Terbinafine Research Articles

Fabrication of β-cyclodextrin-based microgels for enhancing solubility of Terbinafine: An in-vitro and in-vivo toxicological evaluation

Abstract Solubility enhancement of poorly aqueous-soluble drugs, like Terbinafine (TBN), is a critical challenge in formulating effective dosage forms. This study focused on developing β-cyclodextrin (β-CD) and polyacrylamide (PAM)-based microgels to address the solubility issue of TBN, classified as a biopharmaceutics classification system class II drug. The microgels were crafted through free radical polymerization, employing methylene bisacylamide as a cross-linker and methacrylic acid as a monomer, initiated by ammonium persulfate. Comprehensive characterizations, including Fourier transform infrared, thermo-gravimetric analysis, differential scanning calorimetry, scanning electron microscopy, powder X-ray diffractometry analysis, Zeta size, and Zeta potential, were conducted. In vitro studies, such as drug release and swelling, were performed at pH 1.2. Toxicity analysis in rabbits revealed zero toxicity. These β-CD/PAM microgels successfully enhanced the solubility of TBN.

Case of tinea corporis caused by a terbinafine-sensitive Trichophyton indotineae strain in a Vietnamese worker in Japan.

A 42-year-old Vietnamese egg factory worker in Ishikawa prefecture, Japan, presented with itchy concentric erythema on the trunk and left calf. The lesions tested positive by direct potassium hydroxide examination, and two fungal strains were isolated. The isolates produced conidia abundantly and were morphologically indistinguishable from Trichophyton mentagrophytes/interdigitale, but were identified as Trichophyton indotineae by internal transcribed spacer sequence of ribosomal DNA. The lesions were refractory to treatment with topical luliconazole (LLCZ) cream for 4 weeks but subsided with oral itraconazole (ITCZ) 100 mg/day for 4 weeks in combination with topical lanoconazole (LCZ) cream. The lesions recurred 6 weeks after discontinuation of oral ITCZ, and an additional isolate was cultured. The minimum inhibitory concentrations of antimycotics for the isolate cultured at the first visit were: terbinafine (TBF) 0.03 μg/mL, ITCZ 0.015 μg/mL, LLCZ 0.0005 μg/mL, and LCZ 0.002 μg/mL. No TBF-resistant mutation in the amino acid sequence of squalene epoxidase, i.e., Leu 393 Ser/Phe or Phe 397 Leu, was detected in the isolate. The reason for recalcitrance in this case, despite the isolate's sensitivity to antimycotics, was unclear. Possible factors include insufficient use of the antimycotics, incomplete removal of abundantly produced conidia from the lesions, the patient's environment, and a language gap between the patient and physician hindering communication.

Development of formulation and evaluation of topical micro emulsion gel loaded with terbinafine HCL micro emulsion

Fungal infections, particularly in immunocompromised patients, present significant health challenges and are often difficult to treat with conventional topical therapies due to bioavailability issues. This study explores the development of a topical gel formulation using solid lipid nanoparticles (SLNs) loaded with Terbinafine, an antifungal agent, to improve drug delivery and efficacy. SLNs were prepared by a solvent diffusion method and optimized with stearic acid and poloxamer 188. The formulation with the highest entrapment efficiency (SLN F6) exhibited 92.13% ± 0.975. The optimized SLN formulation was incorporated into a gel base containing carbopol 934, resulting in SLN gel G3 with 1.5% carbopol showing the highest drug entrapment (91.39% ± 0.187). The gel was evaluated for physicochemical properties, including viscosity (369 cP), pH (6.12 ± 0.255), and spreadability (4.5). In vitro release studies indicated controlled drug release, fitting best with the Higuchi and Korsmeyer-Peppas models. FTIR analysis confirmed no significant interactions between the drug and excipients, supporting the formulation's purity and effectiveness. Scanning electron microscopy (SEM) confirmed the spherical shape and smooth surface of the nanoparticles. This study demonstrates that Terbinafine-loaded SLNs in a topical gel formulation provide a promising approach for sustained drug delivery in treating fungal infections.

Systemic absorption and safety of topical terbinafine hydrochloride 10% solution (MOB015B): a phase 1 maximal usage trial in patients with moderate-to-severe onychomycosis.

This study is registered with ClinicalTrials.gov as NCT03244280.

Comparison of permeability of topical Cream drug through polymer synthetic membranes of different structures using Franz Cell diffusion test

In this study, in-vitro release experiments were performed using a Franz Diffusion Cell system for Terbinafine Hydrochloride, which is used in the treatment of various fungal infections in the skin caused by many susceptible dermatophytes. In order to evaluate TH transdermally, it was aimed to compare the permeability between polymeric membranes synthesized with polyvinyl alcohol and chitosan mixtures and commercial membranes. In the transdermal drug delivery system calculations, the Fick Diffusion Law was modified and the obtained data were compared. The study was evaluated according to the USP <1724> topical drug products in semisolid form - performance tests. A new high-performance liquid chromatography method was validated for the assay of TH released into the receptor medium in accordance with the ICH guideline. According to the results obtained during the validation process, the limit of detection value was calculated as 0.005 µg/mL and the limit of quantification value was 0.013 µg/mL. Since polymer-based synthetic membranes provide permeability according to molecular size, properties and the ideal environment for measuring and analyzing the diffusion rate of a compound, in experiments conducted using membranes of different structures, the permeability profiles of selected polymer synthetic membranes were statistically evaluated. It has been noted that the hydroxyl groups in PVA and the hydrophilic CS-g-PNDMAAm graft copolymer act at varying rates to enhance or reduce the permeability across the membrane by promoting its diffusion. NaY zeolite has been shown to function as an adsorbent against the medication, lessening the impact of hydrophilic PVA without supplying permeability.

Genetic diversity and antifungal susceptibilities of environmental Cryptococcus neoformans and Cryptococcus gattii species complexes

Cryptococcosis is an opportunistic systemic mycosis caused by Cryptococcus neoformans and C. gattii species complexes and is of increasing global importance. Maintaining continued surveillance of the antifungal susceptibility of environmental C. neoformans and C. gattii isolates is desirable for better managing cryptococcosis by identifying resistant isolates and revealing the emergence of intrinsically resistant species. Relevant research data from Egypt are scarce. Thus, this study aimed to report the genetic diversity of C. neoformans and C. gattii species complexes originating from different environmental sources in Egypt, antifungal susceptibility profiles, antifungal combinations, and correlations of susceptibility with genotypes. A total of 400 environmental samples were collected, 220 from birds and 180 from trees. Cryptococcus spp. were found in 58 (14.5%) of the samples, 44 (75.9%) of the isolates were recovered from birds and 14 (24.1%) from trees. These isolates were genotyped using M13 polymerase chain reaction-fingerprinting and URA5 gene restriction fragment length polymorphism analysis. Of the 31 C. neoformans isolates, 24 (77.4%), 6 (19.4%) and one (4.4%) belonged to VNI, VNII, and VNIII genotypes, respectively. The 27 C. gattii isolates belonged to VGI (70.4%), VGII (18.5%), and VGIII (11.1%) genotypes. Non-wild type C. neoformans and C. gattii isolates that may have acquired resistance to azoles, amphotericin B (AMB), and terbinafine (TRB) were observed. C. gattii VGIII was less susceptible to fluconazole (FCZ) and itraconazole (ITZ) than VGI and VGII. C. neoformans isolates showed higher minimum inhibitory concentrations (MICs) to FCZ, ITZ, and voriconazole (VRZ) than those of C. gattii VGI and VGII. Significant (P < 0.001) correlations were found between the MICs of VRZ and ITZ (r = 0.64) in both C. neoformans and C. gattii isolates, FCZ and TRB in C. neoformans isolates, and FCZ and TRB (r = 0.52) in C. gattii isolates.There is no significant differences in the MICs of TRB in combination with FCZ (P = 0.064) or in combination with AMB (P = 0.543) and that of TRB alone against C. gattii genotypes. By calculating the fractional inhibitory concentration (FIC) index, the combination of FCZ + AMB was synergistic against all tested genotypes. These findings expand our knowledge of ecological niches, genetic diversity, and resistance traits of C. neoformans and C. gattii genotypes in Egypt. Further investigations into how they are related to clinical isolates in the region are warranted.

In vitro effects of N-acetylcysteine in combination with antifungal agents against Malassezia pachydermatis isolated from canine otitis externa.

Many clinicians prescribe antifungal agents to treat canine otitis externa (OE). However, studies evaluating the antifungal effects of N-acetylcysteine (NAC) and its combinations are limited. The aim of this study was to evaluate the antifungal effects of NAC alone and in combination with other antifungal agents against Malassezia pachydermatis isolated from canine OE. M. pachydermatis samples were collected from 13 dogs with OE. The final concentration of the inoculum suspensions of M. pachydermatis was 1-5×106 colony forming units/mL. The concentrations of the test compounds ketoconazole (KTZ), terbinafine (TER), nystatin (NYS) and NAC were 0.02-300µg/mL, 0.04-80µg/mL, 0.16-40µg/mL and 1.25-20mg/mL, respectively. The minimum inhibitory concentration (MIC) was measured to evaluate the susceptibility of the M. pachydermatis to KTZ, TER, NYS and NAC. The checkerboard testing method and fractional inhibitory concentration index were used to evaluate the effect of NAC in combination with KTZ, TER and NYS against M. pachydermatis. The MIC90 values of M. pachydermatis were 4.6875-9.375µg/mL, 1.25µg/mL, 5-10µg/mL and 10mg/mL for KTZ, TER, NYS and NAC, respectively. The synergistic effects of KTZ, TER and NYS with NAC were identified in 0/13, 2/13 and 0/13 isolates, respectively. NAC had an antifungal effect against M. pachydermatis but did not exert synergistic effects when used with KTZ, TER and NYS. Thus, the use of NAC alone as a topical solution could be considered an effective treatment option for canine OE involving M. pachydermatis.

SIMPLE AND SENSITIVE SPECTROPHOTOMETRIC ASSAYS FOR THE DETERMINATION OF TERBINAFINE HCL ANTIFUNGAL DRUG IN PHARMACEUTICALS

Objective: Two highly sensitive, accurate, inexpensive, and simple spectrophotometric assays were developed and validated for the determination of an anti-fungal drug, Terbinafine HCl (TBH), in pure drug and tablets using potassium permanganate (PP) and disodium 2-(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)quinoline-6,8-disulfonate (DSOQ). Material and Method: In the present study, Sebifin and Terbiforce 250 mg tablets were used as pharmaceuticals, potassium permanganate KMnO4 and disodium 2-(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)quinoline-6,8-disulfonate in water were used as reagents, and DR 3900 spectrophotometer equipped with 1cm matched quartz cells was used for absorbance measurements. Result and Discussion: The amount of terbinafine hydrochloride reacting with permanganate and disodium 2-(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)quinoline-6,8-disulfonate in an acidic medium has been determined. The colored reaction products in both cases were measured at the maximum absorptions of 540 nm and 440 nm, respectively. The absorbance measured in each assay as a function of TBH concentration was related to TBH concentrations. Different experimental and variable conditions of assays were done carefully, accurately studied, and optimized. The validation of two assays also was done by following the current guidelines of the International Conference on Harmonization (ICH). Beer’s law for the two methods is obeyed over the concentration ranges 1-15 µg/ml (Correlation coefficient = 0.9983) and 1-18 µg/ml (Correlation coefficient = 0.9989) for methods PP and DSOQ, respectively. Molar absorptivity, limits of detection, and quantification (LOD &amp;amp; LOQ) values were (1.38×104 l/ mol cm, 0.92 &amp;amp; 2.78 µg/ml) for PP assay, and (1.73×104 l/ mol cm, 0.09 &amp;amp; 0.27 µg/ml) for DSOQ assay, respectively. The two assays were successfully applied for the determination of TBH in commercial tablets with reliable and satisfactory results, and hence the proposed assays can be applied in pharmaceutical laboratories of quality control.

The Preparation and Evaluation of a Hydrochloride Hydrogel Patch with an Iontophoresis-Assisted Release of Terbinafine for Transdermal Delivery.

Background: Terbinafine hydrochloride (TEB) is a broad-spectrum antifungal medication commonly used to treat fungal infections of the skin. This study designed a hydrogel patch assisted by an iontophoresis system to enhance the transdermal permeability of TEB, enabling deeper penetration into the skin layers. Methods: The influences of current intensity, pH levels, and drug concentration on the TEB hydrogel patch's permeability were explored using an adaptive ion electroosmosis system. The pharmacokinetic profile, facilitated by iontophoresis for transdermal permeation, was analyzed through the application of microdialysis technology. Scanning electron microscopy and transmission electron microscopy were employed to assess the impact of ion electroosmotic systems on skin integrity. Results: The cumulative drug accumulation within 8 h of the TEB hydrogel patches, assisted by iontophoresis, was 2.9 and 7.9 times higher than without iontophoresis assistance and TEB cream in the control group, respectively. TEB hydrogel patches assisted by iontophoresis can significantly increase the permeability of TEB, and the AUC(0-8 h) was 3.4 and 5.4 times higher, while the Cmax was 4.2 and 7.3 times higher than the TEB hydrogel patches without iontophoresis, respectively. This system has no significant impact on deep-layer cells. Conclusions: This system may offer a safe and effective clinical strategy for the local treatment of deep antifungal infections.

A Derivative Spectrophotometric Method for the Vierordt’s Detection of Terbinafine and Itraconazole in Topical Dosage Form

The goal of the current work was to simultaneously estimate the dosage forms of pharmaceutical topical dosage form and bulk itraconazole and terbinafine HCl by developing and validating a novel and straight forward UV spectrophotometric approach. As of right now, no reports of this medication combination for simultaneous UV spectrophotometric analysis exist. Acetonitrile was utilized as a solvent in the UV Shimadzu 1800 model, which was employed to test the developed approach. For Terbinafine HCl, the wavelength at which the λmax was measured was 235 nm, while for itraconazole, it was 263 nm. It was discovered that the percent RSD of both the system and technique precision for itraconazole and terbinafine HCl was less than 2%. In summary, a new and straightforward UV spectrophotometric technique was created and verified for the simultaneous measurement of terbinafine HCl and itraconazole in pharmaceutical topical dosage form and bulk dose forms. The created approach was determined to be precise, accurate, linear, and stable because the results were found to be within the given range. KEYWORDS Itraconazole, Terbinafine HCl, UV spectrophotometric, Validation, Simultaneous estimation method, vierordt’s method

High Prevalence of Terbinafine Resistance Among Trichophyton mentagrophytes/T. interdigitale Species Complex, a Cross-Sectional Study from 2021 to 2022 in Northern Parts of Iran.

Treatment-resistant dermatophytosis caused by the members of the Trichophyton mentagrophytes/Trichophyton interdigitale species group (TMTISG) is increasing worldwide. We aimed to determine the prevalence of TMTISG in patients with dermatophytosis in two centers from north of Iran and detect the possible mutations in the squalene epoxidase (SQLE) gene in relevant terbinafine (TRB) resistant pathogenic isolates. From November 2021 to December 2022, 1960 patients suspected to dermatophytosis and referred to two mycology referral laboratories in the north of Iran were included in the study. Identification of all dermatophyte isolates was confirmed by RFLP of rDNA internal transcribed spacer (ITS) regions. Antifungal susceptibility testing against five common antifungals using the CLSI-M38-A3 protocol was performed. The TMTISG isolates resistant to TRB, were further analyzed to determine the possible mutations in the SQLE gene. Totally, 647 cases (33%) were positive for dermatophytosis of which 280 cases (43.3%) were identified as members of TMTISG. These were more frequently isolated from tinea corporis 131 (44.56%) and tinea cruris 116 (39.46%). Of 280 TMTISG isolates, 40 (14.3%) were resistant to TRB (MIC ≥ 4µg/mL), all found to be T. indotineae in ITS sequencing. In SQLE sequencing 34 (85%) of TRB-resistant isolates had coincident mutations of Phe397Leu and Ala448Thr whereas four and two isolates had single mutations of Phe397Leu and Leu393Ser, respectively. Overall, the resistance of Iranian TMTISG isolates to TRB greatly occurred by a mutation of Phe397Leu in the SQLE gene as alone or in combination with Ala448Thr. Nevertheless, for the occurrence of in vitro resistance, only the presence of Phe397Leu mutation seems to be decisive.

A phase III randomized controlled clinical trial evaluating the efficacy and safety of naftifine 2% cream versus terbinafine 1% cream in patients with superficial fungal infection of the skin

Background: Dermatophytosis is the prevailing fungal infection, typically addressed through topical, systemic antifungal medications, or a combination of both. Naftifine hydrochloride, belonging to the allylamine group, is a topical antifungal, exhibiting fungicidal properties alongside antibacterial and anti-inflammatory effects. This study evaluated the efficacy and safety of naftifine hydrochloride 2% w/w in 268 patients with dermatophytosis versus terbinafine hydrochloride 1% w/w. Methods: The drugs were applied daily for two weeks, with the primary endpoint being a clinical cure at the end of the treatment. Secondary endpoints included mycological cure, composite cure, global efficacy assessment, and post-treatment relapse. Results: In both groups, most patients experienced both clinical and mycological cures, with composite cures observed in 94.07% of the test group and 87.97% of the reference group. The global assessment of efficacy was 3.59 in the test group and 3.48 in the reference group, showing no notable difference between the two groups. All adverse events in both groups were mild and resolved within four days. Overall tolerability was comparable between the study groups. Conclusions: The study concluded that topical naftifine was effective and safe in patients with dermatophytosis and its efficacy and safety were found comparable to topical terbinafine.

Clinico-mycological study of onychomycosis and in vitro antifungal susceptibility of Trichophyton rubrum.

Onychomycosis, a fungal nail infection, is primarily caused by dermatophytes, yeasts, and non-dermatophyte moulds (NDMs). The incidence of this disease and the predominance of specific pathogens vary across different regions and evolve. This study aimed to elucidate the epidemiology of onychomycosis and the pattern of causative pathogens in Beijing, and to ascertain the in vitro antifungal susceptibility profiles of Trichophyton rubrum against itraconazole (ITR), terbinafine (TER), and fluconazole (FLU). Involving 245 patients of onychomycosis with positive fungal culture results, the study implemented internal transcribed spacer (ITS) sequencing of ribosomal DNA (rDNA) on all collected samples. The mean age of the participants was 37.93 ± 13.73 years, with a male-to-female ratio of 1.53:1. The prevalence of toenail infections was significantly higher than that of fingernails. Distal and lateral subungual onychomycosis (DLSO) were the most frequent clinical classifications. PCR results indicated that dermatophytes were the most prevalent pathogens, followed by yeasts and NDMs, among which T. rubrum was the most dominant dermatophyte. TER demonstrated high sensitivity to T. rubrum. However, in clinical settings, some patients with onychomycosis exhibit a poor response to TER treatment. The relationship between in vitro antifungal sensitivity and clinical effectiveness is complex, and understanding the link between in vitro MIC values and clinical efficacy requires further investigation.

QbD Approach to Method Development, Validation and Degradation Profiling of Antifungal Drugs by RP-HPLC

For the simultaneous estimation of Itraconazole (ITZ) and Terbinafine hydrochloride (TBF HCl) in tablet dosage form, a simple, novel, cost effective and rapid RP-HPLC method was developed. Method development becomes quick, accurate, sensitive, and robust by using quality by design (QbD). RP-HPLC was performed using a C18 (agilent, 4.6 x 250mm, 5µm particle size) column. Methanol and 0.05% OPA (pH 3.5) was used as mobile phase in 84:16 ratio. The analysis was conducted in gradient mode with a flow rate of 0.95mL/min. Detection wavelength was set at 270nm. Retention time for TBF and ITZ was at 2.93 and 6.96min, respectively. The accuracy, precision, repeatability, linearity, LOD, LOQ and robustness parameters have been validated as per the ICH Q2 (R1) guideline: Validation of analytical procedures–text and methodology. Values for LOD and LOQ were found to be 0.131 and 0.398µg/mL and 0.350 and 1.061µg/mL respectively for ITZ and TBF HCl. Thus, the technique can be employed for regular QC analysis of bulk ITZ and TBF HCl and their pharmaceutical formulations. Degradative stress conditions like acid, base, neutral, oxidation applied and degradations were studied.

Design and Evaluate Terbinafine Hydrochloride Loaded gel by using Modified Tamarind for Topical Drug Delivery

The principal objective of this study is to make and survey the properties of Gel containing terbinafine hydrochloride (TH) stacked niosomal gel by functionalized tamarind involving that might work as effective antifungal medication conveyance frameworks (DDS) for the helpful treatment of contagious contaminations by postponing the prescription delivery. Utilizing a characteristic direct functionalized polymer and the ethanol infusion strategy, niosomal gel was made (thionatinated and sulphonated tamarind). TH stacked niosomal scattering of size going from 100 to 627nm and percent ensnarement effectiveness of 63 to 87% were acquired. Both the factors for example length 60 and cholesterol impact the molecule size and EE (%). In-vitro discharge concentrates on completed in PBS (pH 5.5) for N4 and showcased cream displayed an arrival of 82.72% and 74.92% separately more than 24hr. The details of the Nanosponges were assessed for their rates of creation yield (PY), entanglement effectiveness (EE), and medication stacking (%DL). FTIR, DSC and PXRD studies uncovered that the greater part of the medication was scattered all through the niosomes. DSC and XRD concentrates on additionally shown that medication was in undefined state in the N4 cluster while unadulterated TH was in translucent state. FESEM, TEM and AFM pictures showed that niosomes had round shape with smooth surface. CLSM picture demonstrated the smooth and bilayer design of niosomes. 1%w/v TH (0.1%) stacked niosomal Sulphonated and thionated tamarindgel were ready and portrayed for consistency studies. The consistency of fake treatment Sulphonated and thionated tamarind and TH stacked niosomal gels with both were viewed as 20,500cps, 43,000cps, 10,300cps and 34,600cps respectively. It was apparent from the pH and spreadability boundaries that the fake treatment and TH stacked niosomal gels are viable for skin delivery.In-vitro discharge concentrates on did in PBS (pH 5.5) for THNTT gel, THNST gel and showcased cream wereshowed 74.92±0.98 %,99.07±1.03% and 101.02±0.87% discharge toward the finish of 24 hr respectively.Amount of medication held in skin after 24 hr was 47.68 for THNTT gel while for promoted gel, it was viewed as 27.67 showing THNTT has great skin maintenance properties than advertised cream (Texifen).CLSM investigation of Wistar rodent skin uncovered that niosomes were circulated all through skin with high fluorescence power which ready to help ex vivo skin penetration and maintenance result.No indications of disturbance were seen upon the utilization of fake treatment gel, N4 niosomal scattering, THNTT gel, and advertised cream of TH to the Wistar rodents skin ,affirming that pre-arranged N4 niosomal scattering as well as THNTT gel are liberated from irritation. In vitro antifungal movement study for THNTT gel and showcased cream were performed for both Aspergillusniger (ATCC 10578) and Candida albicans (CA14, clinical confine) and results showed that N4 gel would be advised to antifungal action in contrast with promoted cream.In vivo pharmacodynamic concentrates on showed that THNTT gel lessens parasitic weight or count more actually than advertised cream.

A Novel Potentiometric Coated Wire Sensor Based on Functionalized Polymeric CaO/ZnO Nanocomposite Synthesized by Lavandula Spica Mediated Extract for Terbinafine Determination

AbstractThe unique properties of calcium oxide (CaO) and zinc oxide (ZnO) at the nanoscale have attracted the interest of scientists as promising electrically conductive substances for sensing purposes. The content of terbinafine hydrochloride (TRF) in pharmaceutical tablets was determined using a novel coated, wire‐functionalized CaO/ZnO nanocomposite membrane sensor biogenically produced from Lavandula spica extract. Sodium tetraphenylborate was used to prepare the active material (TRF‐TBP). The newly modified sensor gave excellent potentiometric sensitivity with the least squares regression equation EmV=(−58.88X±0.3)+log [TRF]+549.78 and covered a wide linear range (5.0×10−9–1.0×10−2 mol/L) of TRF samples. In contrast, the standard TRF‐TBP sensor wasn't as sensitive when (2.5×10−6–1.0×10−2 mol/L). TRF solutions with regression equation of (−55.728X±0.7)+log [TRF]+396.64. The appropriate pH range was 3–6. The principles of analytical methodology were applied to investigate the validity and suitability of the proposed technique. The proposed sensors were found to be suitable and efficient for the detection of TRF on tablets.

Potentiometric determination of terbinafine hydrochloride antifungal drug in pharmaceutical and biological fluids using ion selective electrodes

Potentiometric determination of terbinafine hydrochloride antifungal drug in pharmaceutical and biological fluids using ion selective electrodes

Formulation And Evolution Of Microemulgel Contain Terbinafine Hcl

Aim of this experiment is to prepare miroemulgel containing terbinafine hcl API and it evaluation tests. API is terbinafine hcl and other polymers like tween 20, span80 surfactants are used and other liquid paraffin, water used. This study shows that microemulgel prepared and good release study both batches show good results. In this all oil and surfaces are mix in carpool base and prepare gel good gel appearance form. The Microemulgel for skin conditions &amp; Cosmetic use have different desirable properties such as good appearance, being thixotropic ratio, easily spreadable, Non-staining, and emollient, without form any harm, clear, transparent &amp; elegant appearance, &amp; these Microemulgel based formulations increase the skin deposition of API, thereby ultimately enhancing its therapeutic activity. Terbinafine is a broad-spectrum anti-antifungal medication.

Antifungal activity of azoles, allylamines, and 8-hidroxiquinolines, alone and in combination, against Malassezia pachydermatis in vitro and in vivo

Malassezia pachydermatis is often reported as the causative agent of dermatitis in dogs. This study aims to evaluate the in vitro and in vivo antifungal activity of azoles and terbinafine (TRB), alone and in combination with the 8-hydroxyquinoline derivatives (8-HQs) clioquinol (CQL), 8-hydroxyquinoline-5-(n-4-chlorophenyl)sulfonamide (PH151), and 8-hydroxyquinoline-5-(n-4-methoxyphenyl)sulfonamide (PH153), against 16 M. pachydermatis isolates. Susceptibility to the drugs was evaluated by in vitro broth microdilution and time-kill assays. The Toll-deficient Drosophila melanogaster fly model was used to assess the efficacy of drugs in vivo. In vitro tests showed that ketoconazole (KTZ) was the most active drug, followed by TRB and CQL. The combinations itraconazole (ITZ)+CQL and ITZ+PH151 resulted in the highest percentages of synergism and none of the combinations resulted in antagonism. TRB showed the highest survival rates after seven days of treatment of the flies, followed by CQL and ITZ, whereas the evaluation of fungal burden of dead flies showed a greater fungicidal effect of azoles when compared to the other drugs. Here we showed for the first time that CQL is effective against M. pachydermatis and potentially interesting for the treatment of malasseziosis.

Development and in vitro characterization of the proliposome gel of terbinafine hydrochloride

The study was conducted to prepare the Proliposome Gel of Terbinafine Hydrochloride to improve the drug loading and to sustain the drug release of terbinafine hydrochloride. Proliposome gel of terbinafine hydrochloride were prepared by modified coacervation phase separation method by varying the concentrations of PC to cholesterol. The prepared proliposome gel was evaluated for its pH, viscosity, drug loading, and In vitro drug release studies. The appearance, particle size and drug entrapment of each produced formulation was also evaluated. All proliposome gel formulation made were consistent, homogenous, and white creamy gel.