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A new simple, precise, and sensitive charge transfer method for estimation of tioconazole drug in pure form and Gyno-Trosyd tablet was developed based on the reaction of the n-electron donor tioconazole drug with π-receptors, namely chloroanilic acid, 2,3-dichloro-5,6-dicyano-1,4-benzoquinon, and picric acid. The complexes were determined spectrophotometrically at 460, 402, and 520 nm for the tioconazole-2,3-dichloro-5,6-dicyano-1,4-benzoquinon, tioconazole-picric acid, and tioconazole-chloroanilic acid complexes, respectively. The conditions under which experiments should be conducted have been extensively studied. Beer's law was obeyed over the working concentration ranges of 10–100, 10–250, and 2–140 μg/mL for tioconazole-2,3-dichloro-5,6-dicyano-1,4-benzoquinon, tioconazole-chloroanilic acid, and tioconazole-picric acid complexes, respectively. [ABSTRACT FROM AUTHOR]

Introduction: Onychomycosis is a fungal infection of the nails that can be challenging to treat. Here, matrix-assisted laser desorption ionization–Fourier transform ion cyclotron resonance (MALDI-FTICR) imaging was applied to the quantitative analysis of the penetration profile of the antifungal compound, amorolfine, in human mycotic toenails. The amorolfine profile was compared with those of three other antifungals, ciclopirox, naftifine, and tioconazole. Methods: Antifungal compounds (amorolfine 5% lacquer, ciclopirox 8% lacquer, naftifine 1% solution, and tioconazole 28% solution) were applied to mycotic nails (n = 42). Nail sections were prepared, and MALDI-FTICR analysis was performed on the sections at a spatial resolution of 70 μm to compare the distribution profiles. Based on the minimum inhibitory concentrations of the four test compounds needed to kill 90% (MIC90) of the fungal organism, Trichophyton rubrum, the fold differences between the MIC90 and the antifungal concentrations in the nails (termed the multiplicity of the MIC90) were calculated for each. Results: The penetration profiles indicated higher concentrations of amorolfine and ciclopirox in the deeper layers of the nails 3 h after treatment, compared with naftifine and tioconazole. The mean concentrations across the entire nail sections at 3 h were significantly different among the four antifungals: amorolfine, 2.46 mM; ciclopirox, 0.95 mM; naftifine, 0.63 mM; and tioconazole, 1.36 mM (p = 0.016; n = 8 per compound). The median multiplicity of the MIC90 at 3 h was 191-fold for amorolfine, tenfold for ciclopirox, 52-fold for naftifine, and 208-fold for tioconazole. Conclusion: In this study, MALDI-FTICR was successfully applied to the quantitative analysis of antifungal distribution in human mycotic nails. The findings suggest that amorolfine penetrates deeper layers of the nail and accumulates at concentrations far exceeding the MIC needed to exert antimycotic activity. [ABSTRACT FROM AUTHOR]

Background: Onychomycosis affecting 5.5% of the population worldwide which may be treated by medical antifungal therapy or laser therapy which is attractive to avoid side effects, prevent developing of microbial resistance and safe with no mutagenic or cytotoxic effect. Aim of the Work: To evaluate the efficacy and safety of diode 577-nm laser in the treatment of onychomycosis.Patients and Methods: This study involved 30 onychomycosis patients with 87 affected nails, everyone had two affected sites [finger nails/toe nails] then randomly allocated into two groups: group [A] in which one site was treated by diode laser [577-nm] plus Tioconazole 28% [Fungibacid 28% nail solution] nail solution while in group [B] the other site in the same patient was treated by Tioconazole 28% nail solution only. We assessed the improvement by Onychomycosis Severity Index [OSI], culture and patient satisfaction. Results: The OSI severity in Diode 577-nm + Tioconazole group decreased from 36.7% before treatment to 20% after 3 months an continue to decrease after 6 months to 3.3%. However, in Tioconazole only group, the severity still the same as before treatment 36.7% after 3 months while after 6 months decreased to 20%. There was a significant difference between patients with severe OSI score while no significant difference between patients with mild and moderate OSI score among both groups at the end of follow up. There were 2 [6.7%] patients after 3 months and 18 [60%] patients after 6 months have complete resolution in Diode 577-nm + Tioconazole group while in Tioconazole only group, no one has complete resolution after 3 months but after 6 months there were 11 [36.7%] patients have complete resolution with significant difference between both groups at 3 and 6 months [p < 0.001 & 0.046].Conclusion: The 577-nm diode yellow laser is an effective and safe option for the treatment of onychomycosis.

Tioconazole (TCZ) is a broad-spectrum fungicidal BCS class II drug with reported activity against Candida albicans, dermatophytes, and certain Staphylococci bacteria. We report the use of TCZ-loaded transethosomes (TEs) to overcome the skin's barrier function. TCZ-loaded TEs were fabricated by using a cold method with slight modification. Box–Behnken composite design was utilized to investigate the effect of independent variables. The fabricated TEs were assessed with various physicochemical characterizations. The optimized formulation of TCZ-loaded TEs was incorporated into gel and evaluated for pH, conductivity, drug content, spreadability, rheology, in vitro permeation, ex vivo permeation, and in vitro and in vivo antifungal activity. The fabricated TCZ-loaded TEs had a % EE of 60.56 to 86.13, with particle sizes ranging from 219.1 to 757.1 nm. The SEM images showed spherically shaped vesicles. The % drug permeation was between 77.01 and 92.03. The kinetic analysis of all release profiles followed Higuchi's diffusion model. The FTIR, DSC, and XRD analysis showed no significant chemical interactions between the drug and excipients. A significantly higher antifungal activity was observed for TCZ-loaded transethosomal gel in comparison to the control. The in vivo antifungal study on albino rats indicated that TCZ-loaded transethosomal gel showed a comparable therapeutic effect in comparison to the market brand Canesten®. Molecular docking demonstrated that the TCZ in the TE composition was surrounded by hydrophobic excipients with increased overall hydrophobicity and better permeation. Therefore, TCZ in the form of transethosomal gel can serve as an effective drug delivery system, having the ability to penetrate the skin and overcome the stratum corneum barrier with improved efficacy. [ABSTRACT FROM AUTHOR]

Dermatophytosis is a fungal disease that affects the superficial skin layers and hair of farm animals all over the world including Egypt. Despite being a self-limiting disease, it has serious effects on public health and devastating economic losses due to its serious skin damage, a long course of treatment, and loss of weight. This study determines the most prevalent species of dermatophyte in sheep and identifies the incriminated species by both microscopic and culture methods with an assessment of animal and environmental risk factors. Moreover, it evaluates the effectiveness of three antifungal compounds (tioconazole cream and clotrimazole spray, and fluconazole capsule), on twenty-four naturally infected sheep. One hundred and three sheep from Sharkia and Dakahalia governorates were examined with clinically suggestive lesions from 2018 to 2019. 47.6% of the cases were positive for the dermatophyte infection either by clinical signs, microscopic or culture, or both. The highest registered infection rate is in males, at the age of ˂ 6 months, and in the winter season. Three antifungal medications are used for the first time in the treatment of ovine dermatophytosis. They are proved to have been effective in subsiding skin lesions with hair growth to return to its normal clinical state with a 100% curative rate. The treatment with preferable and easily applicable topical cures, especially tioconazole cream, is highly effective in the short run. This cream treatment is easily applicable and provides a good alternative to the traditional antifungal medication for sheep. Consequently, such treatment can reduce the possibility of spreading the infection by other animals, and may allow the adaption of efficient control measures.

Bacterial vaginosis is associated with severe infectious and inflammatory diseases and reduces the quality of life in women of reproductive age. Its worldwide prevalence is up to 80%. Thus, the development of new effective and safe methods of antimicrobial therapy becomes an urgent problem. This article provides a review of current antimicrobial therapies for bacterial vaginosis and evaluates the safety and efficacy of short courses of antimicrobial therapy using combined agents for intravaginal use.

The present study was performed to determine the therapeutic effects of tioconazole (Tz)-loaded novel transferosome carriers (TFs) for the treatment of atopic dermatitis (AD). Method: Tioconazole transferosomes suspension (TTFs) was formulated and optimized using a 32 factorial design. After that, the optimized batch of TTFs loaded into Carbopol 934 and sodium CMC was prepared with hydrogel and noted as TTFsH. Subsequently, it was evaluated for pH, spread ability, drug content, in vitro drug release, viscosity, in vivo scratching and erythema score, skin irritation, and histopathology study. Result: The optimized batch of TTFs (B4) showed the values of vesicle size, flux, and entrapment efficiency to be 171.40 ± 9.03 nm, 48.23 ± 0.42, and 93.89 ± 2.41, respectively. All batches of TTFsH showed sustained drug release for up to 24 h. The F2 optimized batch released Tz in an amount of 94.23 ± 0.98% with a flux of 47.23 ± 0.823 and followed the Higuchi kinetic model. The in vivo studies provided evidence that the F2 batch of TTFsH was able to treat atopic dermatitis (AD) by reducing the erythema and the scratching score compared to that of the marketed formulation (Candiderm cream, Glenmark). The histopathology study supported the result of the erythema and scratching score study with intact skin structure. It showed that a formulated low dose of TTFsH was safe and biocompatible to both the dermis and the epidermis layer of skin. Conclusion: Thus, a low dose of F2-TTFsH is a promising tool that effectively targeted the skin for the topical delivery of Tz to treat atopic dermatitis symptoms. [ABSTRACT FROM AUTHOR]

Tioconazole (TCZ) is a broad-spectrum fungicidal BCS class II drug with reported activity against Candida albicans, dermatophytes, and certain Staphylococci bacteria. We report the use of TCZ-loaded transethosomes (TEs) to overcome the skin’s barrier function. TCZ-loaded TEs were fabricated by using a cold method with slight modification. Box–Behnken composite design was utilized to investigate the effect of independent variables. The fabricated TEs were assessed with various physicochemical characterizations. The optimized formulation of TCZ-loaded TEs was incorporated into gel and evaluated for pH, conductivity, drug content, spreadability, rheology, in vitro permeation, ex vivo permeation, and in vitro and in vivo antifungal activity. The fabricated TCZ-loaded TEs had a % EE of 60.56 to 86.13, with particle sizes ranging from 219.1 to 757.1 nm. The SEM images showed spherically shaped vesicles. The % drug permeation was between 77.01 and 92.03. The kinetic analysis of all release profiles followed Higuchi’s diffusion model. The FTIR, DSC, and XRD analysis showed no significant chemical interactions between the drug and excipients. A significantly higher antifungal activity was observed for TCZ-loaded transethosomal gel in comparison to the control. The in vivo antifungal study on albino rats indicated that TCZ-loaded transethosomal gel showed a comparable therapeutic effect in comparison to the market brand Canesten®. Molecular docking demonstrated that the TCZ in the TE composition was surrounded by hydrophobic excipients with increased overall hydrophobicity and better permeation. Therefore, TCZ in the form of transethosomal gel can serve as an effective drug delivery system, having the ability to penetrate the skin and overcome the stratum corneum barrier with improved efficacy.

Aim: To find genes that provide resistance to antifungal drug tioconazole by a genomic DNA screening approach. Materials and Methods: Wild-type yeast (BY4741) cells were transformed with a high copy genomic DNA expression library and transformants that can grow on toxic levels of Tioconazole were determined. Library plasmids were isolated from the transformants and sequenced for the identification of potential tioconazole resistance gene(s). Results: Yeast YLR177w gene was isolated as a potential tioconazole resistance gene. Its overexpression led cells to tolerate normally toxic levels of tioconazole. Deletion of the YLR177w gene from the yeast genome made cells more vulnerable to the drug. Conclusion: Yeast YLR177w gene encodes a putative protein of unknown function. Our analyses suggest a potential function for the YLR177w gene for tioconazole resistance. [ABSTRACT FROM AUTHOR]

The present study was performed to determine the therapeutic effects of tioconazole (Tz)-loaded novel transferosome carriers (TFs) for the treatment of atopic dermatitis (AD). Method: Tioconazole transferosomes suspension (TTFs) was formulated and optimized using a 32 factorial design. After that, the optimized batch of TTFs loaded into Carbopol 934 and sodium CMC was prepared with hydrogel and noted as TTFsH. Subsequently, it was evaluated for pH, spread ability, drug content, in vitro drug release, viscosity, in vivo scratching and erythema score, skin irritation, and histopathology study. Result: The optimized batch of TTFs (B4) showed the values of vesicle size, flux, and entrapment efficiency to be 171.40 ± 9.03 nm, 48.23 ± 0.42, and 93.89 ± 2.41, respectively. All batches of TTFsH showed sustained drug release for up to 24 h. The F2 optimized batch released Tz in an amount of 94.23 ± 0.98% with a flux of 47.23 ± 0.823 and followed the Higuchi kinetic model. The in vivo studies provided evidence that the F2 batch of TTFsH was able to treat atopic dermatitis (AD) by reducing the erythema and the scratching score compared to that of the marketed formulation (Candiderm cream, Glenmark). The histopathology study supported the result of the erythema and scratching score study with intact skin structure. It showed that a formulated low dose of TTFsH was safe and biocompatible to both the dermis and the epidermis layer of skin. Conclusion: Thus, a low dose of F2-TTFsH is a promising tool that effectively targeted the skin for the topical delivery of Tz to treat atopic dermatitis symptoms.

Objective: The objective of this study was to evaluate the efficacy, safety, and tolerability of Gynomax® XL vaginal ovule in the treatment of bacterial vaginosis (BV), candidal vulvovaginitis (CVV), trichomonal vaginitis (TV), and mixed vaginal infections (MVI). Material and Methods: A total of 98 women diagnosed clinically with BV, CVV, TV, or MVI have completed this study. Patients were given Gynomax® XL for 3 consecutive days, and approximately 10 (+/-5) days after the treatment, a follow-up visit was conducted. In addition to the clinical examinations, vaginal swab samples were collected in both visits for microbiological tests. Results: Based on the clinical diagnosis of the investigators, most of the patients had MVIs (54.1%), followed by BV (24.5%) and CVV (20.4%) at the baseline visit. One (1.0%) patient was diagnosed as having TV. According to the microbiologic examination results, 44 (44.9%) patients had BV, 20 (20.4%) had CVV, and 13 (13.3%) had MVIs. According to the clinical findings, overall complete recovery (CR) was observed in 76.5% of the patients and according to the microbiologic findings, overall CR was observed in 85.7% of the patients. Microbiologic results evaluated by each diagnostic criterion showed that CR was detected in 93.2%, 85.0%, and 61.5% of the patients with BV, CVV, and MVIs, respectively. There were no serious or non-serious adverse events leading to patient withdrawal or treatment discontinuation during this study. Conclusion: Gynomax® XL vaginal ovules administered once daily for three consecutive days provide effective and safe treatment in patients with BV, CVV, and MVIs. [ABSTRACT FROM AUTHOR]

[Display omitted] Tioconazole is an effective antifungal agent with very low solubility in aqueous media, which limits its bioavailability and efficacy. Aiming to overcome the drug limitations by improving the solubility of this active pharmaceutical ingredient, solution precipitation techniques were employed to prepare four new crystalline salts, namely the mesylate, tosylate, maleate (1:1), and fumarate (1:1) hemihydrate. The thermal stabilities, dissolution properties, and structural characteristics of the solids were determined, and the study was extended to compare their properties with the already-known oxalate salt. The structural characterization of the new phases was carried out using a multi-method approach, which included thermal (differential scanning calorimetry and thermogravimetry), diffractometric (powder X-ray diffraction), and spectroscopic (near-infrared and mid-infrared) methodologies. The determination of the melting point of the salts confirmed the findings made by thermal methods. Functional characteristics of the salts, involving their intrinsic dissolution rates were also determined. It was found that the salts exhibited improved thermal stability and that the nature of the counterion modulated their dissolution characteristics. The salts displayed better intrinsic dissolution rates than the free base, to the point of being "highly soluble" according to the Biopharmaceutical Classification System. At pH 4.3, the sulfonic acid derivatives exhibited better dissolution rates than their carboxylic acid-derived counterparts, greatly improved regarding bare tioconazole. The results suggest that the salts have great potential to be used as replacements for the free base; in principle, careful salt selection may help to fulfill each solubility need for the different scenarios where the drug may be used. [ABSTRACT FROM AUTHOR]

Vaginal candidiasis is considered a frequent opportunistic mucosal infection and the second most common cause of vaginitis after bacterial vaginosis. In this work, different vaginal films based on different concentrations of polymer chitosan, hydroxyl propyl methyl cellulose containing tioconazole, were developed and thoroughly characterized to improve the conventional therapeutics of vaginal candidiasis. Mechanical properties, swelling, adhesiveness and antifungal activity were evaluated. The purity of drug was analyzed by Differential scanning calorimetry (DSC) a nd Fourier transform infrared spectroscopy (FT-IR). Films showed homogeneous surfaces and presented similar mechanical properties and adhesiveness. Time-kill studies displayed that films were active against Candida albicans and does not cause any harm to natural vaginal flora i.e. Lactobacilli Acidophilus. The system based on 2% chitosan and 1% hydroxyl propyl methyl cellulose with 20% PEG 400 as plasticizer presented fast antimicrobial activity as well as the lowest swelling these indicates that films based on chitosan and hydroxyl propyl methylcellulose could be a promising alternative dosage form for the treatment of vaginal candidiasis. [ABSTRACT FROM AUTHOR]

Background: Onychomycosis is a fungal infection of the nail units caused by dermatophytes, molds or yeasts. Onychomycosis accounts for 50% of all nail diseases, representing a significant cosmetic concern. Topical antifungals are of limited efficacy owing to their poor absorption. Tazarotene was occasionally used as an off-label treatment for onychomycosis. Aim: Based on the immune-modulating and antiinflammatory activity of tazarotene, we aimed to test the activity of tazarotene 0.1 % gel against fungi isolated from patients suffering from onychomycosis and comparing it to another antifungal drug of moderate efficacy, tioconazole 28%. Methods: Seventy patients with confirmed clinical and laboratory diagnosis of onychomycosis were enrolled in the study. Patients were treated with either tazarotene 0.1% gel or tioconazole 28% solution for 12 weeks. Follow-up of the patients was done after 3 months of the therapy stoppage. Determination of the onychomycosis severity based on the onychomycosis severity index and mycological studies was done at week 0 and 24. Antifungal susceptibility testing of tazarotene against the isolated fungi was done. Results: Tazarotene showed antifungal activity manifested by induction of a mycological cure in 25.7 % of cases; however, this effect was comparable to tioconazole 28%. Tazarotene showed a good efficacy against Aspergillus niger in vitro. Conclusions: Tazarotene 0.1 % gel has antifungal activity comparable to tioconazole 28% solution in treating onychomycosis. They both achieved mycological cure in about 25% of cases. Aspergillus niger was the most sensitive species to tazarotene. Tazarotene could be prescribed as an adjuvant to the standard antifungals for treatment of onychomycosis. [ABSTRACT FROM AUTHOR]

Onychomycosis (OM) is a chronic fungal infection of the nail caused by dermatophytes, yeasts, and nondermatophytes. Tioconazole is one of the topical antifungal belonging to imidazole derivatives. Tazarotene is a synthetic retinoid, with immunomodulating properties and anti‐inflammatory activity. To evaluate the efficacy of tazarotene 0.1% gel alone in comparison with its combination with tioconazole nail paint in the treatment of onychomycosis. Forty patients presented with onychomycosis, subjected to a full history taking, clinical examination, and nail examination, which includes a clinical, dermoscopic, assessment of severity by using Onychomycosis Severity Index (OSI), KOH examination, and fungal culture. There was a statistically significant increase in the response of treatment in patients treated by a combination of tazarotene and tioconazole compared to tazarotene alone through (decrease in OSI, dermoscopic features, and mycological clearance). Tazarotene had antifungal activity specially against Aspergillus niger while its combination with tioconazole gave better results and can be used as an adjuvant to the standard systemic or topical antifungal treatment for OM. [ABSTRACT FROM AUTHOR]

Onychomycosis is a common chronic-resistant nail disease. Traditional treatment has its limitations and side effects. This study aimed to evaluate the role of fractional CO2 laser and topical tioconazole 28% nail lacquer in the treatment of fingernail onychomycosis, as sole treatment modalities and in combination. Thirty patients with culture-proven onychomycosis were included and randomly divided into three equal groups. Laser group received six fractional carbon dioxide (CO2) laser sessions at monthly intervals; topical group received topical tioconazole 28% nail lacquer twice daily for 6 months, and combined group received six fractional CO2 laser sessions at monthly intervals with topical tioconazole twice daily for 6 months. Treatment outcome was evaluated through physician's evaluation of improvement using onychomycosis severity index score (OSI), patients' satisfaction, side effect evaluation, and mycological culture (assessed after the end of treatment). At the end of treatment, both laser and combined groups showed significantly better degrees of improvement (P = 0.036, 0.024, respectively) and patient's satisfaction (P = 0.046, 0.003, respectively) in comparison with topical group. Mycological clearance in fungal cultures was significantly higher in combined group than topical group after the end of treatment (P = 0.007). Fractional CO2 laser is a safe and effective treatment modality for onychomycosis. Its efficacy approximates that of fractional CO2 laser combined with topical tioconazole 28% nail lacquer and surpasses that of topical tioconazole 28% monotherapy. It is expected to be an excellent choice for patients in whom systemic antifungals are contraindicated or who are unresponsive or intolerant to topical antifungals. [ABSTRACT FROM AUTHOR]

Cancer is a complex devastating disease with enormous treatment challenges, including chemo- and radiotherapeutic resistance. Combination therapy demonstrated a promising strategy to target hard-to-treat cancers and sensitize cancer cells to conventional anti-cancer drugs such as doxorubicin. This study aimed to establish molecular profiling and therapeutic efficacy assessment of chloroquine and/or tioconazole (TIC) combination with doxorubicin (DOX) as anew combination model in MCF-7 breast cancer. The drugs are tested against apoptotic/autophagic pathways and related redox status. Molecular docking revealed that chloroquine (CQ) and TIC could be potential PI3K and ATG4B pathway inhibitors. Combination therapy significantly inhibited cancer cell viability, PI3K/AkT/mTOR pathway, and tumor-supporting autophagic flux, however, induced apoptotic pathways and altered nuclear genotoxic feature. Our data revealed that the combination cocktail therapy markedly inhibited tumor proliferation marker (KI-67) and cell growth, along with the accumulation of autophagosomes and elevation of LC3-II and p62 levels indicated autophagic flux blockage and increased apoptosis. Additionally, CQ and/or TIC combination therapy with DOX exerts its activity on the redox balance of cancer cells mediated ROS-dependent apoptosis induction achieved by GPX3 suppression. Besides, Autophagy inhibition causes moderately upregulation in ATGs 5,7 redundant proteins strengthened combinations induced apoptosis, whereas inhibition of PI3K/AKT/mTOR pathway with Beclin-1 upregulation leading to cytodestructive autophagy with overcome drug resistance effectively in curing cancer. Notably, the tumor growth inhibition and various antioxidant effects were observed in vivo. These results suggest CQ and/or TIC combination with DOX could act as effective cocktail therapy targeting autophagy and PI3K/AKT/mTOR pathways in MCF-7 breast cancer cells and hence, sensitizes cancer cells to doxorubicin treatment and combat its toxicity.

Background: Onychomycosis is a chronic fungal infection of the nails, and the treatment has been proven to be a challenge to healthcare professionals. Objective: To evaluate the efficacy of fractional carbon dioxide laser-assisted delivery of topical tazarotene versus topical tioconazole in the treatment of onychomycosis. Materials and Methods: A total of 102 patients with onychomycosis were randomly assigned to groups A and B, and both groups were treated with four sessions of fractional CO2 laser and followed by topical tazarotene 0.1% in Group A and topical tioconazole 28% in Group B. The clinical effect, KOH examination, and culture for the affected nails in the two groups were analyzed. Results: One month after the last session, regarding clinical response, 35.3% showed complete improvement in Group A versus 33.3% in Group B without significant difference. There was a significant difference between the two studied groups as regards KOH test and culture result before and after treatment (p value<.001), they were turned negative in 91.7% and 100% of patients in Group A and 78.3% and 95.5% of patients in Group B, respectively. Conclusion: Fractional CO2 laser-assisted drug delivery is an effective and safe treatment option for onychomycosis. [ABSTRACT FROM AUTHOR]

Graphical abstract Abstract Vaginal candidiasis is considered a frequent opportunistic mucosal infection and the second most common cause of vaginitis after bacterial vaginosis. In this work, different vaginal films based on chitosan, hydroxypropyl methylcellulose and blends of these polymers containing tioconazole, were developed and thoroughly characterized to improve the conventional therapeutics of vaginal candidiasis. Mechanical properties, swelling, adhesiveness, morphology, antifungal activity, hemocompatibility and cytotoxicity were evaluated. The drug solid state in the films was analyzed by thermal and X-ray diffraction analysis. Films showed homogeneous surfaces and presented similar mechanical properties and adhesiveness. Time-kill studies displayed that films were more active than both tioconazole pure drug and traditional tioconazole ovule against Candida albicans , which is probably related to the fact that tioconazole is in amorphous state inside the films. Although all formulations proved to be hemocompatible, films based only on chitosan exhibited a certain degree of cytotoxicity and therefore they should be avoided. The system based on chitosan-hydroxypropyl methylcellulose with 40% PEG 400 as plasticizer presented fast antimicrobial activity as well as the lowest swelling. Additionally, this formulation did not produce substantial hemolytic and cytotoxic effects, indicating that films based on chitosan-hydroxypropyl methylcellulose could be a promising alternative dosage form for the treatment of vaginal candidiasis. [ABSTRACT FROM AUTHOR]

Abstract Tioconazole (TCZ), a broad-spectrum antifungal agent, has significant activity against Candida albicans and other Candida species, and therefore, it is indicated for the topical treatment of superficial mycoses. The main goal of this work is to report an exhaustive identification and characterization procedure to improve and facilitate the online quality control and continuous process monitoring of TCZ in bulk material and loaded in two different dosage forms: ovules and nail lacquer. The methodologies were based on thermal (differential scanning calorimetry (DSC), melting point, and thermogravimetry (TG)), spectroscopic (ultraviolet (UV), Raman, near infrared (NIR), infrared spectroscopy coupled to attenuated total reflectance (FTIR-ATR), and nuclear magnetic resonance (NMR)), microscopic and X-ray diffraction (XRD). The TCZ bulk powder showed a high crystallinity, as observed by XRD, with a particles size distribution (3–95 µm) resolved by microscopic measurements. TCZ melting point (82.8 °C) and a degradation peak centered at 297.8 °C were obtained by DSC and DTG, respectively. An unambiguous structure elucidation of TCZ was obtained by mono- and two- dimensional 1H and 13C NMR spectral data analysis. The FTIR-ATR, Raman and NIR spectra of both the raw material and the commercial products were analyzed and their characteristic bands were tabulated. The best methods for TCZ identification in ovules were DSC, TG, XRD, NIR and Raman, while NIR and FTIR-ATR were the most appropriate techniques to analyze it in the nail lacquer. DSC, TG, DRX, Raman, FTIR-ATR and NIR spectroscopy are effective techniques to be used in online process analysis, because they do not require sample preparation, and they are considerably sensitive to analyze complex samples. [ABSTRACT FROM AUTHOR]

Readings on day (D)2 and D4 showed positive reactions to nickel sulfate 5%, tioconazole 1%, and tioconazole 28% nail lacquer "as is" (Figure 2). Keywords: allergic contact dermatitis; case report | fluconazole; tioconazole EN allergic contact dermatitis case report | fluconazole tioconazole 354 356 3 04/07/21 20210501 NES 210501 First-line therapy for both topical and systemic mycosis includes azoles. GLO:FQV/01may21:cod13748-fig-0001.jpg PHOTO (COLOR): 1 Pruriginous cutaneous rash extended to the lower limbs after tioconazole-medicated nail solution and tioconazole cream application and fluconazole systemic assumption gl The patient had no previous history of allergy. [Extracted from the article]

[Display omitted] • Two microbiological and charge transfer complex formation spectrophotometric methods were successfully applied for determination of tioconazole in pure and different pharmaceutical dosage forms. • Different thermodynamic variables associated with the charge transfer complex were investigated and revealed the spontaneity and the exothermic nature of the complex formation. • The two methods were validated in accordance to ICH methodology. Two sensitive microbiological and charge transfer spectrophotometric methods have been developed for the quantitative determination of the antifungal drug, tioconazole, in its pure form and pharmaceutical preparations. The microbiological assay was based on the agar disk diffusion method by measuring the diameter of the inhibition zones related to different concentrations of tioconazole. The spectrophotometric method relied on charge transfer complex formation between tioconazole as an n-donor and chloranilic acid as a π-acceptor at room temperature. The formed complex was measured at λ max = 530 nm. The molar absorptivity and the formation constant of the formed complex were determined using different models, including the Benesi-Hildebrand, Foster-Hammick-Wardley, Scott, Pushkin-Varshney-Kamoonpuri, and Scatchard equations. Different thermodynamic parameters associated with the complex formation, including the free energy change (Δ G °), the standard enthalpy (Δ H °), and the standard entropy change (Δ S °), were evaluated. The two methods were validated in conformity with ICH-recommended guidelines and employed successfully for the quantification of tioconazole in both pure form and pharmaceutical formulations. [ABSTRACT FROM AUTHOR]

Onychomycosis is a disease that affects many adults, whose treatment includes both oral and topical therapies with low cure rates. The topical therapy is less effective but causes fewer side effects. This is why the development of an effective, easy to apply formulation for topical treatment is of high importance. We have used a nanotechnological approach to formulate Pickering emulsions (PEs) with well-defined properties to achieve site-specific delivery for antifungal drug combination of tioconazole and Melaleuca alternifolia essential oil. Silica nanoparticles with tailored size and partially hydrophobic surface have been synthesized and used for the stabilization of PEs. In vitro diffusion studies have been performed to evaluate the drug delivery properties of PEs. Ethanolic solution (ES) and conventional emulsions (CE) have been used as reference drug formulations. The examination of the antifungal effect of PEs has been performed on Candida albicans and Trichophyton rubrum as main pathogens. In vitro microbiological experimental results suggest that PEs are better candidates for onychomycosis topical treatment than CE or ES of the examined drugs. The used drugs have shown a significant synergistic effect, and the combination with an effective drug delivery system can result in a promising drug form for the topical treatment of onychomycosis.

Charge-transfer complex (CTC) formation between tioconazole (TCZ) as an n -electron donor and 7, 7, 8, 8-tetracyanoquinodimethane (TCNQ) as a π-acceptor was studied spectrophotometrically with an accompanying kinetic and thermodynamic investigation. Multivariate data analysis via a set of experimental designs was executed for this purpose. A 2 3 - two-level full factorial design (FFD) was used for inspecting the proposed variables while a face-centered central composite design (FCCCD) was used to adjust the levels of variables proved to be significant. Two responses were quantified as a result of this interaction; complex I (Y1, measured at 743 nm) and complex II (Y2, measured at 842 nm). Derringer's function and overlaid contour plots were used to concurrently optimize both responses. Benesi–Hildebrand equation was applied to determine of formation constant (K), and the molar absorptivity (Ɛ) of the formed complex. Different thermodynamic parameters; the standard Gibbs free energy change (∆ G °), the standard enthalpy of formation (∆ H °) and the standard entropy change (∆ S °) were determined for the reaction product. The proposed method was validated regarding the linearity, intra-, and inter-day precision and accuracy, limit of detection, limit of quantification and following the ICH standards. The proposed method was also applied for the determination of TCZ in its pharmaceutical preparations. Having a higher molar absorptivity and higher formation constant, complex II was of choice for all subsequent measurements. Application of Benesi–Hildebrand equation supported the formation of 1: 1 CTC. Thermodynamic study revealed the endothermic characters and the spontaneity of formation of the CTC at high temperature. [ABSTRACT FROM AUTHOR]