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Alhakamy, Nabil Abdulhafiz, and Khaled Mohamed Hosny. Journal of drug delivery science and technology 49 (2019): 316-322.
Bifonazole (BF) is a broad-spectrum, highly lipophilic antifungal agent with inherently low aqueous solubility and limited absorption, restricting its therapeutic potential in topical applications. To address these challenges, a self-nano-emulsifying drug delivery system (SNEDDS) was developed using a mixture design optimization strategy. Component selection was based on solubility screening across various oils, surfactants, and cosurfactants, with Peceol, Kolliphore, and Plurol Oleique identified as optimal excipients.
The experimental design varied the proportions of oil (X1), surfactant (X2), and cosurfactant (X3) to minimize globule size while maximizing delivery performance. The optimized formulation-Peceol 15%, Kolliphore 65%, and Plurol Oleique 20%-produced nano-globules with an average diameter of 36 ± 3 nm. This system demonstrated a marked increase in antifungal activity against Candida albicans (26 ± 3 mm inhibition zone) and enhanced ex vivo permeability across rat abdominal membrane (permeability coefficient: 7.3 × 10⁻⁴ cm/min).
Pharmacokinetic evaluation revealed significant improvements over an aqueous BF suspension, with bioavailability, permeability, and antifungal efficacy enhanced by factors of 6.0, 2.179, and 1.85, respectively. The nano-emulsion's ultra-small droplet size and surfactant-mediated membrane interaction likely contributed to superior skin penetration and drug absorption.
This study highlights BF-SNEDDS as a promising transdermal delivery platform for improving the therapeutic profile of bifonazole, offering enhanced bioavailability and antifungal potency for clinical applications in dermal mycoses management.
Hiranphinyophat, Suphatra, et al. Colloids and Surfaces B: Biointerfaces 197 (2021): 111423.
Bifonazole (BFZ), a potent lipophilic antifungal drug, faces challenges in topical therapy due to limited skin penetration and formulation instability. To address these limitations, a stable oil-in-water (O/W) emulsion system was developed, employing poly(2-isopropoxy-2-oxo-1,3,2-dioxaphospholane)-modified cellulose nanocrystals (CNC-g-PIPP) as particle stabilizers. This particle-stabilized emulsion (BFZ-loaded CP-PE) was designed to improve BFZ permeation while maintaining biocompatibility.
The optimized formulation incorporated isopropyl myristate (IPM) as the oil phase (oil-to-water ratio 1:1) and CNC-g-PIPP at 0.4 wt% as the stabilizing agent, producing emulsions with a mean droplet size of 2.54 ± 1.39 μm. The BFZ loading efficiency reached 83.1%, and the system demonstrated stability for over 15 days without significant droplet size change. in vitro release studies revealed a sustained drug release profile, with only 17% BFZ released after 48 h, indicating prolonged drug availability at the application site.
Skin permeation studies using a porcine model showed that BFZ-loaded CP-PE achieved a ~4.4-fold increase in permeation and penetration compared to both a conventional surfactant-stabilized emulsion and a BFZ control solution. Fluorescence imaging confirmed deep penetration from the stratum corneum to the dermis, while histopathology confirmed skin integrity without inflammation.
These findings establish BFZ-loaded CP-PE as a promising, low-environmental-impact transdermal delivery platform, offering enhanced penetration and sustained release for improved management of dermal fungal infections.
Ahmed, Imteaz, et al. Fuel Processing Technology 215 (2021): 106741.
Bifonazole (BFZ), beyond its conventional role as an antifungal agent, has been utilized as a structural building block in the synthesis of cross-linked aromatic porous polymers (CAPP) for catalytic applications. In this study, BFZ was reacted with 4,4'-bis(bromomethyl)biphenyl via a Friedel-Crafts benzoylation, catalyzed by anhydrous AlCl₃ in dichloromethane, to form a highly cross-linked polymeric network. Post-synthetic functionalization with diethyltriamine (DETA) produced CAPP-DETA, a nitrogen-rich porous catalyst.
CAPP-DETA exhibited outstanding catalytic performance in the oxidative desulfurization (ODS) of thiophenic sulfur compounds, using molecular oxygen as a green oxidant. Under optimized conditions (50 mg catalyst, 400 ppm dibenzothiophene (DBT) in decane, 120 °C, 4 h), 100% DBT conversion was achieved. The catalytic activity was attributed to the triamine groups generating superoxide radicals (O₂·⁻), enabling efficient sulfur oxidation. The reactivity order for thiophenic compounds followed DBT > benzothiophene > thiophene, reflecting differences in electron density and steric hindrance.
The catalyst maintained full activity over four consecutive cycles, underscoring its stability and reusability. Reaction parameter studies revealed that increasing temperature, catalyst loading, and substrate concentration directly influenced the ODS rate.
This work demonstrates that BFZ can serve as a versatile aromatic precursor for the preparation of functional porous polymeric catalysts, expanding its application from pharmaceuticals to environmental catalysis. The resulting CAPP-DETA offers a sustainable and efficient platform for deep desulfurization of fuels, contributing to cleaner energy production.
What is the CAS number of Bifonazole?
The CAS number of Bifonazole is 60628-96-8.
What is the molecular weight of Bifonazole?
The molecular weight of Bifonazole is 310.39.
What is the molecular formula of Bifonazole?
The molecular formula of Bifonazole is C22H18N2.
What percentage of actives does Bifonazole contain?
Bifonazole contains 95% actives.
What is the physical state of Bifonazole?
Bifonazole is in solid form.
What are the typical applications of Bifonazole?
Bifonazole is used as an antimicrobial agent.
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