Sertaconazole Research Articles

A chiral enantioseparation generic strategy for anti-Alzheimer and antifungal drugs by short end injection capillary electrophoresis using an experimental design approach.

The present study describes a generic strategy using capillary electrophoretic (CE) method for chiral enantioseparation of anti-Alzheimer drugs, namely, donepezil (DON), rivastigmine (RIV), and antifungal drugs, namely, ketoconazole (KET), Itraconazole (ITR), fluconazole (FLU), and sertaconazole (SRT) in which these drugs have different basic and acidic properties. Several modified cyclodextrins (CDs) were applied for enantioseparation of racemates such as highly sulfated α, γ CDs, hydroxyl propyl-β-CD, and Sulfobutyl ether-β-CD. The starting screening conditions consist of 50-mM phosphate-triethanolamine buffer at pH2.5, an applied voltage of 15kV, and a temperature of 25°C. The CE strategy implemented in the separation starts by screening prior to the optimization stage in which an experimental design is applied. The design of experiment (DOE) was based on a full factorial design of the crucial two factors (pH and %CD) at three levels, to make a total of nine (32 ) experiments with high, intermediate, and low values for both factors. Evaluation of the proposed strategy pointed out that best resolution was obtained at pH2.5 for five racemates using low percentages of HS-γ-CD, while SBE-β-CD was the most successful chiral selector offering acceptable resolution for all the six racemates, with the best separation at low pH values and at higher %CD within 10-min runtime. Regression study showed that the linear model shows a significant lack of fit for all chiral selectors, anticipating that higher orders of the factors are most likely to be present in the equation with possible interactions.

P.1.l.026 - Chronic magnesium supplementation increases hippocampal neurogenesis and decreases proliferation in myocardium in ACTH-treated rats

The aim of this study was to compare the efficacy of different approaches for enhancement of dermal availability of the highly lipophilic antifungal model drug – sertaconazole nitrate (SN). For this purpose, a physical penetration enhancer – dissolving microneedles (MNs) was fabricated by filling moulds with liquid formulation based on polyvinylpyrrolidone and loaded with SN. Dissolving MNs were characterised regarding their morphological and mechanical characteristics. A penetration enhancement efficacy of MNs was evaluated in vitro using porcine ear skin in parallel with the efficacy of formerly developed chemical penetration enhancer – biocompatible microemulsion (ME) formulation. Moreover, an ability of solid silicon MNs to significantly improve delivery of SN from ME into the skin has also been investigated. The obtained results showed that dissolving MNs had satisfying morphological properties and mechanical strength. This type of MNs provided comparable drug deposition in the skin as ME formulation, but also revealed an indication of percutaneous absorption of a portion of the administered drug dose. However, the penetration/permeation study results were largely influenced by experimental setup and dosing regimen. Although solid silicon MNs assisted SN dermal delivery led to increase of drug cutaneous retention (1.9-fold) under infinite dosing regimen, the synergistic action of solid MNs and ME applied under finite dosing was more pronounced in comparison with the application either of physical (dissolving MNs) or chemical enhancer (ME) alone. Namely, SN amount accumulated into the skin increased up to 4.67 and 4.37 folds in comparison with ME and dissolving MNs alone, respectively, while reaching a significant decrease in drug permeation through the skin compared to the use of dissolving MNs. Application of ME per se was the only approach that provided selective in vitro dermal drug delivery without SN permeation across the skin. However, despite both types of the used MNs lead to SN permeation in vitro, the ratio between the drug amount deposited in the skin and SN content permeated was significantly higher for the combined approach (12.05) than for dissolving MNs (2.10). Therefore, a combination of solid silicon MNs and biocompatible ME favoured more pronouncedly SN skin accumulation, which is preferable in the treatment of skin fungal infections.

Sertaconazole nitrate loaded nanovesicular systems for targeting skin fungal infection: In-vitro, ex-vivo and in-vivo evaluation

The aim of this study was to develop different vesicular systems for sertaconazole nitrate and evaluate the ability of targeting deep skin layers to treat dermal fungal infection. Therefore, different phospholipid based nanovesicles, namely liposomes, glycerosomes, transferosmes and ethosomes were prepared and in-vitro evaluated for morphology, entrapment efficiency, vesicle size and zeta potential value, followed by ex-vivo evaluation through skin penetration and permeation. The selected vesicular formula was incorporated into gel base system and assessed by ex-vivo permeation visualization study using confocal laser scanning microscopy (CLSM). In-vivo study was performed to compare antifungal efficacy of STZL loaded vesicular gel with commercial cream (Dermofix®). All nanovesicles were unilamller and almost spherical in shape. Entrapment efficiency, vesicle size and zeta potential were dependent upon vesicle composition. Vesicular formulae promoted drug permeation compared to commercial cream where transferosomal system containing 3% soyphospholipid (SPC) and 0.15% sodium deoxychloate (SDC) exhibited highest flux (645μg/cm2/h). The CLSM images confirmed the penetration of the developed probe-loaded tansferosomal system to viable epidermis layers with fluorescence intensity greater than unencapsulated probe. The in-vivo study revealed significant prevention effect in immunecompromised rat model. Furthermore, the antifungal activity with lowest histopathological changes was significantly observed in the developed STZL-loaded transferosomal gel compared to commercial cream using immunecompromised rat model with fungal skin infection.

Spectrophotometric methods based on charge transfer complexation reaction for the determination of some antifungal drugs in pure and dosage forms

Charge transfer complexes of some antifungal drugs fluconazole (FLU), sertaconazole nitrate (SER) and miconazole nitrate (MCO) as electron donor with the σ-acceptor iodine (I2) and 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ), p-chloranilic acid (p-CLA) and 7,7,8,8-tetracyanoquinodimethane (TCNQ) as π-acceptors in acetonitrile were investigated. The formation of the colored charge-transfer complexes were utilized in the development of simple, rapid and accurate spectrophotometric methods for the analysis of the cited drugs in pure forms and pharmaceutical formulations at 365 nm for MCO and SER using I2 method, at 460 nm for FLU and SER using DDQ method, at 535 and 530 nm for FLU and SER, respectively, using p-CLA method and at 842 nm for MCO and SER using TCNQ method. The optimum experimental conditions have been studied carefully and optimized. Beer’s law was obeyed over the concentration ranges of 2.0–28, 10–240 and 2.0–160 µg mL−1 for MCO, FLU and SER, respectively, with good correlation coefficients (0.9996–0.9999). Molar absorpitivity, Sandell sensitivity, relative standard deviation, limit of detection and quantification were calculated. The obtained data refer to high accuracy and precision of the proposed method. The obtained results were confirmed by inter and intra-day accuracy and precision with percent recovery of 99.1–100%, 99.3–101% and 99.1–101% for MCO, FLU and SER, respectively. These data were compared with those obtained using official methods for the determination of the cited drugs. The proposed methods were applied successfully for simultaneous determination of the cited drugs in their pharmaceutical formulations with good accuracy and precision and without interferences from common additives. KEY WORDS: Fluconazole, Sertaconazole nitrate, Miconazole nitrate, Charge transfer complexes, Spectrophotometry, Pharmaceutical formulations Bull. Chem. Soc. Ethiop. 2016, 30(3), 333-346.DOI: http://dx.doi.org/10.4314/bcse.v30i3.2

Investigation of the Dermal Absorption and Irritation Potential of Sertaconazole Nitrate Anhydrous Gel.

Effective topical therapy of cutaneous fungal diseases requires the delivery of the active agent to the target site in adequate concentrations to produce a pharmacological effect and inhibit the growth of the pathogen. In addition, it is important to determine the concentration of the drug in the skin in order to evaluate the subsequent efficacy and potential toxicity for topical formulations. For this purpose, an anhydrous gel containing sertaconazole nitrate as a model drug was formulated and the amount of the drug in the skin was determined by in vitro tape stripping. The apparent diffusivity and partition coefficients were then calculated by a mathematical model describing the dermal absorption as passive diffusion through a pseudo-homogenous membrane. The skin irritation potential of the formulation was also assessed by using the in vitro Epiderm™ model. An estimation of the dermal absorption parameters allowed us to evaluate drug transport across the stratum corneum following topical application. The estimated concentration for the formulation was found to be higher than the MIC100 at the target site which suggested its potential efficacy for treating fungal infections. The skin irritation test showed the formulation to be non-irritating in nature. Thus, in vitro techniques can be used for laying the groundwork in developing efficient and non-toxic topical products.

Comparative study of the efficacy and safety of topical sertaconazole versus topical terbinafine in the treatment of dermatophytoses in a tertiary care centre

Background: Dermatophytes are superficial fungal infection termed dermatophytosis, diagnosed by direct microscopy and confirmed with culture and treated with antifungal agents by both topical and systemic therapy. The objective of this study was to compare the efficacy of topical sertaconazole with topical terbinafine applied twice daily in reducing the size and severity of the lesions. Methods: Two groups of patients, the topical sertaconazole nitrate 2% cream (group 1) and the topical terbinafine hydrochloride 1% cream (group 2) were treated twice daily for 2 weeks and followed after 4 weeks. Skin scrapings were taken to confirm the diagnosis, to assess the efficacy and potency of the study drugs. The statistical analysis was performed using statistical package for Social Sciences. Assessment of the groups was analysed using Chi-square test. Baseline demographic data was analysed using ANOVA. Results: At the end of first week, sertaconazole group showed significant changes in pruritis (p value 0.045) as compared to terbinafine group (p value <0.05) and no severe symptoms of erythema in both grups. After 2 weeks, resolution of vesicle was seen higher in terbinafine group. But after ‘follow-up phase’, all patients showed absence of vesicles and negative mycological assessment. Conclusions: Topical sertaconazole nitrate was better in reducing the severity of pruritis and achieving faster mycological cure compared to terbinafine and found to possess additional anti-pruritic and anti-inflammatory action.

Purity assessment and determination of sertaconazole in bulk and pharmaceutical formulations based on spectrophotometric and chromatographic approaches

Stability evaluation of the drug substance is an integral part of the systematic approach to stability studies. Hence, three simple, sensitive and precise methods depending on two different techniques as UV spectrophotometry and chromatography were adopted for the task of stability indicating determination of sertaconazole (SER) in presence of its acidic degradation products. The first method is Zero-crossing first derivative ( 1 D) spectrophotometric one, which allows the determination of SER over a concentration range of 4-64 µg/mL at 290 nm with mean percentage recoveries 99.77±0.781. While first-derivative of the ratio spectra ( 1 DR) is the method of choice for determination of pure SER at a maximum 300 nm and at a trough 304 nm, with mean percentage recoveries 99.98±0.720 and 100.46±0.640, respectively. The third developed HPLC method used a RP-ZORBAX C18 column (5 μm particle size, 250×4.6 mm; id) with isocratic elution. The mobile phase was methanol: 0.2% formic acid aqueous solution (75:25, v : v ); pH = 3.5 at the flow rate of 1.0 mL/min, with UV detection at 260 nm. The method could determine SER in the range of 0.8-40 µg/mL with a mean percentage recovery of 99.65±0.630. The developed methods were succeeded in the determination of SER in bulk powder, pharmaceutical dosage forms and in presence of its acidic degradation products. The results obtained were validated in compliance with ICH guidelines and compared statistically with each other and to those of the official method in the British Pharmacopoeia regarding both accuracy and precision.

Optimized and validated spectrophotometric determination of two antifungal drugs in pharmaceutical formulations using an ion-pair complexation reaction

Simple, rapid, cost-effective, sensitive and extractive spectrophotometric methods were developed for the determination of two antifungal drugs (i.e., sertaconazole nitrate (SER) and miconazole nitrate (MCO)) in pure and dosage forms. The methods are based on the formation of ion-pair complexes between the drugs and acid dyes (i.e., bromocresol purple (BCP), bromophenol blue (BPB) and methyl orange (MO)) in acidic buffer solutions. The formed complexes were extracted with chloroform and measured at 410, 416 and 427nm for SER and at 408, 415 and 426nm for MCO using BCP, BPB and MO, respectively. The analytical parameters and their effects on the reported systems were investigated. Beer's law was obeyed in the 1.0–20 and 1.0–24μgmL−1 ranges for SER and MCO, respectively. The composition of the ion pairs was determined to be 1:1. The molar absorptivity, Sandell sensitivity, limits of detection and limits of quantification were calculated. Other method validation parameters, such as precision, accuracy, robustness, ruggedness and selectivity, were satisfactory. The proposed methods have been successfully applied for the analysis of the studied drugs in their pure and dosage forms. Statistical comparison of the results with the reference methods indicated excellent agreement and no significant difference in accuracy and precision.

Fabrication and Characterization of Sertaconazole Nitrate Microsponge as a Topical Drug Delivery System.

Present study was taken up to develop a topical formulation that releases the drug in controlled manner, reduce the side effects associated with topical drug delivery and improve product efficacy with aid of microsponges. Microsponges loaded with sertaconazole nitrate were prepared by using quasi emulsion solvent diffusion with five different proportions of the polymer (Eudragit RS 100). The developed microsponges were analyzed for particle size, production yield, entrapment efficiency and drug content. Scanning electron microscopic images of microsponges revealed that they are spherical in shape and contain pores. Pore structure analysis was done by using mercury intrusion porosimetry technique, which confirmed the porous nature of microsponges. Microsponges were then incorporated in to a 1% corbopol gel and evaluated for pH, drug content, texture profile analysis and in vitro drug release. The batch F IV was found to be optimal as it shown 69.38% controlled drug release in 8 h that followed Higuchi model.

Spectrophotometric Determination of Sertaconazole Nitrate in Pharmaceutical Dosage Form using Quality by Design (QbD) Framework

An accurate and reliable ultra-violet spectrophotometric method was developed based on the Quality by Design framework, for the determination of sertaconazole nitrate in solid oral dosage form. Sampling interval and scanning speed were the two critical method variables, which were also evaluated by design of experiment approach, for establishing method robustness using optimization technique. Sertaconazole shows absorption maximums at 260 nm, 293 nm and 302 nm, respectively using methanol as solvent. Good linearity was obtained for sertaconazole over concentration of 10-60 μg/ml with R2 >0.99 at all the three wavelengths. The results of validation study were within acceptance limits as per ICH guidelines. The QbD instigated method for determination of sertaconazole nitrate can be highly effective for routine analysis purpose.

Poly(ethylene glycol)-block-poly(ε-caprolactone) nanomicelles for the solubilization and enhancement of antifungal activity of sertaconazole.

Sertaconazole nitrate is a broad spectrum imidazole antifungal agent with antibacterial and anti-inflammatory properties. However, its lipophilic nature and very poor aqueous solubility limit its use in the clinic. The aim of this study was to develop and characterize poly(ethylene glycol)-block-poly(ε-caprolactone) (PEG-b-PCL) polymeric nanomicelles for the solubilization and enhancement of sertaconazole antifungal activity. Sertaconazole was incorporated into PEG-b- PCL polymeric nanomicelles by a co-solvent evaporation method and micelle size, drug loading capacity and drug release properties were determined. The antifungal properties of nanomicelle-loaded drug were evaluated in Fusarium miscanthi, Microsporum canis, and Trichophyton mentagrophytes isolated, respectively from fungal keratitis, ringworm, and tinea corporis. PEG-b-PCL formed nanomicelles in aqueous solution with a diameter ranging from 40-80 nm, depending on the polymer composition and level of drug loading. Drug loading properties of the nanomicelles were dependent on the PCL block molecular weight and drug/polymer weight feed ratio. Drug encapsulation efficiency of up to 85% was achieved and this resulted in more than 80-fold enhancement in sertaconazole aqueous solubility at polymer concentration of 0.2%. Drug release studies showed an initial burst release followed by sustained drug release for 72 hours. In vitro antimycotic studies showed that nanomicelle-incorporated sertaconazole inhibited fungal growth in a concentration dependent manner. Further, it was more effective than the free drug in inhibiting the growth of Fusarium miscanthi and Microsporum canis. These results confirm the utility of PEG-b-PCL nanomicelles in enhancing the aqueous solubility and antifungal activity of sertaconazole or other similar antifungal drugs.

Microemulsion based topical hydrogel of sertaconazole: Formulation, characterization and evaluation

A microemulsion (ME) based hydrogel had studied as a topical delivery of sertaconazole (STZL) for effective eradication of cutaneous fungal infection. The existence of microemulsion region was investigated in pseudo-ternary phase diagrams and various ME formulations were prepared using oleic acid, Tween 80, propylene glycol and water. Hydrogel of STZL microemulsions (HSM) were prepared in Carbopol 940 (0.75%, w/w) and characterized. The prepared HSM and commercial cream of STZL were evaluated in vitro and ex vivo. The permeation rate of STZL from optimized formulation (HSM-4), composed with oleic acid (8.75%, w/w), tween 80 (33.35%, w/w), propylene glycol (33.35%, w/w) and water (24.55%, w/w) was observed higher in compare with other HSMs and commercial cream. HSM-4 was stable, had 3 times higher drug retention capacity in skin than commercial cream and did not caused any erythema or edema based on skin sensitivity study on rabbit. The average zone of inhibition of HSM-4 (23.54±0.72mm) was higher in compare with commercial cream (16.53±0.63mm) against Candida albicans which may be due to permeation enhancing effect of ME and skin retention effect of HSM. It is promising that the concentration of STZL used to treat cutaneous fungal infection could be decreased due to the high permeation and anti-fungal effect of STZL in HSM-4.

Effect of microemulsion in topical sertaconazole hydrogel: in vitro and in vivo study

Purpose: A topical microemulsion (ME)-based hydrogel was developed to enhance permeation of an antifungal drug, sertaconazole (STZL) for effective eradication of cutaneous fungal infection.Methods: Pseudo-ternary phase diagrams were used to determine the existence of MEs region. ME formulations were prepared with oleic acid, Tween 80, propylene glycol (PG) and water. Carbopol 940 (0.75% w/w) was used for preparation of hydrogel of STZL microemulsion (HSM) and characterized. The in vitro and in vivo evaluation of prepared HSM and commercial cream of STZL were compared.Results: The viscosity, average droplet size and pH of HSM were 154.23 ± 0.54 to 162.52 ± 0.21 Pas, 42.3–91.7 nm and 6.9–7.2 , respectively. Permeation rate of STZL from optimized formulation (HSM-4), composed with oleic acid (8.75 % w/w), Tween 80 (33.35% w/w), PG (33.35% w/w) and water (24.55% w/w) was observed higher in compare with other HSMs and commercial cream. HSM-4 was stable, three times higher drug retention capacity in skin than commercial cream and did not caused any erythema or edema based on skin sensitivity study on rabbit. The average zone of inhibition of HSM-4 (23.54 ± 0.72 mm) was higher in compare with commercial cream (16.53 ± 0.63 mm) against Candida albicans.Conclusion: The results of study showed that ME played a major role in permeation enhancing and skin retention effect of HSM and the concentration of STZL used for cutaneous fungal infection could be decreased by using ME based hydrogel preparation.

Design expert assisted formulation of topical bioadhesive gel of sertaconazole nitrate.

The objective of this work was to develop a bioadhesive topical gel of sertaconazole nitrate with the help of response-surface approach. Experiments were performed according to a 3-level factorial design to evaluate the effects of two independent variables [amount of Carbapol 934 = X1) and Sodium carboxymethylcellulose (NaCMC) = X2)] on the bioadhesive character of gel, rheological property of gel (consistency index), and in-vitro drug release. The best model was selected to fit the data. Mathematical equation was generated by Design Expert® software for the model which assists in determining the effect of independent variables. Response surface plots were also generated by the software for analyzing effect of the independent variables on the response. The effect of formulation variables on the product characteristics can be easily predicted and precisely interpreted by using a 3-level factorial design and generated quadratic mathematical equations. On the basis of product characteristics viscosity, bioadhesiveness, permeation study, in-vitro release, in-vivo studies, TPA and spreadability it can be concluded that the best batch of topical bioadhesive gel of Sertaconazole nitrate would be with 1% Carbopol 934 and 1% NaCMC.

COMPARATIVE EVALUATION OF NEWER TOPICAL ANTIFUNGAL AGENTS IN THE TREATMENT OF SUPERFICIAL FUNGAL INFECTIONS (TINEA OR DERMATOPHYTIC)

Within the past few years, new extended - spectrum triazoles and allylamines have been introduced into market. Few of them include Luliconazole, Sertaconazo le and Amorolfine. It is a multicentric, randomized, open - label, comparative study to evaluate the efficacy of newer antifungal drugs. A total 150 patients needed to be enrolled in the study based on the inclusion and exclusion criteria. All the patients a re aged between 18 to 80 years. Patients above the age of 18 with clinical evidence of cutaneous mycoses (commonest pres entation - tinea corporis) were treated with newer antifungals like Luliconazole, Sertaconazo le, Amorolfine and eber conazole and Terbin afine and a potassium hydroxide (KOH) preparation of scrapings from a selected lesion was examined microscopically and clinically evaluated. The symptoms and signs of erythema, scaling and pruritus were scored on a scale of 1 (nil) to 3 (severe). Patients were eligible for the study if they had a combined score of at least 5. S ertaconazole showed higher efficacy with 93.3% (p<0.05) and also found to produce least percentage of adverse events with 6.6% compared to other antifungals . Sertaconazole proved to be highly efficient compared to other newer antifungals in terms of efficacy and safety.

Efficacy of Topical Antifungals in the Treatment of Dermatophytosis

Considering that most randomized controlled trials compare antifungals with placebo instead of other antifungals, conventional meta-analysis is insufficient to define superiority between the evaluated strategies. To our knowledge, this is the first mixed-treatment comparison meta-analysis on antifungal treatments in the literature and shows all the evidence available at the time of the study. To evaluate and compare the efficacy of topical antifungals used in dermatophytosis treatment, using mixed-treatment comparisons. We performed a comprehensive search (up to July 31, 2012) for all entries in MEDLINE, Cochrane Central Register of Controlled Trials, EMBASE, Literatura Latino Americana e do Caribe em Ciências da Saúde, and International Pharmaceutical Abstracts. Randomized controlled trials that compared topical antifungals with one another or with placebo in dermatophytosis treatment were selected for analysis. Methodologic quality of the trials was assessed using the Jadad scale. We excluded studies that scored less than 3 points. The outcomes evaluated were mycologic cure at the end of treatment and sustained cure. A random-effects Bayesian mixed-treatment comparisons model was applied to combine placebo-controlled and direct topical antifungals comparison trials. RESULTS Pooled data of the 65 trials identified did not show any statistically significant differences among the antifungals concerning the outcome of mycologic cure at the end of treatment. Regarding the sustained cure outcome, butenafine hydrochloride and terbinafine hydrochloride were significantly more efficacious than were clotrimazole, oxiconazole nitrate, and sertaconazole nitrate. Terbinafine also demonstrated statistical superiority when compared with ciclopirox (ciclopiroxolamine), and naftifine hydrochloride showed better response compared with oxiconazole. No inconsistency was detected in the network of evidence for both outcomes, sustaining the validity of the mixed-treatment comparisons results. With the outcome mycologic cure at the end of treatment, there was no significant difference among the antifungals. Butenafine, naftifine, and terbinafine might be the best strategies for maintaining cured status. Because of the different costs of the antifungals, pharmacoeconomic analysis is required to identify the most efficient strategy for dermatophytosis management.

Atrophying pityriasis versicolor

A 26-year-old woman presented with scaly atrophic erythema on the chest and abdomen for nearly 2 years.Direct microscopic examination of the lesion scrapings revealed numerous stubby hyphae and clustered spores.Periodic acid-Schiff (PAS) staining of the biopsy tissue showed the presence of numerous hyphae and spores in the horny layer.The stain for elastic fibers revealed that the number of elastic fibers decreased,and some elastic fibers became fine and disrupted.The patient was diagnosed with atrophying pityriasis versicolor.The lesions subsided and direct microscopic examination was negative after 1-week treatment with oral itraconazole of 200 mg once daily and 4-week treatment with topical 2％ sertaconazole cream.

Nasal Cutaneous Infection in a Healthy Boy Caused by Fusarium moniliforme

A healthy 10-year-old Chinese boy developed verrucous plaques on the nose. The fungus was identified as Fusarium moniliforme via culture of biopsy fragments. The patient had normal immune status and was successfully treated with oral itraconazole (100 mg/day) for 2 months and application of oral itraconazole and topical sertaconazole nitrate cream. Fusarium is a ubiquitous hyalohyphomycete isolated from food that is also widespread in the environment and is present at all latitudes. Infections due to this mold may be disseminated or localized. Fusarium species have been known to colonize the cornea, nails, and burn eschars in otherwise healthy patients. Cutaneous and disseminated infections have been reported mostly in immunocompromised hosts. Here we describe an unusual case of localized infection caused by Fusarium moniliforme in an otherwise healthy child, with significant improvement after 2 months of oral itraconazole and topical sertaconazole nitrate cream therapy.

Efficacy and safety of terbinafine hydrochloride 1% cream vs. sertaconazole nitrate 2% cream in tinea corporis and tinea cruris: A comparative therapeutic trial

Context:To the best of our knowledge, till date no study comparing the efficacy and safety of terbinafine hydrochloride 1% cream and sertaconazole nitrate 2% cream has been done in localized tinea corporis and tinea cruris.Aims:This clinical trial was carried out to study and compare the efficacy of topical terbinafine hydrochloride 1% cream and sertaconazole nitrate 2% cream in localized tinea corporis and tinea cruris and to know the adverse effects of these antifungal creams.Settings and Design:In this prospective, single blind, randomized control trial with two arms, patient were randomized into two groups Group A (treatment with terbinafine cream) and Group B (treatment with sertaconazole cream). A total of 38 patients were enrolled for the study, 20 patients in group A and 18 patients in group B. But five patients of group A and three patients of group B were lost for follow-ups. Therefore sample size was of 30 patients with 15 patients in group A and group B each.Materials and Methods:Patients in group A and B were treated with twice daily topical 1% terbinafine hydrochloride and 2% sertaconazole nitrate cream respectively for a total duration of three weeks. Clinical improvement in signs and symptoms of each clinical parameter, namely itching, erythema, papules, pustules, vesicles, and scaling were graded weekly and clinical cure was assessed. KOH mount and culture was done weekly up to 3 weeks to access mycological cure. Fungal culture was done on Sabouraud's dextrose agar with chloramphenicol and cycloheximide.Statistical Analysis Used:Statistical analysis was done using students paired and unpaired t-tests from the data obtained.Results:Comparison between Group A and Group B for complete cure (clinical and mycological) showed that at the end of 3 weeks both terbinafine and sertaconazole groups had 100% complete cure. When the two groups were compared for complete cure, at the end of 1st and 2nd week, statistically non-significant results were observed (P = 0.461 and P = 0.679 respectively). However, at the end of 2nd week, complete cure rate for terbinafine was 80% as compared to 73.35% for sertaconazole with no statistical significance. In both Group A and Group B, clinically significant local side effects like erythema, swelling, stinging sensation, or increased itching were not noticed. A majority of our patients in both the group showed Trichophyton rubrum followed by Trichophyton mentagrophytes growth on culture. In Group A, 11 patients showed growth of T. rubrum, 2 patients showed growth of T. mentagrophytes, and 1 patient had only KOH test positive. In Group B, 10 patients revealed growth of T. rubrum, followed by growth of T. mentagrophytes in 3 and Microsporum canis in 2 patients. The therapeutic response is more or less same in infection with different species.Conclusions:The newer fungistatic drug sertaconazole nitrate 2% cream was as effective as terbinafine hydrochloride 1% cream which is one of the fungicidal drugs, though terbinafine hydrochloride 1% cream has higher rates of complete cure at the end of 2 weeks as compared to sertaconazole nitrate 2% cream. Both the drugs showed good tolerability with no adverse effects.

Sertaconazole Antifungal Profile Determined by a Microdilution Method versus Nine Topical Substances against Dermatophyte Fungi

Antifungal activity and in vitro inhibition time for sertaconazole (STZ) and 9 other topical drugs, namely amorolfine, bifonazole, clotrimazole, econazole, ketoconazole, miconazole, oxiconazole, terbinafine, and tioconazole were determined against 124 clinical isolates of dermatophyte (12 species) fungi by the microdilution method in a liquid medium and the measurement of optical density. STZ’s antifungal activity was not always affected by the tested dermatophyte genus, as was the case with the remaining antifungals. In vitro antifungal activity was at the same level for all the studied azole derivatives, but, in terms of partial inhibitory concentrations, STZ starts its in vitro inhibitory activity in a shorter time than the other tested substances, particularly in those incubation periods when the growth of the dermatophyte fungi was more developed.