The rabbit vagina as an in vivo model for vaginal fenticonazole permeability and toxicity

Campos, Rafael; Bittencourt, Samara Favi; Rojas-Moscoso, Julio Alejandro; Pissinatti, Lorenzo; Chen, Lu Shi; Porto, Mariana Alves; Moreno, Ronílson Agnaldo; Mendes, Gustavo Duarte; Nucci, Gilberto De

doi:10.1016/j.vascn.2018.04.001

Cited by 8 publications

(5 citation statements)

References 14 publications

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“…Fenticonazole nitrate (FTN) is an antifungal agent that belongs to imidazoles. It works by blocking ergosterol production and therefore damaging the cell membrane (Campos et al., 2018 ). FTN has both fungistatic and fungicidal properties against yeasts, fungi, and dermatophytes.…”

Section: Introductionmentioning

confidence: 99%

Fenticonazole nitrate loaded trans-novasomes for effective management of tinea corporis: design characterization, in silico study, and exploratory clinical appraisal

Albash

Ragaie

Hassab³

et al. 2022

Drug Delivery

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The current investigation aimed for loading fenticonazole nitrate (FTN), an antifungal agent with low aqueous solubility, into trans-novasomes (TNs) for management of tinea corporis topically. TNs contain Brij ® as an edge activator besides the components of novasomes (cholesterol, Span 60, and oleic acid) owing to augment the topical delivery of FTN. TNs were fabricated applying ethanol injection method based on D-optimal experiment. TNs were evaluated with regard to entrapment efficiency percent (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). Further explorations were conducted on the optimum formulation (F7). F7 showed spherical appearance with EE%, PS, PDI, and ZP of 100.00 ± 1.10%, 358.60 ± 10.76 nm, 0.51 ± 0.004, and −30.00 ± 0.80 mV, respectively. The in silico study revealed the ability of the FTN–cholesterol complex to maintain favorable interactions throughout the molecular dynamics simulation (MDS) study. Moreover, Trichophyton mentagrophytes growth was inhibited effectively by F7 than by FTN suspension applying 2,3-bis(2-methyloxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction assay. Furthermore, a clinical appraisal on patients with tinea corporis fungal lesions confirmed the superiority of F7 compared to Miconaz ® cream in the magnitude of clinical cure of tinea corporis. Thereby, TNs could be considered as promising vesicles for enhancing the antifungal potential of FTN for the topical management of tinea corporis.

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Section: Introductionmentioning

confidence: 99%

Fenticonazole nitrate loaded trans-novasomes for effective management of tinea corporis: design characterization, in silico study, and exploratory clinical appraisal

Albash

Ragaie

Hassab³

et al. 2022

Drug Delivery

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“…FTN is suggested for treatment of mycoses, and vaginal candidiasis (Campos et al. 2018 ). FTN has fungicidal, and fungistatic actions on fungi, yeasts and dermatophytes.…”

Section: Introductionmentioning

confidence: 99%

“…Fenticonazole nitrate (FTN) is an antifungal imidazole ring derivative that operates via hindering ergosterol integration, and sequentially destructing the cytoplasmatic outer membrane. FTN is suggested for treatment of mycoses, and vaginal candidiasis (Campos et al 2018). FTN has fungicidal, and fungistatic actions on fungi, yeasts and dermatophytes.…”

Section: Introductionmentioning

confidence: 99%

Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies

et al. 2020

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Fenticonazole nitrate (FTN) is a potent antifungal drug adopted in the treatment of vaginal candidiasis. It has inadequate aqueous solubility hence, novel ultra-deformable liposomes ‘Terpesomes’ (TPs) were developed that might prevail over FTN poor solubility besides TPs might abstain the obstacles of mucus invasion. TPs were assembled by thin-film hydration then optimized by Box Behnken design utilizing terpenes ratio (X 1 ), sodium deoxycholate amount (X 2 ), and ethanol concentration (X 3 ) as independent variable, whereas their impact was inspected for entrapment efficiency (Y 1 ), particle size (Y 2 ), and polydispersity index (Y 3 ). Design Expert ® was bestowed to select the optimal TP for more studies. The optimal TP had entrapment efficiency of 62.18 ± 1.39%, particle size of 310.00 ± 8.16 nm, polydispersity index of 0.20 ± 0.10, and zeta potential of −10.19 ± 0.2.00 mV. Elasticity results were greater in the optimal TP related to classical bilosomes. Further, ex vivo permeation illustrated tremendous permeability from the optimal TP correlated to classical bilosomes, and FTN suspension. Besides, in vivo assessment displayed significant inhibition effect in rats from FTN-TPs gel compared to FTN gel. The antifungal potency with undermost histopathological variation was detected in rats treated with FTN-TPs gel. Overall, the acquired findings verified the potency of utilizing FTN-TPs gel for treatment of vaginal candidiasis.

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“…Recently, anti-fungal drugs are consumed separately or in combination with antibiotics and corticosteroids (Veraldi & Milani, 2008 ). Fenticonazole nitrate (FTN) is an antifungal imidazole compound whose mechanism of action involves preventing ergosterol production, resulting in harming the cytoplasmic membrane of the fungi (Campos et al, 2018 ). FTN has both fungistatic and fungicidal actions on dermatophytes, yeasts and fungi, in addition to its activity against Gram positive bacteria.…”

Section: Introductionmentioning

confidence: 99%

Corneal targeted fenticonazole nitrate-loaded novasomes for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

et al. 2022

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The purpose of this manuscript was to develop and optimize Fenticonazole Nitrate (FTN)-loaded novasomes aiming to enhance drug corneal penetration and to improve its antifungal activity. Ethanol injection was used to formulate FTN-loaded novasomes adopting a central composite design. The researched factors were: stearic acid concentration (g%) (A), span 80: drug ratio (B) and cholesterol amount (mg) (C), and their effects on percent entrapment efficiency (EE%), particle size (PS), poly-dispersity index (PDI), zeta potential (ZP), and in vitro drug release after 8 hours (Q8h) were studied. Numerical optimization by Design-Expert® software was employed to select the optimum formula in respect to highest EE%, ZP (as absolute value), and Q8h >80% and lowest PS and PDI. Additional evaluation of the optimum formula was accomplished by short term stability study, effect of gamma sterilization, determination of Minimal Inhibitory Concentration and ex vivo corneal permeation study. The in vivo evaluation of the optimum formula was done to ensure its safety via in vivo ocular irritancy and in vivo corneal tolerance studies. Also, the efficacy was confirmed through in vivo corneal uptake study and susceptibility test. The optimum formula with the highest desirability value (0.738) showed EE% (94.31%), PS (197.05 nm), ZP (-66.95 mV) and Q8h (85.33%). It revealed to be safe, with augmented corneal permeation (527.98 µg/cm 2 ) that leads to higher antifungal activity. The above results confirmed the validity of novasomes to improve the corneal permeation and antifungal activity of Fenticonazole Nitrate.

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The rabbit vagina as an in vivo model for vaginal fenticonazole permeability and toxicity

Cited by 8 publications

References 14 publications

Fenticonazole nitrate loaded trans-novasomes for effective management of tinea corporis: design characterization, in silico study, and exploratory clinical appraisal

Fenticonazole nitrate loaded trans-novasomes for effective management of tinea corporis: design characterization, in silico study, and exploratory clinical appraisal

Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies

Corneal targeted fenticonazole nitrate-loaded novasomes for the management of ocular candidiasis: Preparation, in vitro characterization, ex vivo and in vivo assessments

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