofulvin (GF)...The prepared nanosuspensions displayed enhanced solubility of the poorly soluble drug reaching approximately 1.2 mg/mL. The results showed that the dispersions that contained DTAB displayed maximum efficacy while the inclusion of colloidal silver did not seem to significantly improve the antifungal activity compared to other formulations.
- |||||||||| Clinical, Preclinical, Journal: In Vitro Activity of 23 Antifungal Drugs against 54 Clinical and Environmental Aspergillus oryzae isolates. (Pubmed Central) - Oct 12, 2022
In contrast, ketoconazole, terbinafine, econazole, tioconazole, ravuconazole, miconazole, nystatin, clotrimazole, griseofulvin, sertaconazole, natamycin, tolnaftate, and fluconazole had no or low activity. Further studies are required to determine how well this in vitro activity translates into in vivo efficacy.
- |||||||||| Jublia (efinaconazole) / Kaken, Bausch Health, Kerydin (tavaborole) / Pfizer
Review, Journal: Updated Perspectives on the Diagnosis and Management of Onychomycosis. (Pubmed Central) - Sep 23, 2022
Physicians should consider the disease severity, infecting pathogen, medication safety, efficacy and cost, and patient age, comorbidities, medication history, and likelihood of compliance when determining management plans. Onychomycosis is a chronic disease with high recurrence rates and patients should be counseled on an appropriate plan to minimize recurrence risk following effective antifungal therapy.
- |||||||||| griseofulvin / Generic mfg.
Journal: Antioxidant and cytotoxicity activities of δ-tocotrienol from the seeds of Allophylus africanus. (Pubmed Central) - Sep 14, 2022
Compound (1) and its semi-synthetic derivatives (1a-c) were tested for their antioxydant activity using DPPH radical scavenging assay and also for their cytotoxicity using human cervix carcinoma KB-3-1 cell lines. The results showed that compound (1) exhibited antioxidant activity with an IC value of 0.25 μM compared to the reference control trolox (26 µM); and good cytotoxic activity with IC values of 97 μM compared to the reference (+)-griseofulvin (IC between17-21 μM).
- |||||||||| griseofulvin / Generic mfg.
Journal: Unprecedented Combination of Polyketide Natural Product Fragments Identifies the New Hedgehog Signaling Pathway Inhibitor Grismonone. (Pubmed Central) - Sep 12, 2022
We describe the synthesis of the polyketide pseudo-NP grismonone and identify it as a structurally novel and potent inhibitor of Hedgehog signalling. The insight that the de novo combination of fragments derived from biosynthetically related NPs also may yield new biologically relevant compound classes with unexpected bioactivity may be considered a chemical extension or diversion of existing biosynthetic pathways and greatly expands the opportunities for exploration of biologically relevant chemical space by means of the pseudo-NP principle.
- |||||||||| thioguanine / Generic mfg.
Journal: Evaluation of Pharmaceuticals for DNA Damage in the Chicken Egg Genotoxicity Assay (CEGA). (Pubmed Central) - Jul 20, 2022
No DNA damage was detected for 7 compounds, including the purine antagonist 6-thioguanine, antipyretic analgesics acetaminophen and phenacetin, antibiotic ciprofloxacin, antilipidemic clofibrate, anti-inflammatory ibuprofen, and sedative phenobarbital...Overall, results in CEGA were largely in concordance with the outcomes in other systems in vitro and in vivo, indicating that CEGA provides reliable detection of DNA damaging activity of genotoxic compounds. Further evaluations with a broader set of compounds would support this conclusion.
- |||||||||| griseofulvin / Generic mfg.
Journal: A Prospective Clinical and Trichoscopic Study of Tinea Capitis in Children during Treatment. (Pubmed Central) - Jul 16, 2022
Despite the paucity of data evaluating trichoscopic features in patients with tinea capitis, this tool can serve as a rapid diagnostic and monitoring tool during antifungal treatment. Trichoscopic signs of tinea capitis resolution occur before clinical improvement and can guide for treatment adjustment during the course of therapy.
- |||||||||| griseofulvin / Generic mfg.
Preclinical, Journal: Malaria parasite heme biosynthesis promotes and griseofulvin protects against cerebral malaria in mice. (Pubmed Central) - Jul 15, 2022
Biosynthetic heme regulates food vacuole integrity and the food vacuoles from knockout parasites are compromised in pH, lipid unsaturation and proteins, essential for hemozoin formation. Targeting parasite heme synthesis by griseofulvin-a FDA-approved antifungal drug, prevents cerebral malaria in mice and provides an adjunct therapeutic option for cerebral and severe malaria.
- |||||||||| griseofulvin / Generic mfg.
Journal: The Shelf Life of ASDs: 1. Measuring the Crystallization Kinetics at Humid Conditions. (Pubmed Central) - Jul 9, 2022
Using the two independent methods, factors influencing the crystallization kinetics of ASDs containing the API griseofulvin were investigated quantitatively...Additionally, the influence of different polymers (poly(vinylpyrrolidone-co-vinyl acetate) and Soluplus) on crystallization kinetics were investigated. The experimentally obtained crystallization kinetics were described using the Johnson-Mehl-Avrami-Kolmogorov model and are the basis for future shelf life predictions at desired storage conditions.
- |||||||||| Noxafil (posaconazole) / Merck (MSD)
Journal: Structured solubility behaviour in bioequivalent fasted simulated intestinal fluids. (Pubmed Central) - Jun 22, 2022
These media have been applied in this study to examine the equilibrium solubility of twenty one exemplar drugs (naproxen, indomethacin, phenytoin, zafirlukast, piroxicam, ibuprofen, mefenamic acid, furosemide, aprepitant, carvedilol, tadalafil, dipyridamole, posaconazole, atazanavir, fenofibrate, felodipine, griseofulvin, probucol, paracetamol, acyclovir and carbamazepine) to determine if consistent solubility behaviour was present...The study indicates that the use of two appropriate bioequivalent fasted intestinal media from the nine will identify in vitro the maximum and minimum solubility boundaries for drugs and due to the media derivation this is probably applicable in vivo. These media could be applied during discovery and development activities to provide a solubility range, which would assist placement of the drug within the BCS/DCS and rationalise drug and formulation decisions.
- |||||||||| griseofulvin / Generic mfg.
Journal: CaCO-based carriers with prolonged release properties for antifungal drug delivery to hair follicles. (Pubmed Central) - Jun 19, 2022
We designed a novel particulate system for the encapsulation and intrafollicular delivery of griseofulvin (Gf) antifungal drug, which is water-insoluble and currently commercially available in oral dosage forms...These findings open new prospects for the efficiency enhancement of topical therapeutics. Importantly, the elaborated system could be adapted for the dermal delivery of various water-insoluble drugs beyond the scope of antifungal therapy.
- |||||||||| ketoconazole / Generic mfg., griseofulvin / Generic mfg., itraconazole / Generic mfg.
Journal: What can GP data tell us about the treatment of onychomycosis in the UK? (Pubmed Central) - Jun 8, 2022
A greater proportion of women, compared to men, were prescribed fluconazole. Onychomycosis treatment in primary care in the UK is broadly in concordance with national guidelines.
- |||||||||| Cytovene (ganciclovir) / Roche, Vistide (cidofovir) / Gilead
Review, Journal: Antimicrobials and Resistance Part II: Antifungals, Antivirals, and Antiparasitics. (Pubmed Central) - May 20, 2022
As evidenced by a dry pipeline, the gravity of antifungal, antiviral, and antiparasitic resistance has yet to draw the same attention as antibacterial resistance. Resistance disproportionately affects immunocompromised and vulnerable hosts, underscoring the urgent need for the development of novel therapeutics.
- |||||||||| griseofulvin / Generic mfg.
Preclinical, Journal: Prediction of In Vitro Drug Dissolution into Fed-state Biorelevant Media: Contributions of Solubility Enhancement and Relatively Low Colloid Diffusivity. (Pubmed Central) - Apr 28, 2022
Results showed drug-saturated FeSSGF globules and FeSSIF-V2 mixed micelles were large and slow diffusing (diffusivities of about 1×10 and 7×10 cm/s, respectively), compared to free drug (about 7×10 cm/s) and drug-bound micelles from pharmaceutical surfactants (about 0.5-1×10 cm/s). Of the three drugs, griseofulvin exhibited the greatest biorelevant media-enhanced solubility and dissolution (652-fold and 6.23-fold respectively in FeSSGF, and 190-fold and 12.7-fold respectively in FeSSIF-V2), but slow colloid diffusivity markedly attenuated large solubility benefits, particularly in FeSSGF.
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