The Experts below are selected from a list of 309 Experts worldwide ranked by ideXlab platform
Bojan Calija - One of the best experts on this subject based on the ideXlab platform.
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biocompatible microemulsions for improved dermal delivery of Sertaconazole nitrate phase behavior study and microstructure influence on drug biopharamaceutical properties
Journal of Molecular Liquids, 2018Co-Authors: Natasa Bubic Pajic, Vladimir Dobricic, Ines Nikolic, Evgenia Mitsou, Vassiliki Papadimitriou, Aristotelis Xenakis, D Randjelovic, Aleksandra Smitran, Nebojsa Cekic, Bojan CalijaAbstract:Abstract The aim of this study was development of biocompatible topical microemulsions (MEs) for incorporation and improved dermal delivery of Sertaconazole nitrate (SN). For this purpose, phase behavior and microstructure of pseudo-ternary glycereth-7-caprylate/caprate (Emanon EV-E, EV)/cosurfactant/Capryol™ 90/water systems were investigated. Furhermore, the influence of these properties on the drug skin delivery was also assessed. Expansion of ME single-phase regions with the use of short chain alcohols was a consequence of the more fluid interface when compared to other investigated systems, which was confirmed by electron paramagnetic resonance spectroscopy – EPR. The chosen bicontinuous to inverted bicontinuous formulations were assessed against the ME based on polysorbate 80 as referent sample. Despite incorporation of SN within the selected formulations induced similar alternations in electrical conductivity, viscosity and pH values, obtained EPR spectra suggested different SN localization: within the oil phase (for most of the EV based formulations), or interacting with the interface (polysorbate 80 based formulation). Due to higher in vitro drug release (12.24%–18.53%), ex vivo SN penetration into porcine ear skin (dermal retention Enhancement Ratio (ERD) ranged from 2.66 to 4.25) and pronounced antifungal activity, the chosen MEs represent promising vehicles for dermal delivery of SN in treatment of cutaneous fungal infections. The biopharmaceutical and skin performance differences obtained with different formulations were possible to be explained on the basis of their physicochemical characteristics.
Antony M Jose - One of the best experts on this subject based on the ideXlab platform.
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the fda approved drugs ticlopidine Sertaconazole and dexlansoprazole can cause morphological changes in c elegans
Chemosphere, 2020Co-Authors: Kyle F Galford, Antony M JoseAbstract:Abstract Urgent need for treatments limit studies of therapeutic drugs before approval by regulatory agencies. Analyses of drugs after approval can therefore improve our understanding of their mechanism of action and enable better therapies. We screened a library of 1443 Food and Drug Administration (FDA)-approved drugs using a simple assay in the nematode C. elegans and found three compounds that caused morphological changes. While the anticoagulant ticlopidine and the antifungal Sertaconazole caused both accumulations that resulted in distinct distortions of pharyngeal anatomy and lethality upon acute exposure, the proton-pump inhibitor dexlansoprazole caused molting defects and required exposure during larval development. Such easily detectable defects in a powerful genetic model system advocate the continued exploration of current medicines using a variety of model organisms to better understand drugs already prescribed to millions of patients.
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the fda approved drugs ticlopidine Sertaconazole and dexlansoprazole can cause morphological changes in c elegans
bioRxiv, 2020Co-Authors: Kyle F Galford, Antony M JoseAbstract:Urgent need for treatments limit studies of therapeutic drugs before approval by regulatory agencies. Analyses of drugs after approval can therefore improve our understanding of their mechanism of action and enable better therapies. We screened a library of 1443 Food and Drug Administration (FDA)-approved drugs using a simple assay in the nematode C. elegans and found three compounds that caused morphological changes. While the anticoagulant ticlopidine and the antifungal Sertaconazole caused morphologically distinct pharyngeal defects upon acute exposure, the proton-pump inhibitor dexlansoprazole caused molting defects and required exposure during larval development. Such easily detectable defects in a powerful genetic model system advocate the continued exploration of current medicines using a variety of model organisms to better understand drugs already prescribed to millions of patients.
Natasa Bubic Pajic - One of the best experts on this subject based on the ideXlab platform.
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biocompatible microemulsions for improved dermal delivery of Sertaconazole nitrate phase behavior study and microstructure influence on drug biopharamaceutical properties
Journal of Molecular Liquids, 2018Co-Authors: Natasa Bubic Pajic, Vladimir Dobricic, Ines Nikolic, Evgenia Mitsou, Vassiliki Papadimitriou, Aristotelis Xenakis, D Randjelovic, Aleksandra Smitran, Nebojsa Cekic, Bojan CalijaAbstract:Abstract The aim of this study was development of biocompatible topical microemulsions (MEs) for incorporation and improved dermal delivery of Sertaconazole nitrate (SN). For this purpose, phase behavior and microstructure of pseudo-ternary glycereth-7-caprylate/caprate (Emanon EV-E, EV)/cosurfactant/Capryol™ 90/water systems were investigated. Furhermore, the influence of these properties on the drug skin delivery was also assessed. Expansion of ME single-phase regions with the use of short chain alcohols was a consequence of the more fluid interface when compared to other investigated systems, which was confirmed by electron paramagnetic resonance spectroscopy – EPR. The chosen bicontinuous to inverted bicontinuous formulations were assessed against the ME based on polysorbate 80 as referent sample. Despite incorporation of SN within the selected formulations induced similar alternations in electrical conductivity, viscosity and pH values, obtained EPR spectra suggested different SN localization: within the oil phase (for most of the EV based formulations), or interacting with the interface (polysorbate 80 based formulation). Due to higher in vitro drug release (12.24%–18.53%), ex vivo SN penetration into porcine ear skin (dermal retention Enhancement Ratio (ERD) ranged from 2.66 to 4.25) and pronounced antifungal activity, the chosen MEs represent promising vehicles for dermal delivery of SN in treatment of cutaneous fungal infections. The biopharmaceutical and skin performance differences obtained with different formulations were possible to be explained on the basis of their physicochemical characteristics.
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Alkyl polyglucoside vs. ethoxylated surfactant- based microemulsions as vehicles for two poorly water-soluble drugs: physicochemical characterization and in vivo skin performance
Acta Pharmaceutica, 2017Co-Authors: Natasa Bubic Pajic, Marija N. Todosijević, Nebojša Cekić, Sonja Vucen, Bojan Čalija, Milica Ž. Lukić, Tanja Ilić, Vladimir Dobricic, Gordana Vuleta, Snežana SavićAbstract:: Two types of biocompatible surfactants were evaluated for their capability to formulate skin-friendly/non-irritant microemulsions as vehicles for two poorly water-soluble model drugs differing in properties and concentrations: alkyl polyglucosides (decyl glucoside and caprylyl/capryl glucoside) and ethoxylated surfactants (glycereth-7-caprylate/ caprate and polysorbate 80). Phase behavior, structural inversion and microemulsion solubilization potential for Sertaconazole nitrate and adapalene were found to be highly dependent on the surfactants structure and HLB value. Performed characterization (polarized light microscopy, pH, electrical conductivity, rheological, FTIR and DSC measurements) indicated a formulation containing glycereth- 7-caprylate/caprate as suitable for incorporation of both drugs, whereas alkyl polyglucoside-based systems did not exhibit satisfying solubilization capacity for Sertaconazole nitrate. Further, monitored parameters were strongly affected by Sertaconazole nitrate incorporation, while they remained almost unchanged in adapalene-loaded vehicles. In addition, results of the in vivo skin performance study supported acceptable tolerability for all investigated formulations, suggesting selected microemulsions as promising carriers worth exploring further for effective skin delivery of model drugs.
Arunaloke Chakrabarti - One of the best experts on this subject based on the ideXlab platform.
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mic and upper limit of wild type distribution for 13 antifungal agents against a trichophyton mentagrophytes trichophyton interdigitale complex of indian origin
Antimicrobial Agents and Chemotherapy, 2020Co-Authors: Dipika Shaw, Sunil Dogra, Arunaloke Chakrabarti, Shreya Singh, Jyothi Jayaraman, Ramesh M Bhat, Saumya Panda, Nishat Anjum, Aruna Chowdappa, Mahantesh B NagamotiAbstract:Dermatophytosis due to the Trichophyton mentagrophytes-Trichophyton interdigitale complex is being increasingly reported across India. Reports of therapeutic failure have surfaced recently, but there are no clinical break points (CBP) or epidemiological cutoffs (ECVs) available to guide the treatment of dermatophytosis. In this study, a total of 498 isolates of the T. mentagrophytes -interdigitale complex were collected from six medical centers over a period of five years (2014 to 2018). Antifungal susceptibility testing of the isolates was carried out for itraconazole, fluconazole, ketoconazole, voriconazole, luliconazole, Sertaconazole, miconazole, clotrimazole, terbinafine, amorolfine, naftifine, ciclopirox olamine, and griseofulvin. The MICs (in mg/liter) comprising >95% of the modeled populations were as follows: 0.06 for miconazole, luliconazole, and amorolfine; 0.25 for voriconazole; 0.5 for itraconazole, ketoconazole, and ciclopirox olamine; 1 for clotrimazole and Sertaconazole; 8 for terbinafine; 16 for naftifine; 32 for fluconazole; and 64 for griseofulvin. A high percentage of isolates above the upper limit of the wild-type MIC (UL-WT) were observed for miconazole (29%), luliconazole (13.9%), terbinafine (11.4%), naftifine (5.2%), and voriconazole (4.8%), while they were low for itraconazole (0.2%). Since the MICs of itraconazole were low against the T. mentagrophytes -interdigitale complex, this could be considered the choice of first-line treatment. The F397L mutation in the squalene epoxidase (SE) gene was observed in 77.1% of isolates with a terbinafine MIC of ≥1 mg/liter, but no mutation was detected in isolates with a terbinafine MIC of <1 mg/liter. In the absence of CBPs, evaluation of the UL-WT may be beneficial for managing dermatophytosis and monitoring the emergence of isolates with reduced susceptibility.
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mutation in the squalene epoxidase gene of trichophyton interdigitale and trichophyton rubrum associated with allylamine resistance
Antimicrobial Agents and Chemotherapy, 2018Co-Authors: Shivaprakash M Rudramurthy, Shamanth A Shankarnarayan, Sunil Dogra, Dipika Shaw, Khurram Mushtaq, Raees A Paul, Tarun Narang, Arunaloke ChakrabartiAbstract:Dermatophytosis, the commonest superficial fungal infection, has gained recent attention due to its change of epidemiology and treatment failures. Despite the availability of several agents effective against dermatophytes, the incidences of chronic infection, reinfection, and treatment failures are on the rise. Trichophyton rubrum and Trichophyton interdigitale are the two species most frequently identified among clinical isolates in India. Consecutive patients (n = 195) with suspected dermatophytosis during the second half of 2014 were included in this study. Patients were categorized into relapse and new cases according to standard definitions. Antifungal susceptibility testing of the isolated Trichophyton species (n = 127) was carried out with 12 antifungal agents: fluconazole, voriconazole, itraconazole, ketoconazole, Sertaconazole, clotrimazole, terbinafine, naftifine, amorolfine, ciclopirox olamine, griseofulvin, and luliconazole. The squalene epoxidase gene was evaluated for mutation (if any) in 15 T. interdigitale and 5 T. rubrum isolates exhibiting high MICs for terbinafine. A T1189C mutation was observed in four T. interdigitale and two T. rubrum isolates. This transition leads to the change of phenylalanine to leucine in the 397th position of the squalene epoxidase enzyme. In homology modeling the mutant residue was smaller than the wild type and positioned in the dominant site of squalene epoxidase during drug interaction, which may lead to a failure to block the ergosterol biosynthesis pathway by the antifungal drug.
V Baliga - One of the best experts on this subject based on the ideXlab platform.
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efficacy and tolerability of Sertaconazole nitrate 2 cream vs miconazole in patients with cutaneous dermatophytosis
Mycoses, 2011Co-Authors: Ashutosh Sharma, D G Saple, Amar Surjushe, G R R Rao, M Kura, S Ghosh, C Bolmall, V BaligaAbstract:Sertaconazole is a new antifungal agent. To compare the efficacy and tolerability of Sertaconazole and miconazole cream in cutaneous dermatophytosis, this prospective, randomized, multicentric comparative, phase 4 study was undertaken in 260 patients with cutaneous dermatophytosis after approvals from Institutional Ethics Committees. Patients were assigned to Sertaconazole cream (2%) or miconazole cream (2%) topically twice daily for 2 weeks after obtaining informed consent. Efficacy variables included changes in mean scores of erythema, pruritus, desquamation, erythema/itching, burning/weeping, scaling/pustule and overall global assessment. Safety and tolerability were also assessed. A total of 122 patients in the Sertaconazole group and 128 in the miconazole group completed the study with 10 drop-outs. There was a significant decrease (P < 0.05) in mean symptom scores and total scores from the first week onwards, sustained till 2 weeks and statistically significant (P < 0.05) in favour of Sertaconazole. Moreover, 62.3% patients had complete clinical cure in the Sertaconazole group (P < 0.05) compared with 44.6% in miconazole users. Both drugs were well tolerated and five patients in the Sertaconazole group and nine in the miconazole group reported mild to moderate adverse events. Therapy with Sertaconazole cream (2%) provided a better efficacy and tolerability compared with the miconazole cream (2%) and could thus be a therapeutic option in cutaneous dermatophytosis.
