Nail Lacquer Formulation Research Articles

Nail Lacquer Containing Origanum vulgare and Rosmarinus officinalis Essential Oils and Biogenic Silver Nanoparticles for Onychomycosis: Development, Characterization, and Evaluation of Antifungal Efficacy.

Onychomycosis is a common fungal nail infection for which new antifungals are needed to overcome antimicrobial resistance and the limitations of conventional treatments. This study reports the development of antifungal nail lacquers containing oregano essential oil (OEO), rosemary essential oil (REO), and biogenic silver nanoparticles (bioAgNPs). The formulations (F) were tested against dermatophytes using agar diffusion, ex vivo nail infection, and scanning electron microscopy techniques. They were evaluated for their pharmacotechnical characteristics and by FTIR-PAS to assess permeation across the nail. F-OEO and F-OEO/bioAgNPs were promising candidates for the final nail lacquer formulation, as they permeated through the nail and showed antifungal efficacy against dermatophytes-contaminated nails after 5 days of treatment. Treated nails exhibited decreased hyphae and spores compared to the untreated control; the hyphae were atypically flattened, indicating loss of cytoplasmic content due to damage to the cytoplasmic membrane. The formulations were stable after centrifugation and thermal stress, maintaining organoleptic and physicochemical characteristics. Both F-OEO and F-OEO/bioAgNPs had pH compatible with the nail and drying times (59-90 s) within the reference for nail lacquer. For the first time, OEO and bioAgNPs were incorporated into nail lacquer, resulting in a natural and nanotechnological product for onychomycosis that could combat microbial resistance.

Development and Evaluation of Luliconazole Nail Lacquer Containing Potential Permeation Enhancers for an Enhanced Transungual Drug Delivery

Background: Topical therapy for nail infection has a serious drawback of drug permea-tion via keratinized human nail plate. Onychomycosis, or tinea unguium, is a human nail fungal infection affecting nearly 19% of the world’s population. Aim: Purposely, we aimed to develop and evaluate nail lacquer formulations incorporated with lu-liconazole utilizing different permeation enhancers for targeted transungual drug delivery. Nail clippings were treated with luliconazole solution (5% w/v) with or without permeation enhancers and screened by determining the hydration enhancement factor and retention of the drug in the nail clippings. Different batches of nail lacquer formulations were prepared to employ Eudragit, poly-ethylene glycol 400, Tween 80, and permeation enhancer with the highest hydration enhancement factor value. Methods: Successively, the formulations were evaluated for studies like compatibility, application, gloss, blush, smoothness of flow, adhesion, non-volatile content, etc. Based on the results of physi-cal characterization and in vitro release study, formulations based on Eudragit RLPO and RSPO containing N-acetylcysteine and urea and the Eudragit RL100 containing urea as penetration en-hancer were found to be potentially useful. Furthermore, a comparative ex vivo evaluation of the formulations for permeation across the nail clippings revealed that the luliconazole-loaded Eudragit RLPO formulations containing N-acetylcysteine and urea provided the highest flux (5.12 μg/cm2/min) and shortest lag time (17.4 min). Results: Morphological analysis showed an increase in the number of pores on the nail surface, leading to the enhancement of drug diffusion across the nail matrix and nail bed. Conclusion: Furthermore, the luliconazole nail lacquer formulation exhibited higher antifungal ac-tivity, viscosity, and stability properties. Hence, the results suggest that the developed luliconazole nail lacquer formulation is an efficient topical transungual drug delivery system.

Formulation and Evaluation of Nail Drug Delivery System of Anti Fungal Drug

The purpose of this study was to prepare nail lacquer for nail drug delivery system of anti fungal drug in order to improve the physicochemical parameters that influence the drug permeation through a nail plate to reach the systemic circulation and the neighbouring target sites. The success of local topical therapy for onychomycosis depends on the achievement of effective chemical concentrations into/through the human nail plate; therefore, a suitable antifungal drug must be coupled with an appropriate delivery method. The method should maximize the effect of the active principle by aiding its diffusion into the nail bed to levels exceeding the minimum inhibitory concentration (MIC) against local infection by dermatophytes. Thus, a suitable carrier may be needed to enhance drug penetration through the nail barrier.
 The nail lacquer formulations were prepared by simple mixing method and analyzed for non volatile content, gloss, smoothness to flow, drug diffusion studies, and % drug content. Among all formulations, nail lacquer prepared with 2% oxiconazole, 6% nitrocellulose, 1% ethyl cellulose, 15% salicylic acid, 10% propylene glycol and 10% 2-H β-CD exhibited good non volatile content, drug release, drug content estimation and zone inhibition i.e. F4 formulation. The drug release profiles were achieved 93.2% at 12 h. The in vitro ungual permeation studies revealed a good in vitro in vivo correlation. Nail lacquer were substantially stable after 1 month storage at 40±2℃.

Preparation and Evaluation of Nail Lacquer containing Luliconazole as Ungual Drug Delivery System

Background: The primary goal of developing the antifungal nail lacquer is to determine its suitability for delivering medicine to the desired location. Because the area between the nail and the skin is commonly impacted, topical treatment is difficult to reach. Statistical techniques were used in this study to understand the source of variables.
 Methods: Nail lacquer formulations were prepared using luliconazole using a simple mixing method. The drug's permeability was made better by using the permeation enhancers in different amounts.
 Results: The drug-excipient study revealed no physical or chemical interaction, while the standard calibration curve showed that the drug follows Beers-Lamberts' law with a coefficient value of 0.984. The medicated nail lacquer was evaluated for various parameters such as non-volatile content, which was in the range of 37.020.72-43.050.57%, drying time was found to be in the range of 42-97 seconds, water resistance was found to be 0.10-0.24gm, the drug content in the prepared nail paint was found to be in the range of 94.331.52-98.33.51%, and the drug release study revealed the drug release in the range of 0.70.1-51.580.28%, which shows satisfactory results. The antifungal study revealed a zone of inhibition for the prepared nail paint of 47 mm, which was the highest among all the formulations and also the highest among the studies conducted with pure drug and control formulation. The stability study revealed that the optimised formulation, i.e., F2, was stable during the time span of the study, and hence it was concluded that the prepared formulation was stable.
 Conclusion: From the results above, it can be concluded that nail lacquer containing luliconazole could be a promising drug delivery system for treating fungal nail infections.

Application of central composite design for the optimization of itraconazole loaded nail lacquer formulation.

Onychomycosis is a common fungal infection of the nails that mostly affects the elderly and athletes. Antifungal drug-like itraconazole is one of the therapeutic agents of choice for the topical treatment of onychomycosis. The current work aimed for the preparation and optimization of itraconazole-loaded nail lacquer formulation. Central composite design was employed; independent variables were polymer concentration (X1) and thioglycolic acid (TGA) concentration (X2). While the dependent variables were cumulative amount of drug permeated per unit area (CADP/A, Y1), drying time (Y2) and nonvolatile content (Y3). The optimized formulation was characterized for various parameters including ex-vivo permeation study, confocal laser scanning microscopy (CLSM) and antifungal study. The optimized nail lacquer formulation (F7) exhibited CADP/A of 198.23µg/cm2, drying time of 185s and nonvolatile content of 97.23%. The scanning electron microscopy of goat hoof treated with optimized nail lacquer formulation demonstrated loosening of the structure and marked increase in surface roughness. The CLSM micrograph of goat hoof treated with optimized nail lacquer formulation demonstrated that the probe dye was eventually distributed and penetrated through the hoof. Bio-adhesiveness analysis showed that the prepared nail lacquer film has ample adhesiveness to be maintained on the nail plate surface for a sufficient time. In antifungal study, the optimized nail lacquer, and marketed gel exhibited a zone inhibition of 21mm, and 10mm against Candida albicans, respectively. The stability study showed that the optimized nail lacquer is stable at storage condition. The prepared nail lacquers have been shown to serve as a useful dosage form for the delivery of itraconazole across nail plate for controlling the problems associated with onychomycosis.

The rheologically-complex fluid beauty of nail lacquer formulations.

Nail lacquer formulations are multi-ingredient complex fluids with additives that affect color, smell, texture, evaporation rate, viscosity, stability, leveling behavior, consumer's sensory experience, and dried coating's decorative and wear performance. Optimizing and characterizing the formulation rheology is critical for achieving longer shelf-life, better control over the nail painting process and adhesion, continuous manufacturing of large product volumes, and increasing overall consumer satisfaction. Dispensing, bottle filling, brush application, and dripping, as well as perceived tackiness of nail polishes, all involve capillarity-driven pinching flows associated with strong extensional deformation fields. However, a significant lack of characterization of pinching dynamics and extensional rheology response of multicomponent formulations, especially particle suspensions in viscoelastic solutions, motivates this study. Here, we characterize the shear rheology response of twelve commercial nail lacquer formulations using torsional rheometry and characterize pinching dynamics and extensional rheology response using dripping-onto-substrate (DoS) rheometry protocols we developed. We visualize and analyze brush loading, nail coating, dripping from brush, sagging, and lacquer application on a nail to outline the challenges posed by free-surface flows and non-Newtonian rheology. We find that the radius evolution over time obtained using DoS rheometry displays power law exponents distinct from those exhibited in shear thinning. Both shear and extensional viscosity decrease with deformation rate. However, the extensional viscosity appears to be rate-independent at the highest rates and displays nearly an order of magnitude larger values than the high shear rate viscosity. We envision that the findings and protocols described here will help and motivate industrial scientists to design better multicomponent formulations through a better characterization and understanding of the influence of ingredients like particles and polymers on rheology, processing, and applications.

Efinaconazole nail lacquer for the transungual drug delivery: Formulation, optimization, characterization and in vitro evaluation

AimThe objective of the present study was to develop a nail lacquer of Efinaconazole for the onychomycosis treatment. Materials and methodsHydration enhancement study was carried out for initial screening of penetration enhancers and enhancers with highest hydration enhancement factor value was further evaluated to select the enhancer to be incorporated in the Nail lacquer formulation. 32 full factorial design with different solvent and polymer ratio was employed to optimize the nail lacquer formulation. Optimized formulation was selected on the basis of drying time, flux and viscosity which was further evaluated for non-volatile content, water resistance, film adhesion, blush test, scanning electron microscopy analysis and Fourier transform infrared spectroscopy. Results2-mercaptoethanol, N-acetyl-l-cysteine and thioglycolic acid showed highest hydration enhancement factor value and 2-mercaptoethanol was selected for incorporation in nail lacquer formulation as it showed better penetration in comparison to other enhancers. Optimized formulation comprised of 70:30 solvent ratio and 50:50 polymer ratio. The formulation was able to achieve flux of 181.98 ± 3.19 μg/cm2/h in comparison to 52.88 ± 3.11 μg/cm2/h of the marketed preparation. The promising potential of the nail lacquer was proven by scanning electron microscopy analysis. ConclusionFor the efficient transungual delivery of Efinaconazole, promising and durable nail lacquer was formulated which ensured drug is delivered to the nail bed and effective onychomycosis treatment is achieved.

Polyurethanes as New Excipients in Nail Therapeutics.

Onychomycosis affects about 15% of the population. This disease causes physical and psychosocial discomfort to infected patients. Topical treatment (creams, solutions, gels, colloidal carriers, and nail lacquers) is usually the most commonly required due to the high toxicity of oral drugs. Currently, the most common topical formulations (creams and lotions) present a low drug delivery to the nail infection. Nail lacquers appear to increase drug delivery and simultaneously improve the effectiveness of treatment with increased patient compliance. These formulations leave a polymer film on the nail plate after solvent evaporation. The duration of the film residence in the nail constitutes an important property of nail lacquer formulation. In this study, a polyurethane polymer was used to delivery antifungals drugs, such as terbinafine hydrochloride (TH) and ciclopirox olamine (CPX) and the influence of its concentration on the properties of nail lacquer formulations was assessed. The nail lacquer containing the lowest polymer concentration (10%) was the most effective regarding the in vitro release, permeation, and antifungal activity. It has also been demonstrated that the application of PU-based nail lacquer improves the nail plate, making it smooth and uniform and reduces the porosity contributing to the greater effectiveness of these vehicles. To conclude, the use of polyurethane in nail formulations is promising for nail therapeutics.

Terbinafine hydrochloride nail lacquer for the management of onychomycosis: formulation, characterization and in vitro evaluation.

The present investigation's intention was to develop an optimized nail lacquer (NL) for the management of onychomycosis. The NL was optimized statistically adopting 32 full factorial design having different polymer ratios and solvent ratios. The formulations were assessed for drug permeation drying time and peak adhesive strength of the film. Characterization was done using techniques including attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), x-ray diffraction (XRD), etc. The formulation that had 1:1 polymer ratio and 80:20 solvent ratio was chosen as the optimized formulation. In vitro permeation studies showed better penetration (∼3.25-fold) as well as retention (∼11-fold) of the optimized NL formulation in the animal hoof as compared with the commercial formulation. The findings of in vitro and ex vivo studies elucidated the potential of the optimized formulation. [Formula: see text].

In-situ gels and nail lacquers as potential delivery systems for treatment of onychomycosis. A comparative study

The aim of this study was to prepare and incorporate TBH-loaded spanlastics into different delivery systems for treatment of onychomycosis via the trans-ungual route. Two drug delivery dosage forms; the in-situ gel and the nail lacquer, were developed and evaluated for their ability to deliver TBH encapsulated in spanlastic carriers to the nail plate. In-situ gel formulations were prepared using different Pluronics® in different concentrations using the cold method, and evaluated for sol-gel transition temperature, viscosity, and in-vitro release studies. The nail lacquer formulation were prepared using Eudragit® RLPO as a film forming polymer in different concentrations, and evaluated for drying time, non-volatile content, water resistance and in-vitro release studies. Finally, an ex vivo human cadaver nail permeation study with the optimized formulations was employed in order to assess TBH permeation and retention in the nails compared to the commercially available TBH cream (Lamisil® 1% cream). The optimized in-situ gel formulation G6, showed higher amounts of retained TBH in the nails (2.05 ± 0.008 mg/cm2) compared to the marketed product Lamisil® cream 1% (1.36 ± 0.03 mg/cm2), by an increase of 51%, indicating successful trans-ungual delivery of TBH from the prepared in-situ gels.

Enhanced Ungual Permeation of Terbinafine HCl Delivered Through Liposome-Loaded Nail Lacquer Formulation Optimized by QbD Approach.

The present investigation focused on developing, optimizing, and evaluating a novel liposome-loaded nail lacquer formulation for increasing the transungual permeation flux of terbinafine HCl for efficient treatment of onychomycosis. A three-factor, three-level, Box-Behnken design was employed for optimizing process and formulation parameters of liposomal formulation. Liposomes were formulated by thin film hydration technique followed by sonication. Drug to lipid ratio, sonication amplitude, and sonication time were screened as independent variables while particle size, PDI, entrapment efficiency, and zeta potential were selected as quality attributes for liposomal formulation. Multiple regression analysis was employed to construct a second-order quadratic polynomial equation and contour plots. Design space (overlay plot) was generated to optimize a liposomal system, with software-suggested levels of independent variables that could be transformed to desired responses. The optimized liposome formulation was characterized and dispersed in nail lacquer which was further evaluated for different parameters. Results depicted that the optimized terbinafine HCl-loaded liposome formulation exhibited particle size of 182nm, PDI of 0.175, zeta potential of -26.8mV, and entrapment efficiency of 80%. Transungual permeability flux of terbinafine HCl through liposome-dispersed nail lacquer formulation was observed to be significantly higher in comparison to nail lacquer with a permeation enhancer. The developed formulation was also observed to be as efficient as pure drug dispersion in its antifungal activity. Thus, it was concluded that the developed formulation can serve as an efficient tool for enhancing the permeability of terbinafine HCl across human nail plate thereby improving its therapeutic efficiency.

A Novel Apremilast Nail Lacquer Formulation for the Treatment of Nail Psoriasis.

The objective was to prepare a novel nail lacquer formulation to improve the ungual and trans-ungual delivery of apremilast for the potential treatment of nail psoriasis. Nail lacquer formulation was prepared using Eudragit® S 100 as a film-forming polymer and the mixture of ethanol, ethyl acetate, and water as a solvent system. As a result of high-throughput screening studies, dexpanthenol and salicylic acid were found to be the potential penetration enhancers. After 7days of in vitro studies, the cumulative amount of apremilast delivered by the nail lacquer formulation across the nail plate was found to be ~3-fold (0.52±0.07μg/cm2) more compared to control (nail lacquer formulation without enhancers) (0.19±0.02μg/cm2). The cumulative amount of apremilast retained in the nail plate in the case of nail lacquer formulation was 1.26±0.18μg/mg which was found to be ~2-fold more compared to control (0.57±0.07μg/mg). Human subject studies were performed on the nails of thumb and index finger of six volunteers for 15days. As a result, the cumulative amount of apremilast retained in the free distal edge of the nail plate in the case of nail lacquer was found to be ~2-fold (0.93±0.14μg/mg) more related to control (0.41±0.04μg/mg). As a conclusion, nail lacquer formulation was found to be capable of delivering a substantial amount of apremilast into the nail apparatus; thus, it can be a potential option for the treatment of nail psoriasis.

New Polyurethane Nail Lacquers for the Delivery of Terbinafine: Formulation and Antifungal Activity Evaluation

Onychomycosis is a fungal nail infection. The development of new topical antifungal agents for the treatment of onychomycosis has focused on formulation enhancements that optimize the pharmacological characteristics required for its effective treatment. Polyurethanes (PUs) have never been used in therapeutic nail lacquers. The aim of this work has been the development of new PU-based nail lacquers with antifungal activity containing 1.0% (wt/wt) of terbinafine hydrochloride. The biocompatibility, wettability, and the prediction of the free volume in the polymeric matrix were assessed using a human keratinocytes cell line, contact angle, and Positron Annihilation Lifetime Spectroscopy determinations, respectively. The morphology of the films obtained was confirmed by scanning electron microscopy, while the nail lacquers’ bioadhesion to nails was determined by mechanical tests. Viscosity, in vitro release profiles, and antifungal activity were also assessed. This study demonstrated that PU-terbinafine-based nail lacquers have good keratinocyte compatibility, good wettability properties, and adequate free volume. They formed a homogenous film after application, with suitable adhesion to the nail plate. Furthermore, the antifungal test results demonstrated that the terbinafine released from the nail lacquer Formulation A PU 19 showed activity against dermatophytes, namely Trichophyton rubrum.

Effect of Film-Forming Polymers on Release of Naftifine Hydrochloride from Nail Lacquers

The successful topical therapy of onychomycosis depends on effective drug release and penetration into nail, which can be achieved by using an adequately developed delivery system. This study evaluated and compared effect of film-forming polymers Eudragit RL100, Eudragit RS100, and ethyl cellulose on naftifine hydrochloride release from experimental nail lacquer formulations. Quality of formulations was evaluated by determining drying time and water resistance. Interactions between active pharmaceutical ingredient and excipients were investigated using microcalorimetry and FT-IR. Optimization of nail lacquer formulations was performed by naftifine hydrochloride release testing. Release of naftifine hydrochloride increased with increasing concentration of Eudragit RL100. Plasticizer triacetin affected the release of naftifine hydrochloride, when Eudragit RS100 polymer was used. Ethyl cellulose polymer was determined to be not applicable for naftifine hydrochloride nail lacquer formulations. Two compositions of nail lacquers were optimized and could be used in further development of transungual delivery systems.

Development of ciclopirox nail lacquer with enhanced permeation and retention.

Onychomycosis is a prevailing disease caused by fungal infection of nails that mostly affects athletes and the elderly. Ciclopirox is approved by the US Food and Drug Administration for the topical treatment of onychomycosis. However, the desired penetration of ciclopirox into the nail bed has not been achieved via topical application for efficient treatment. Therefore, the main aim of this study was to enhance ciclopirox permeation and retention in nail by the development of a new nail lacquer formulation. We screened the effects of different solvents, alkalizing agents, and permeation enhancers on the permeation of bovine hooves by ciclopirox and its retention in human nail clippings. The results suggest that isopropyl alcohol, potassium hydroxide, and urea as the solvent, alkalizing agent, and permeation enhancer, respectively, improved the permeation of the ciclopirox nail lacquer formulation the most with high flux rates. Comparison of the final formulation and marketed product revealed enhanced retention of ciclopirox from our developed formulation in human nail clippings. Therefore, our newly developed nail lacquer may be a potentially effective formulation for the treatment of onychomycosis in humans.

Hydroxypropyl-β-cyclodextrin: A Novel Transungual Permeation Enhancer for Development of Topical Drug Delivery System for Onychomycosis

The treatment of onychomycosis is a challenging task because of unique barrier properties of the nail plate which hampers the passage of antifungal drugs in a concentration required to eradicate the deeply seated causative fungi in the nail bed. In present investigation, application of hydroxypropyl-β-cyclodextrin (HP-β-CD) was established as an effective and nail friendly transungual drug permeation enhancer especially for poorly water soluble drugs using terbinafine hydrochloride as a poorly soluble drug. HP-β-CD significantly improves hydration of nail plates and increases solubility of terbinafine hydrochloride in the aqueous environment available therein, which leads to uninterrupted drug permeation through water filled pores of hydrogel-like structure of hydrated nail plates. A nail lacquer formulation was designed with an objective to deliver the drug in an effective concentration across nail plates, using HP-β-CD as a permeation enhancer. The formulations containing HP-β-CD showed higher flux than the control formulation in in vitro drug permeation study. The formulation containing 10% w/v of HP-β-CD showed maximum flux of 4.586 ± 0.08 μg/mL/cm2 as compared to the control flux of 0.868 ± 0.06 μg/mL/cm2. This finding supports application of HP-β-CD as an effective permeation enhancer for transungual delivery of terbinafine hydrochloride and possibly other poorly water soluble drugs where HP-β-CD can act as a solubilizer.

Double blind clinical trial of the Ageratina pichinchensis extract in the topical treatment of onychomycosis

Onychomycosis is a high-prevalence infectious disease that is usually treated with drugs administered chronically via the oral pathway, which produce important side effects. Ageratina pichinchensis, used in traditional medicine to treat dermatophytosis, has shown antifungal activity against Thrichophyton rubrum, and T. mentagrophytes. Clinically, a nail lacquer elaborated with the extract obtained from this plant showed similar rates of therapeutic effectiveness than 8% ciclopirox in patients with onichomycosis. OBJECTIVE: Evaluate two different concentrations of the standardized extract of A. pichinchensis in patients with mild to moderate onychomycosis. METHODOLOGY: By means of a randomly and comparative double blind clinical trial, 122 patients of either sex, within 19 and 65 years were included. A toenail sample was taken and submitted to direct microscopic identification before and after treatment. Two experimental groups were organized; group 1 was administered with a cosmetic nail lacquer formulation containing a 12.6% A. pichinchenis extract, while group 2 received an identical product containing 16.8% A. pichinchenis extract. All patients were treated and followed clinically for 6 months by means of monthly appointments. ANOVA and X2 test were employed to identify differences between groups. Values of p<0.05 were considered significant. Results: 103 patients concluded the treatment. The therapeutic effectiveness exhibited by the 12.6% formulation was 67.2% while that of the 16.8% was 79.1%. Regarding clinical evolution analysis of results at the end of the treatment evidenced that the 16.8% concentration possesses higher therapeutic effectiveness (p=0.01).

Double blind clinical trial of the ageratina pichinchensis extract in the topical treatment of onychomycosis

Onychomycosis is a high-prevalence infectious disease that is usually treated with drugs administered chronically via the oral pathway, which produce important side effects. Ageratina pichinchensis, used in traditional medicine to treat dermatophytosis, has shown antifungal activity against Thrichophyton rubrum, and T. mentagrophytes. Clinically, a nail lacquer elaborated with the extract obtained from this plant showed similar rates of therapeutic effectiveness than 8% ciclopirox in patients with onichomycosis. OBJECTIVE: Evaluate two different concentrations of the standardized extract of A. pichinchensis in patients with mild to moderate onychomycosis. METHODOLOGY: By means of a randomly and comparative double blind clinical trial, 122 patients of either sex, within 19 and 65 years were included. A toenail sample was taken and submitted to direct microscopic identification before and after treatment. Two experimental groups were organized; group 1 was administered with a cosmetic nail lacquer formulation containing a 12.6% A. pichinchenis extract, while group 2 received an identical product containing 16.8% A. pichinchenis extract. All patients were treated and followed clinically for 6 months by means of monthly appointments. ANOVA and X2 test were employed to identify differences between groups. Values of p<0.05 were considered significant. Results: 103 patients concluded the treatment. The therapeutic effectiveness exhibited by the 12.6% formulation was 67.2% while that of the 16.8% was 79.1%. Regarding clinical evolution analysis of results at the end of the treatment evidenced that the 16.8% concentration possesses higher therapeutic effectiveness (p=0.01).

Comparative clinical evaluation of efficacy and safety of a formulation containing ciclopirox 8% in the form of a therapeutic nail lacquer in two different posologies for the treatment of onychomycosis of the toes

The use of topical antifungal agents in the treatment of onychomycosis is of great value in clinical practice as there are different limitations regarding the use of systemic treatment. To evaluate the efficacy and safety of a nail lacquer formulation containing ciclopirox 8% in two different posologies: the traditional regimen (3/2/1) and a regimen of weekly use. A blind, randomized, comparative trial which included 41 patients divided into 02 groups, with Group I using the nail lacquer once weekly and Group II using the traditional regimen (3/2/1). Both groups applied the medication for 06 months. The species most frequently found in groups I and II were Trichophyton rubrum (55% and 61.9%) and Trichophyton mentagrophytes (30% and 19%). There was a tendency to a higher level of treatment resistance by T. mentagrophytes infection in both groups, without any predilection for sex, age, proportion of the nail affected at the beginning of the study, duration of the clinical disease and quantity of nails affected per person. Both groups had significant levels of mycological cure, clinical response and therapeutic success and there was no statistically significant difference between groups I and II (p >0.05). The nail lacquer containing ciclopirox 8% was equally effective at a weekly dose when compared to the traditional dosing (3/2/1), allowing a more comfortable regimen.

TRANSUNGUAL PERMEATION OF THE VORICONAZOLE NAIL LACQUER AGAINST TRICHOPHYTON RUBRUM

Introduction: The oral therapies encounter side effects and topical therapies for nail diseases are limited by poor permeability of nail plate. An optimal penetration enhancer would improve drug delivery through nail plate facilitating new possibilities for treating neighboring target sites if the systemic circulation is reached. The purpose of study was to determine amount of voriconazole permeating through the nail plate from the nail lacquer formulation containing permeation enhancer and to demonstrate its susceptibility to the onchomycotic dermatophyte. Methods and materials: The permeability studies were performed on avulsed human cadaver nail plates using modified Franz diffusion apparatus containing phosphate buffer saline in the acceptor chamber. The amount of Voriconazole permeated was quantitatively determined by the UV spectrophotometer. The amount of Voriconazole remaining in the nail after permeation had been retrieved by milling test. Results and discussion: The addition of thioglycolic acid, 5% improved the permeability of the drug by 0.7 as the enhancement factor. The formulation followed zero order kinetics and Korsmeyer- Peppas mechanism of drug release on analyzing on DDSolver. The voriconazole flux of 5592.1 µg/cm/min and 596.75 µg/cm/min had been observed at 24 and 48 hours aliquots respectively for the nail lacquer containing an enhancer. Significantly higher permeation rates were achieved in the presence of an enhancer. Conclusion: The inhibitory zones for the voriconazole transungual nail lacquer were evaluated by testing against the dermatophyte, Trichophyton rubrum on Sabouraud’s Dextrose Agar. The effective zones of inhibitions suggested Voriconazole nail lacquer exhibiting moderate antifungal activity for the onchomycosis treatment.