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This study's main focus was on the process by which Ciclopirox adhered to AlN nanostructures, Calculations using the density functional theory were done to reach this goal. The calculations encompassed the assessment of Ciclopirox's adsorption energy, the evaluation of the energy band gap, the analysis of variations in the energy band gap, the examination of charge transfers, and the characterisation of the types of interactions that arise from Ciclopirox's adsorption onto AlN nanostructures. We carried out an investigation using the AIM method to explore deeper into the binding properties between the studied AlN nanostructures and Ciclopirox. Our discoveries provide light on the Ciclopirox/AlN nanosheet interaction's electrostatic characteristics. Moreover, the presence of Ciclopirox led to an augmentation in the electrical conductivity of the AlN nanostructures. This intriguing outcome suggests the potential application of these AlN nanomaterials as chemical sensors, capable of generating an electronic signal upon detection of this chemically modified amino acid. The observed sensitivity sequence indicated that the AlN nanosheet exhibited the highest sensitivity, followed by the AlN nanotube and the AlN nanocluster. In conclusion, our study provides compelling evidence supporting the AlN nanosheet as an excellent choice for the detection of Ciclopirox compared to other AlN nanostructures. [ABSTRACT FROM AUTHOR]

A substantial amount of scholarly inquiry has focused on the advancement of innovative methodologies for drug administration. In this research, both graphyne (GY) and BN-analog GY (BNY) nanosheets are presented. The study focuses on the carbon allotrope GY. Density Functional Theory (DFT) calculations were used to assess how GY, BNY, and the anticancer drug ciclopirox (CPX) interact with one another. It was observed that the inherent capability of pristine GY to augment CPX adsorption is intensified by the involvement of nitrogen (N) and boron (B) atoms. Furthermore, examination using Ultraviolet–Visible (UV-Vis) analysis exhibited a shift towards less energetic states, corresponding to longer wavelengths. Moreover, the interaction between CPX and BNY displayed chemical reactivity, rendering it conducive for forming bonds at the adsorption site. Additionally, a thorough investigation via the Atoms-In-Molecules (AIM) analysis furnished a more profound comprehension of the associations between the drug and the nanosheet. Notably robust connections between CPX and BNY were detected. As a consequence, the potential of BNY to function as a viable transporter for CPX in the realm of drug delivery was substantiated. [ABSTRACT FROM AUTHOR]

Objective: Septic shock, the most severe stage of sepsis, is a deadly inflammatory disorder with high mortality. Ciclopirox (CPX) is a broad-spectrum antimycotic agent which also exerts anti-inflammatory effects in human diseases. However, whether CPX can relieve inflammatory response in LPS-induced septic shock remains unclear. Materials and Methods: Male C57BL/6 mice LPS were injected intraperitoneally with LPS to simulate septic shock in vivo. RAW264.7 cells and bone marrow-derived macrophages (BMDMs) were subject to LPS treatment to simulate septic shock in vitro. ELISA was applied to detect the level of pro-inflammatory cytokines. Cell viability was assessed by CCK-8 assay. Protein levels was detected by western blotting. Results: CPX enhanced the survival rate and attenuated inflammation in mice with LPS-induced septic shock. Similarly, CPX dose-dependently mitigated LPS-induced inflammation in BMDMs. It was also found that Sortilin 1 (SORT1) was upregulated in both in vivo and in vitro models of LPS-induced septic shock. In addition, SORT1 overexpression counteracted the alleviative effects of CPX on the inflammation response of LPS-challenged BMDMs by activating the Wnt/ß-Catenin signaling. Furthermore, BML-284 (a Wnt/ß-Catenin agonist) treatment also abrogated CPX-mediated moderation of LPS-triggered inflammatory reaction in BMDMs. Conclusions: In sum, we found that CPX protected against LPS-induced septic shock by mitigating inflammation via SORT1-mediated Wnt/ß-Catenin signaling pathway. [ABSTRACT FROM AUTHOR]

Onychomycosis accounts for 90% of nail infections worldwide. Topical therapy provides localized effects with minimal adverse systemic actions, yet its effectiveness is limited by minimal drug permeation through the keratinized nail plate. Ciclopirox (CIX) is a FDA-approved broad-spectrum antimycotic agent. However, the complete cure with its nail lacquer (8% w/v) may continue for one year with a high cost. Therefore, poly lactide-co-glycolide (PLGA) nanocapsules (NCs) of CIX were prepared by nanoprecipitation and optimized through a 23 factorial design to be incorporated into hydroxypropyl chitosan (HPCH) based nail lacquer. Nail hydration, in vitro nail absorption, minimum inhibitory concentration (MIC), inhibition zones and ex vivo fungal growth on nail fragments were evaluated. The optimized NCs of CIX based on 100 mg PLGA 2 A and lipoid S75 showed a mean diameter of 174.77 ± 7.90 nm, entrapment efficiency (EE%) of 90.57 ± 0.98%, zeta potential (ZP) of -52.27 ± 0.40 mV and a prolonged drug release. Nail lacquer of the optimized NCs exhibited a higher stability than NCs dispersion. Compared to CIX solution (1% w/v), the respective decrease in MIC for NCs and their lacquer was four- and eight-fold. The lacquer superiority was confirmed by the enhancement in the nail hydration and absorption by 4 and 2.60 times, respectively, relative to CIX solution and the minimal ex vivo fungal growth. Therefore, HPCH nail lacquer of (1% w/v) CIX-PLGA-NCs can be represented as a potential topical delivery system for enhanced in vitro nail absorption and therapeutic efficacy against onychomycosis at a low dose. [ABSTRACT FROM AUTHOR]

With the aim of reducing system absorption and consequently, the side effects, and simultaneously select a penetration enhancing, three topical formulations with 0.5% ciclopirox olamine (CO) and 15% of propylene glycol (PG), ethoxydiglycol or oleic acid were developed and evaluated regarding the skin penetration and cutaneous retention of the drug using Franz diffusion cells. Release experiments were performed through synthetic membrane while dermatomed pig ear skin was used to evaluate CO skin penetration and skin retention. Retention studies were carried out applying tape stripping method and dosing CO in stratum corneum and in epidermis and dermis. A HPLC method was validated for quantifying CO. All formulations tested with synthetic membrane presented no retention of the drug. Permeation data suggested that there was no systemic absorption of ciclopirox olamine from the studied formulations, even when the skin penetration enhancers were applied. Higher concentrations of the drug were found in the stratum corneum (SC) and also in epidermis and dermis, for all of the developed formulations. The addition of enhancers improved the penetration and cutaneous retention of CO, and propylene glycol promoted higher concentrations in epidermis and dermis, probably because its cumulative effect on the skin and by an efficient solvent power. [ABSTRACT FROM AUTHOR]

Context: Onychomycosis is a common fungal infection of the nail plate and bed that affects up to 14% of the population and can have a substantial impact on the quality of life of those affected. Objective: This study compared the onychopharmacokinetics, nail absorption, nail distribution, and nail penetration of [14C]-ciclopirox dissolved in novel lipid diffusion enhancers with that of a commercial ciclopirox nail lacquer using the in vitro finite dose model. Materials and methods: The penetration rate of ciclopirox was determined by applying doses of topical formulation twice daily to human nail plates for 11 d. Drug absorption was then measured by monitoring its rate of appearance in each nail layer and in the cotton pad/nail supporting bed. Results: After a multiple day treatment, cumulative concentrations of ciclopirox formulated with lipid enhancers in the deep nail layer and the nail bed were significantly greater than cumulative concentrations of the commercial ciclopirox lacquer ( p < 0.001) as well as several orders of magnitude greater than the minimal inhibitory concentration (MIC) deemed necessary to inhibit the growth of the causative dermatophyte species. Conclusion: When formulated with lipid enhancers, the amount of ciclopirox in the ventral/intermediate layer and supporting bed dramatically exceed the inhibitory concentration of ciclopirox for the most common onychomycosis organisms. These results suggest that topical ciclopirox with lipid enhancers has the potential to be an effective topical treatment for onychomycosis, and the lipidic pathway of the nail can be utilized as a means of effective transungual delivery. [ABSTRACT FROM AUTHOR]

Context: Ciclopirox olamine (CPO) is indicated in the treatment of vaginal fungal infections. The frequent and large dosing of available vaginal CPO creams gives rise to poor compliance amongst females. In such a situation a delivery system capable of providing sustained release of CPO is warranted and can be realized through incorporation of its liposomal formulation into a mucoadhesive gel base. The liposomal formulation would offer sustained release whereas mucoadhesive gel would prolong the contact with vaginal wall; thus avoiding frequent and large dosing. Objective: The present study aimed at investigating mucoadhesive liposomal CPO gel for vaginal use. Method: The study embarked on evaluating liposomal CPO and its Carbopol 974®P gel for stability at vaginal pH, release profile, rheological characteristics, mucoadhesive behavior and finally antifungal activity. Results: The results revealed that CPO liposomes were stable at vaginal pH; its Carbopol gel released 58.75 ± 6.4% of CPO at the end of 24 h which suggested sustained release. Rheology via viscometric, oscillatory stress sweep and oscillatory frequency sweep testing of the gel, studied at different temperatures and under different dilutions with vaginal fluid simulant testified pseudoplastic behavior of the gel. It also pointed towards the predominance of elastic behavior of the gel at all the dilutions. The gel exhibited good mucoadhesivity to sheep vaginal tissue. Furthermore, CPO entrapped in liposome too displayed antifungal activity. Conclusion: The study undertaken recommended Carbopol 974®P gel loaded with CPO liposomes as a potential delivery system for treatment of fungal vaginal infections. [ABSTRACT FROM AUTHOR]

Ciclopirox olamine is an antifungal agent widely used in dermatological formulations for topical application. The methods described for its determination usually present time-consuming sample treatment or require major human participation. Here we present a rapid flow system for the determination of ciclopirox olamine, based on the use of sequential injection analysis with terbium-sensitized luminescence detection. The reaction between terbium and the analyte is carried out on-line, recording the analytical signal at 300/545 nm (λex/λem). A detection limit of 15 µg L−1and a R.S.D. of 3% (n = 10) were obtained. It is worth mentioning that the method here presented is the only one that uses a flow system for the determination of ciclopirox olamine. The flow system was applied to the analysis of different pharmaceutical preparations available in the Spanish Pharmacopoeia. A recovery study was performed, obtaining satisfactory results. The high solution throughput obtained, 50 samples per hour, makes the method suitable for its implementation in pharmaceutical laboratories for routine analysis. [ABSTRACT FROM AUTHOR]

This review outlines recent data on treatment modalities and outcomes with antifungal therapy in onychomycosis. Included are topical, mechanical, chemical and systemic treatments or a combination thereof. Topical treatments, or transungual drug delivery systems (TUDDS), including ciclopirox and amorolfine were shown to be effective if used alone for mild-moderate nail involvement. Specifically, superficial white onychomycosis (SWO) restricted to the dorsum of the nail plate and moderate distal lateral subungual onychomycosis (DLSO). Mechanical treatments were mostly effective as adjuncts to topical therapy which include nail avulsion and abrasion. In particular, partial nail avulsion aids topical therapy in DLSO and partial subungual onychomycosis for a more effective therapy. Chemical avulsion is a painless method of debridement which uses a keratinolysis formula that is effective only in limited and early disease. Systemic therapies have been shown to be effective with terbinafine and itraconazole is suggested as being the most cost-effective therapy. Systemic therapies require consideration of side effects and monitoring by both patient and physician prior to treatment application. An effective suggestion is the use of a topical with debridement for mild-moderate onychomycosis and systemic (terbinafine) plus topical for severe onychomycosis. Most treatment modalities will require long-term use from 3 to 9 months to be most effective, with strategies presented in Part II of this review. [ABSTRACT FROM AUTHOR]

Objective : To assess the daily treatment costs and the average cost-effectiveness of three topical onychomycosis therapies – amorolfine 5% and ciclopirox 8% nail lacquers and tioconazole 28% nail solution – when used as indicated in France, the UK, Germany and Italy. Methods : The quantity of drug required and nail size measurements were investigated and, knowing the cost per bottle of each study drug, used to calculate the average treatment cost per patient. Using the prevalence of infection data, the weighted average total treatment cost per patient and hence the weighted average daily treatment cost and cost per patient cured, were calculated. Results : Amorolfine was consistently more cost-effective in terms of weighted average daily treatment cost and cost per patient cured than ciclopirox and tioconazole, when all therapies were used as indicated to treat onychomycosis. In France, for example, the weighted average daily treatment cost of amorolfine was found to be €0.23 and €0.40 when used once and twice a week, respectively; the cost per patient cured for amorolfine was €84. By comparison, the weighted average daily treatment cost of ciclopirox was found to be €0.81; the cost per patient cured was €252. Conclusions : When used as indicated, amorolfine 5% nail lacquer is more cost-effective than ciclopirox 8% and tioconazole 28% for onychomycosis of toenail, fingernail or both in males and females in France, UK, Germany and Italy. [ABSTRACT FROM AUTHOR]

Background: Treatment of onychomycosis has recently been enhanced by the introduction of combination therapies. Objective: To evaluate the efficacy of a combination therapy of ciclopirox nail lacquer and oral terbinafine compared to oral terbinafine monotherapy for the treatment of onychomycosis caused by dermatophytes. Patients and methods: Eighty patients with onychomycosis were randomly assigned to receive either oral terbinafine 250 mg/day for 16 weeks or a combination of oral terbinafine 250 mg/day for 16 weeks and topical ciclopirox nail lacquer once daily for 9 months. Both groups were followed up for 9 months from start of treatment. Results: After 9 months of treatment, the mycological cure rates were 22/ 34 (64.7%) for the terbinafine-only group and 30/34 (88.2%) for the combination therapy group (p <0.05). No significant difference was noted in the complete cure rate. Conclusion: Combination therapy of oral terbinafine and ciclopirox nail lacquer is a safe and more effective treatment for onychomycosis than terbinafine alone, especially in younger patients and in shorter-duration onychomycosis. [ABSTRACT FROM AUTHOR]

Commercial antimycotic nail lacquers are commonly based on water-insoluble resins. The present study was aimed at evaluating a novel, experimental nail lacquer (P-3051, Polichem SA, Lugano, Switzerland) based on the water-soluble film-forming agent hydroxypropyl chitosan (HPCH). The in vitro permeation of ciclopirox (CPX) from P-3051 and from a commercial, water-insoluble lacquer based on a vinyl resin (PenlacTM, Aventis Pharma), was investigated using thin membranes obtained from bovine hooves, an accepted model for human nails. Similar CPX permeation fluxes at steady state through the membranes, but signiticandy different lag times were observed for P-3051 and PenlacTM, when these were tested as dry films. The formulations thus appeared to influence only the time required by CPX to saturate the membrane, and not the final drug concentration gradient in the membrane. Permeation experiments performed on the same membranes and on hairless mouse skin with P-3051 and with a similar, HPCH-free vehicle (ERV), both tested in liquid form, disproved the possibility that HPCH might act as a permeation enhancer for CPX in either substrate. The possible reasons for the greater efficiency of the HPCH vehicle in terms of CPX transfer from the vehicle itself to the keratin membrane are discussed. This effect might be tentatively attributed to a particular affinity of HPCH for the membrane, resulting in intimate contact and strong adhesion of the HPCH lacquer to the keratin substrate. [ABSTRACT FROM AUTHOR]

BACKGROUND: Dandruff is a chronic scalp condition characterized by scaling. The common causative agent is now accepted to be the lipophilic yeast Malassezia furfur . Ketoconazole, a highly effective antifungal agent against M. furfur has been used for the treatment of dandruff. AIM: To determine whether a 1.5% ciclopirox olamine shampoo is as effective as a 2% ketoconazole shampoo for the treatment of mild to moderate dandruff. METHODS: A total of 64 patients, with mild to moderate dandruff, participated in the study. The study consisted of three consecutive phases: a 2-week washout period, a 4-week treatment period and a 2-week post-treatment period. Patients were randomized equally to either the 1.5% ciclopirox olamine shampoo or 2% ketoconazole shampoo. An overall dandruff score was calculated using an area of dandruff involvement score and a severity score. Patients evaluated the presence of pruritus and also reported a global evaluation of efficacy. RESULTS: In all, 57 patients successfully completed all three phases. The overall dandruff score declined progressively throughout the treatment period for both shampoos. A slight increase in pruritus was observed in the ciclopirox olamine treatment group during the post-treatment phase. Regarding global self-assessment of efficacy, both treatment groups were pleased with their scalp condition following treatment. CONCLUSION: Ciclopirox olamine shampoo appears to offer an effective, safe and easy to use treatment for mild to moderate dandruff. [ABSTRACT FROM AUTHOR]

BACKGROUND: The association between seborrhoeic dermatitis and dandruff and the yeast Malassezia furfur is well recognized. Symptoms include scalp itchiness and scaling. Due to its antimycotic activity, ciclopirox olamine is established as an effective treatment for these scalp conditions. Salicylic acid has keratolytic properties and aids in the removal of scales. OBJECTIVE: To compare the therapeutic efficacy of a shampoo containing 1.5% ciclopirox olamine and 3% salicylic acid (CPO/SA) with Nizoral[sup ®] (2.0% ketoconazole shampoo) in a study involving 154 subjects with dandruff - 70 of whom also had seborrhoeic dermatitis of the scalp. Nizoral[sup ®] is currently a registered treatment for dandruff and seborrhoeic dermatitis. METHODS: The shampoos were used three times week for 4 weeks, with 2-week washout and follow-up periods. Clinical and self-assessments were made throughout treatment and after follow-up (day 43). Within and between-treatment assessments of signs and symptoms were analysed. RESULTS: In the two groups, seborrhoeic dermatitis and dandruff improved significantly throughout treatment, with lower clinical and self-assessment scores at both the end of treatment (day 29) and follow-up (day 43). Only the subjects treated with CPO/SA shampoo showed a significant reduction in the itching of seborrhoeic dermatitis at these times. CONCLUSION: The study demonstrated that both CPO/SA and Nizoral[sup ®] were safe and effective in the treatment of dandruff and seborrhoeic dermatitis. [ABSTRACT FROM AUTHOR]