Econazole Research Articles

Enhanced imaging of developed fingerprints and its contaminated substance using ToF-SIMS

Fingerprint is a common form of evidence utilized in crime cases, providing crucial information for suspect identification and the proof of key facts. However, traditional development methods are often ineffective for challenging fingerprints due to variations in information and surface characteristics, potentially causing damage to the fingerprint substance. Time-of-flight secondary ion mass spectrometry (ToF-SIMS) offers a non-destructive approach that combines spatial imaging with mass spectrometry capabilities. This study employed ToF-SIMS to enhance natural fingerprints that showed poor visualization when treated with 1,2-indandione and ninhydrin on porous surfaces such as printing paper, kraft paper, newspaper, and thermal paper, especially on challenging textiles. We also imaged fingerprints on nonporous surfaces that were deposited over 30 days ago using ToF-SIMS, like aluminum foil, express packaging bags, and slides. We then extended the age of fingerprint detection to 3 months to explore the relationship between the aging of fingerprints and the morphological characteristics of sweat pores. Furthermore, the study examined the detection capabilities of ToF-SIMS on fingerprints contaminated with compound econazole nitrate cream after being interfered with by development agents, illustrating its effectiveness in extracting comprehensive fingerprint information.

Structural mechanism of TRPV5 inhibition by econazole

The calcium-selective TRPV5 channel activated by phosphatidylinositol 4,5-bisphosphate [PI(4,5)P2] is involved in calcium homeostasis. Recently, cryoelectron microscopy (cryo-EM) provided molecular details of TRPV5 modulation by exogenous and endogenous molecules. However, the details of TRPV5 inhibition by the antifungal agent econazole (ECN) remain elusive due to the low resolution of the currently available structure. In this study, we employ cryo-EM to comprehensively examine how the ECN inhibits TRPV5. By combining our structural findings with site-directed mutagenesis, calcium measurements, electrophysiology, and molecular dynamics simulations, we determined that residues F472 and L475 on the S4 helix, along with residue W495 on the S5 helix, collectively constitute the ECN-binding site. Additionally, the structure of TRPV5 in the presence of ECN and PI(4,5)P2, which does not show the bound activator, reveals a potential inhibition mechanism in which ECN competes with PI(4,5)P2, preventing the latter from binding, and ultimately pore closure.

Finite sample corrections for average equivalence testing.

Average (bio)equivalence tests are used to assess if a parameter, like the mean difference in treatment response between two conditions for example, lies within a given equivalence interval, hence allowing to conclude that the conditions have "equivalent" means. The two one-sided tests (TOST) procedure, consisting in testing whether the target parameter is respectively significantly greater and lower than some pre-defined lower and upper equivalence limits, is typically used in this context, usually by checking whether the confidence interval for the target parameter lies within these limits. This intuitive and visual procedure is however known to be conservative, especially in the case of highly variable drugs, where it shows a rapid power loss, often reaching zero, hence making it impossible to conclude for equivalence when it is actually true. Here, we propose a finite sample correction of the TOST procedure, the -TOST, which consists in a correction of the significance level of the TOST allowing to guarantee a test size (or type-I error rate) of . This new procedure essentially corresponds to a finite sample and variability correction of the TOST procedure. We show that this procedure is uniformly more powerful than the TOST, easy to compute, and that its operating characteristics outperform the ones of its competitors. A case study about econazole nitrate deposition in porcine skin is used to illustrate the benefits of the proposed method and its advantages compared to other available procedures.

Econazole selectively induces cell death in NF1-homozygous mutant tumor cells

Cutaneous neurofibromas (cNFs) are tumors that develop in more than 99% of individuals with neurofibromatosis type 1 (NF1). They develop in the dermis and can number in the thousands. cNFs can be itchy and painful and negatively impact self-esteem. There is no US Food and Drug Administration (FDA)-approved drug for their treatment. Here, we screen a library of FDA-approved drugs using a cNF cell model derived from human induced pluripotent stem cells (hiPSCs) generated from an NF1 patient. We engineer an NF1 mutation in the second allele to mimic loss of heterozygosity, differentiate the NF1+/- and NF1-/- hiPSCs into Schwann cell precursors (SCPs), and use them to screen a drug library to assess for inhibition of NF1-/- but not NF1+/- cell proliferation. We identify econazole nitrate as being effective against NF1-/- hiPSC-SCPs. Econazole cream selectively induces apoptosis in Nf1-/- murine nerve root neurosphere cells and human cNF xenografts. This study supports further testing of econazole for cNF treatment.

Development and Characterization of Econazole Topical Gel.

The purpose of this work was to develop a novel topical formulation of econazole nitrate based on gel that can be easily scaled up in one pot for the potential treatment of fungal and yeast infections. Econazole nitrate, a topical antifungal, is used to treat tinea versicolor, tinea pedis, and tinea cruris. Compared to applying cream or ointment, topical gels offer numerous advantages, one of which is that the drug is released more quickly to the intended site of action. A viscous mixture of propylene glycol, Capmul® MCM C8, methyl and propyl paraben, and econazole nitrate were mixed together before being formulated into the optimized Carbopol® gel bases. The gel's color, appearance, and homogeneity were assessed visually. For every formulation, the drug content, pH, viscosity, spreadability, and gel strength were characterized. The cup plate diffusion method was used to evaluate the anti-fungal activity of the prepared formulations. To assess the behavior of the developed system, studies on in vitro release and mechanism were conducted. The manufactured formulations were transparent, pale yellow, and exhibited excellent homogeneity. The pH of each formulation was roughly 6.0, making them suitable for topical use. The concentration of Carbopol® 940 resulted in a significant increase in viscosity and gel strength but a significant decrease in spreadability. It was demonstrated that the prepared formulations inhibited the growth of Candida albicans and Aspergillus fumigatus. In contrast, the standard blank gel showed no signs of antifungal action. By increasing the concentration of Carbopol® 940, the in vitro release profile of econazole nitrate significantly decreased. Following the Korsmeyer-Peppas model fitting, all formulations exhibited n values greater than 0.5 and less than 1, indicating that diffusion and gel swelling control econazole nitrate release.

Imidazole based nanofungicides: antifungal efficacy against Rhizoctonia solani and biosafety assessment

Various nanotechnology advancements are used to protect crops and the safety concerns of nanopesticides for soil quality need to be addressed. Soil enzymes and certain beneficial bacteria play a vital role in preserving soil health by carrying out required biochemical reactions. In the present study, clotrimazole, econazole nitrate, and miconazole nitrate based nano-fungicides were investigated for their antifungal efficacy followed by their biosafety assessment. Antifungal studies of all the test nano-fungicides demonstrated their effectiveness against Rhizoctonia solani. The relative lesion heights were 29–38% under field conditions and they ranged from 17% to 33% in pot experiments. Impact of these nano-fungicides on urease activity in soil was comparable with the conventional fungicide hexaconazole, as evident from the presence of 0.5–2.7 mg/kg urea-nitrogen after 24 h of 200 mg/kg urea-nitrogen application. In all the treatments, the activity of soil nitrifiers was not adversely affected after application of these nano-fungicides. After 21 days of incubation, the nitrate-N contents were in the range of 150–180 mg/kg in nano-fungicide treated soils as compared to 180 mg/kg of nitrate-N in urea control. Virtual risk assessment using docking of these imidazole derivatives on soil enzymes revealed their behavior similar to that of hexaconazole.

Design, Development and Characterization of Econazole loaded Nanoparticles for Topical Application

Background and Objectives: Econazole nitrate (ECN) loaded nanoparticles with topical administration were the focus of the current study, which aimed to improve the topical efficacy of the medicine in treating fungal infections while also mitigating the drug’s gastrointestinal (GI) side effects. Further colloidal carrier methodology was employed as a method for the topical administration of medications with precision. Method: The emulsification-diffusion (E-D) method is an alternate approach for preparing nanogels that avoids the toxicitysolvent issues associated with the emulsification-evaporation technique. Its ease of use, enhanced stability, and adaptability have all been verified by a variety of research groups. ECN loaded with dichloromethane in stabilizer solution, formulated by high-speed homogenization at elevated pressure. The addition of aqueous phase with repeated homogenization cycles causes drug diffusion into nanogels. Further addition of mannitol as cryoprotectant and Carbapol 940 as gelling agent stabiles the formulation. Results: The typical size of the particles, polydispersity index (PDI), and zeta potential were all measured with the use of the Malvern zetasizer. Of the five NFs, the lyophilized batch of NF3 exhibited the lowest zeta potential (-11.6 mV) and the PDI (0.208), indicating that the composition was stable. DSC and XRD analysis revealed an amorphous transformation of ECN. The scanning electron micrograph demonstrated discrete, roundish particles. The existence, viscosity, and spreading ability of a gelled dispersion of the selected NLCs were evaluated. Total od 77% of the medication was released in-vitro from a chosen formulation of ECN-loaded nanogels. As a result, it is reasonable to assume that ECN-loaded nanogels are an effective drug delivery system for treating fungal infections since they prolong the duration of drug release. Conclusion: Under degraded conditions, there are not any peaks that conflict with one another. As a result, a technique was developed that is highly applicable due to its sensitivity, strength, accuracy, and demonstration of stability.

The effect of charges on the corneal penetration of solid lipid nanoparticles loaded Econazole after topical administration in rabbits

Fungal keratitis is an infectious disease caused by pathogenic fungi with a high blindness rate. Econazole (ECZ) is an imidazole antifungal drug with insoluble ability. Econazole-loaded solid lipid nanoparticles (E-SLNs) were prepared by microemulsion method, then modified with positive and negative charge. The mean diameter of cationic E-SLNs, nearly neutral E-SLNs and anionic E-SLNs were 18.73±0.14, 19.05±0.28, 18.54±0.10 nm respectively. The Zeta potential of these different charged SLNs formulations were 19.13±0.89, -2.20±0.10, -27.40±0.67 mV respectively. The Polydispersity Index (PDI) of these three kinds of nanoparticles were all about 0.2. The Transmission Electron Microscopy (TEM) and Differential Scanning Calorimetry (DSC) analysis showed that the nanoparticles were a homogeneous system. Compared with Econazole suspension (E-Susp), SLNs exhibited sustained release capability, stronger corneal penetration and enhanced inhibition of pathogenic fungi without irritation. The antifungal ability was further improved after cationic charge modification compared with E-SLNs. Studies on pharmacokinetics showed that the order of the AUC and t1/2 of different preparations was cationic E-SLNs > nearly neutral E-SLNs > anionic E-SLNs > E-Susp in cornea and aqueous humor. It was shown that SLNs could increase corneal penetrability and ocular bioavailability while these capabilities were further enhanced with positive charge modification compared with negative charge ones.

Inverse psoriasis: the diagnostic value of dermatoscopic assessment and the experience of treatment with a combination topical agent (a clinical series)

Background: Inverse psoriasis that is characterized by skinfold rash is seen in 12 to 36% of European patients with psoriasis. Isolated involvement of skinfolds can mimic a number of dermatoses with similar location. The differential diagnosis is increasingly frequently based on non-invasive methods, including dermatoscopy. Taking into account the warm and wet milieu of skinfolds, facilitating secondary infection, topical antibacterials and antiseptics are recommended for treatment, along with topical glucocorticosteroids and vitamin D3 analogues.
 Materials and methods: We have analyzed the results of assessment and treatment of 15 patients with psoriasis of major skinfolds that were admitted to the in-patient department of dermatology. All patients underwent dermatoscopy at 20 magnification. The patients were treated with desensitizing agents, hepatic protectors, and group B vitamins. Topical treatments applied in the rash areas included a combination topical agent containing mometasone furoate (0.5 mg), gentamicin sulfate (1 mg), econazole nitrate (10 mg), and dexpanthenol (50 mg). The treatment was considered effective if the M-PASI decreased at least by 75%; the results were assessed after 7 and 14 days of treatment.
 Results: In all cases, dermatoscopy of the vulgar psoriasis lesions showed vermilion or red to rosy background with evenly distributed dotted vessels and white scales diffusely located all over the visualized surface. The skinfold lesions were characterized by rosy or red background with evenly distributed dotted vessels, white scales located either as isolated groups, or at the periphery of the visualized areas; some plaques had local erosions, and in one case, hemorrhages. Morphological assessment of the biopsy samples in all patients with isolated skinfold lesions (n = 5) confirmed the diagnosis of psoriasis. Treatment-induced improvement was seen at day 2 to 3, and at day 14, there was a decrease of M-PASI by 90% in 6 (40%) patients and resolution of the lesions in 9 (60%). There were no treatment-associated adverse events or reactions.
 Conclusion: Dermatoscopy has proved to be a useful tool for non-invasive diagnostics of inverse psoriasis. At low magnification ( 20), its main sign was an even distribution of dotted vessels throughout the visualized area. In a number of cases, the dermatoscopic symptoms additionally included white scales grouped as isolated foci. The addition of the combination topical agent (mometasone furoate, gentamicin sulfate, econazole nitrate, and dexpanthenol) to the standard systemic therapy facilitated almost full resolution of skinfold psoriatic lesions.

Studies on Development and Evaluation of Topical Ethosomal Gel Embedded Antifungal Agent for Athlete's Foot

BackgroundnbspAthletes foot also known as lsquotinea pedisrsquo is a fungal skin infection caused by different fungi and is associated with itching scaling cracking and redness. Several topical products of antifungal agents such as lotions sprays powders creams jellies and pastes are applied for treating fungal skin infections. All these topical formulations have certain potential bioavailability issues such as less residual time poor skin permeability and absorption thus resulting in poor patient compliance.AimnbspTo formulate and evaluate a novel vesicular carrier Econazole nitrate ECN as Ethosomes in the form of gel for improving antifungal activity against Athletes foot.MethodsnbspIn the present study ECN drug loaded ethosomal vesicular suspension formulations ES-1 ES-2 ES-3 ES-4 were prepared by solvent dispersion technique by mixing ECN with other excipients. Further ethosomal gel of ECN EG-5 EG-6 EG-7 EG-8 was formulated by adding 0.5 0.8 1.0 1.5 wv of Carbopol into the vesicular suspension. The drug-excipient interactions were evaluated using Fourier-transform infrared FT-IR spectroscopy and differential scanning calorimeter DSC while shape and surface characteristics were assessed using scanning electron microscopy SEM. In vitro drug release of gel was examined in phosphate buffer pH-7.4 by Franz diffusion cell technique.ResultsnbspAll rheological properties of gel showed satisfactory results. No significant drug-excipient interactions were observed in FT-IR and DSC. While increase in concentrations of soya lecithin and carbopol influenced vesicular shape and surface morphology particle size zeta potential and drug entrapment efficiency the in vitro drug release significantly increased from carbopol drug loaded ethosomal gel.ConclusionnbspThe formulated carbopol drug loaded ethosomal gel enhanced residential time permeability of drug and provided greater bioavailability to improve therapy.

Development and Optimization of Cubosomal Econazole Nitrate

Development and Optimization of Cubosomal Econazole Nitrate

A Biocompatible Liquid Pillar[n]arene-Based Drug Reservoir for Topical Drug Delivery.

Advanced external preparations that possess a sustained-release effect and integrate few irritant elements are urgently needed to satisfy the special requirements of topical administration in the clinic. Here, a series of liquid pillar[n]arene-bearing varying-length oligoethylene oxide chains (OEPns) were designed and synthesized. Following rheological property and biocompatibility investigations, pillar[6]arene with triethylene oxide substituents (TEP6) with satisfactory cavity size were screened as optimal candidate compounds. Then, a supramolecular liquid reservoir was constructed from host-guest complexes between TEP6 and econazole nitrate (ECN), an external antimicrobial agent without additional solvents. In vitro drug-release studies revealed that complexation by TEP6 could regulate the release rate of ECN and afford effective cumulative amounts. In vivo pharmacodynamic studies confirmed the formation of a supramolecular liquid reservoir contributed to the accelerated healing rate of a S. aureus-infected mouse wound model. Overall, these findings have provided the first insights into the construction of a supramolecular liquid reservoir for topical administration.

FTIR SPECTRAL CHANGES IN Candida albicans BIOFILM FOLLOWING EXPOSURE TO ANTIFUNGALS

Candida albicans is a microbial fungus that exists as a commensal member of the human microbiome and an opportunistic pathogen. Biofilm formation by this fungal pathogen occurs mostly in the mucosa or endothelium associated with candidiasis and colonizes medical devices. The present work was performed to determine the efficacy of the antifungal creams on the viability and biochemical composition of C. albicans biofilm. Four commercial antifungal creams were used herein namely econazole nitrate, miconazole nitrate, ketoconazole and tolnaftate. Resazurin assay and Fourier transform infrared (FTIR) spectroscopy were performed to determine the viability and biochemical composition of C. albicans biofilm, respectively. Results demonstrated that the antifungal creams inhibited C. albicans biofilm. The highest percent inhibition shown by econazole nitrate, miconazole nitrate, ketoconazole, and tolnaftate were 16.5%, 17.1%, 15.8%, and 6.9%, respectively. Econazole nitrate with the lowest IC50 value of 43.42 µg/mL caused changes in the FTIR spectral peak shape at 1377 cm-1 and 1736 cm-1. On the other hand, miconazole nitrate with the second lowest IC50 value of 118.26 µg/mL caused spectral peak shifting from 1237 cm-1 to 1228 cm-1. In conclusion, the inhibition of C. albicans biofilm may be mediated by the changes in protein, lipid, and nucleic acid compositions.

Antifungal Nail Lacquer for Enhanced Transungual Delivery of Econazole Nitrate.

The fungal disease of the nail, onychomycosis, which is also the most prevalent nail disturbance, demands effective topical treatment options considering the possible adverse effects of systemic antifungal therapy. The current work is focused on development of an adhesive and resistant, drug-delivering and permeation-enhancing polymeric film containing econazole nitrate (ECN) for topical antifungal treatment. The development of the lacquer formulation was guided by the Quality by Design approach to achieve the critical quality attributes needed to obtain the product of desired quality. Eudragit RSPO at 10% w/w was found to be the ideal adhesive polymer for the application and an optimal permeation-enhancing lacquer formulation was achieved by the optimization of other formulation excipients, such as plasticizer and the solvent system. Additionally, novel experimental enhancements introduced to the research included refined D50 drying time and drying rate tests for lacquer characterization as well as a multi-mechanism permeation-enhancing pre-treatment. Moreover, a practical implication was provided by a handwashing simulation designed to test the performance of the lacquer during actual use. In vitro drug release testing and ex vivo nail permeation testing demonstrated that the optimized nail lacquer performed better than control lacquer lacking the permeation enhancer by achieving a faster and sustained delivery of ECN. It can be concluded that this is a promising drug delivery system for topical antifungal treatment of onychomycotic nails, and the novel characterization techniques may be adapted for similar formulations in the future.

Polycomponent drugs in the treatment of intertriginous dermatosis

The most common localization of dermatoses of combined etiology are intertriginous areas. In recent years, an increase in the number of patients suffering from dermatoses of combined etiology has been recorded. The reasons for this situation can be both irrational therapy and background comorbidities in the patient, as well as a number of anatomical and physiological prerequisites for the formation and maintenance of an inflammatory infectious process with localization, namely in the area of skin folds. The article describes in detail the anatomical and physiological features of these areas, the causes of the development of dermatosis of the combined etiology of the fold area. Epidemiological and statistical data on the distribution of a combination of acute, chronic, infectious and non-infectious dermatoses, the causes and frequency of their occurrence are given. Particular attention is paid to the microbiocenosis of the skin in various dermatoses with an emphasis on intertriginous localizations. Approaches to the treatment of such conditions involve the use of combined external agents containing topical corticosteroids, antimicrobial and antifungal components. The article presents data available in the literature on the effectiveness of the use of a multicomponent preparation – Tetraderm cream (consisting of an antibiotic-aminoglycoside + tissue repair stimulant + GCS for local use + an antifungal agent – econazole nitrate) for various dermatoses localized in intertriginous areas. We present our own clinical observations of the effectiveness of the use of this polycomponent preparation Tetraderm in the treatment of patients with skin lesions of combined etiology in the area of folds in atopic dermatitis, allergic dermatitis, mycotic, staphylo-streptococcal infections occurring in combination.

A Composite System Based upon Hydroxypropyl Cyclodextrins and Soft Hydrogel Contact Lenses for the Delivery of Therapeutic Doses of Econazole to the Cornea, In Vitro.

Fungal keratitis, a disease in which the cornea becomes inflamed due to an invasive fungal infection, remains difficult to treat due in part to limited choices of available treatments. Topical eye drops are first-line treatment, but can be ineffective as low levels of drug reach the target site due to precorneal losses and the impenetrability of the cornea. The aim of this study was to determine the corneal delivery of econazole using a novel topical enhancement approach using a composite delivery system based upon cyclodextrins and soft hydrogel contact lenses. Excess econazole nitrate was added to hydroxypropyl-α-cyclodextrin (HP-α-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) solutions, and the solubility determined using HPLC. Proprietary soft hydrogel contact lenses were then impregnated with saturated solutions and applied to freshly enucleated porcine eyeballs. Econazole nitrate ‘eye drops’ at the same concentrations served as the control. After 6 h, the corneas were excised and drug-extracted, prior to quantification using HPLC. Molecular dynamic simulations were performed to examine econazole–HP-β-CD inclusion complexation and dissociation. The minimum inhibitory concentration (MIC) of econazole was determined against four fungal species associated with keratitis, and these data were then related to the amount of drug delivered to the cornea, using an average corneal volume of 0.19 mL. The solubility of econazole increased greatly in the presence of HP-β-CD and more so with HP-α-CD (p < 0.001), with ratios >> 2. Hydrogel contact lenses delivered ×2.8 more drug across the corneas in comparison to eye drops alone, and ×5 more drug delivered to the cornea when cyclodextrin was present. Molecular graphics demonstrated dynamic econazole release, which would create transient enhanced drug concentration at the cornea surface. The solution-only drops achieved the least satisfactory result, producing sub-MIC levels with factors of ×0.81 for both Fusarium semitectum and Fusarium solani and ×0.40 for both Scolecobasidium tshawytschae and Bipolaris hawaiiensis. All other treatments delivered econazole at > MIC for all four fungal species. The efficacies of the delivery platforms evaluated were ranked: HP-α-CD contact lens > HP-β-CD contact lens > contact lens = HP-α-CD drops > HP-β-CD drops > solution-only drops. In summary, the results in this study have demonstrated that a composite drug delivery system based upon econazole–HP-β-CD inclusion complexes loaded into contact lenses can achieve significantly greater corneal drug delivery with the potential for improved clinical responses.

Diversity of Parengyodontium spp. strains isolated from the cultural heritage environment: Phylogenetic diversity, phenotypical diversity, and occurrence

ABSTRACT Parengyodontium album is a fungal species that frequently occurs in the cultural heritage environment. Although three subclades were initially described in the species, no study has sought to determine the occurrence of each subclade in the cultural heritage context. These subclades are easily distinguishable phylogenetically, but their morphological identification is more difficult. Eighteen strains isolated from different cultural sites and initially identified as P. album were studied phylogenetically, morphologically, and in terms of their susceptibility to econazole nitrate 0.2%, an antifungal product used as preservation treatment in cultural heritage domain. The phylogenetic study revealed that all studied strains belonged to P. album subclade 1 or P. torokii (P. album subclade 3) and none belonged to P. album subclade 2. The morphological study revealed the best characteristics to differentiate the three subclades/species, namely, the ability of the strains to grow at 32 C and 35 C on potato dextrose agar (PDA) medium and the shape of conidia. Finally, the strains displayed variable susceptibilities to econazole nitrate, with no apparent link to any particular subclade/species.

The results of open-label, randomized, actively-controlled study of the efficacy, safety and tolerability of the novel combined product (terbinafine hydrochloride + econazole nitrate), medicinal nail polish for local monotherapy of onychomycosis

Background. Currently, onychomycosis is an urgent and widespread problem in dermatology. The defeat of the nail plates is the cause of a cosmetic defect and a decrease in the quality of life of patients. Systemic antimycotics are effective, but have a number of side effects when used. Thus, a modern and effective approach to the treatment of patients with this pathology is needed.&#x0D; The aim of the study. To prove the efficacy, safety and tolerability of Ekzilak as local monotherapy of onychomycosis compared with cyclopyrox monotherapy.&#x0D; Materials and methods. А randomized open-label study with active control included 172 outpatient subjects: men and women aged 18 to 75 years, with microscopically confirmed onychomycosis of the big toe (one or both feet), a superficial or distal form of onychomycosis with a lesion of no more than 1/3 of the nail length (KIOTOS from 1 to 6). Patients were randomized into two groups: the 1st group of patients applied Ekzilak locally daily for 6 months, the 2nd group of patients applied Ciclopirox nail lacquer topical solution 8% as follows: 1 time a day for the first month, 2 times a week for the second one and 1 time a week for the months third-sixth. The preparations were applied in a thin layer to the affected nail. The primary efficacy endpoint in the study was the proportion of patients who achieved complete recovery of the target toenail at the end of therapy (clinical + mycological recovery). Secondary endpoints included the proportion of patients who achieved clinical recovery after 6 months of treatment (clinical recovery is a complete restoration of the normal morphology of the affected nail), the proportion of patients who achieved mycological recovery (microscopy with KOH solution) after 3 months of treatment, the proportion of patients who achieved complete recovery of the target toenail in 4 weeks after the end of treatment; IGA (Investigator's Global Assessment), Integrated Medicine Patient Satisfaction Scale (IMPSS); the safety Analysis was carried out throughout the study and included an assessment of adverse events, laboratory data, vital signs.&#x0D; Results. The results of the study showed that Ekzilak is superior in terms of efficacy to the registered drug Ciclopirox nail lacquer topical solution 8% as a local monotherapy of onychomycosis. The difference in the proportion of patients who achieved complete recovery between the study drug and the reference drug was 22.09%, 95% CI for the difference in the proportion was [8.21%; 35.97%], the differences between the groups are statistically significant (p=0.002). At the same time, the analysis of safety data, including the assessment of adverse events, laboratory studies and impact on vital signs, did not reveal statistically and clinically significant differences between the treatment groups.&#x0D; Conclusions. New combination drug Ekzilak is an effective and safe treatment option for patients with onychomycosis.

Formulation and evaluation of econazole nitrate microemulsion

Econazole Nitrate microemulsion is presently considered as the novel drug delivery system. It shows prolonged action. It is considered as the imidazole antifungal agent which shows broad spectrum activity. Antifungal agent contains the lipophilic groups which are administered in the microemulsions as they are able to penetrate the system easily. It belongs to BCS Class II drug. i.e., low soluble and highly permeable. The drug efficacy of topical formulation is limited to instability due to poor solubility and low permeability. These are the basic reasons which increase the scope for designing of microemulsion. The topical microemulsion containing Econazole Nitrate prepared using oleic acid as the oil phase, tween 20 as surfactant and propylene glycol as co- surfactant. The optimized formulation B1 was evaluated for various tests such as Particle size, Zeta potential, pH, Viscosity, Scanning electron microscopy and Electrical conductivity.

Pilot study of tolerability and safety of combination product containing terbinafne hydrochloride and econazole nitrate

Therapy of onychomycosis today presents a number of diffculties, and the effect does not always meet the expectations of patients. The purpose of the study. To study the tolerability and safety of the use of the drug Exilac(terbinafne hydrochloride + econazole nitrate), medical nail polish for external use. Methods. Eighteen volunteers participated in a pilot, prospective, monocentre, open-label tolerability and safety study. The study lasted 6 weeks and consisted of screening and fve visits, at each visit a visual examination, laboratory and instrumental examination methods were performed. Results. Eighteen healthy volunteers aged 18 to 34 participated in the study. Adverse events associated with the application of the study drug Exilac were observed in 1 (5.56%) volunteer, in the form of signs of delamination of the nail plate of the 1st fnger. This phenomenon is associated with mechanical damage to the nail plate when removing the old layer of the study drug and was regarded as a minor adverse event of mild severity. The remaining adverse events were not related to the use of the drug. Conclusion. The combined drug Exilac, when used twice daily for 6 weeks, demonstrated a high level of tolerability and safety.