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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Miconazole is a synthetic phenethyl imidazole antifungal agent that can be used topically and by intravenous infusion. This agent selectively affects the integrity of fungal cell membranes, high in ergosterol content and different in composition from mammalian cell membranes. Miconazole is indicated for topical application in the treatment of tinea pedis, tinea cruris, and tinea corporis caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum, in the treatment of cutaneous candidiasis and in the treatment of pityriasis (tinea) versicolor. In pharmaceutical products, miconazole is nearly always employed as miconazole nitrate (CAS number 22832-87-7, EC number 245-256-6, molecular formula C18H15Cl4N3O4); buccal tablets may contain miconazole base (1).
Novel methods of antifungal administration
Published in Mahmoud A. Ghannoum, John R. Perfect, Antifungal Therapy, 2019
Relative to administration of amphotericin B, direct administration of other antifungals into the CNS is infrequently reported. Miconazole has been administered intrathecally in the treatment of various CNS infections, to include coccidioidal meningitis, cryptococcal meningitis, histoplasmosis meningitis, and Candida albicans infections [162–167]. Doses in adults ranged from 1 to 30 mg [162–167], with lower doses of 3–5 mg in children [166,167]. Adverse effects of intrathecal miconazole may include arachnoiditis [124,164], cisternal hemorrhage [124,147,164], ventricle hemorrhage [162], transient numbness [162], and bacterial infections when administered via Ommaya reservoir [166].
Formulary
Published in Sarah Bekaert, Alison White, Integrated Contraceptive and Sexual Healthcare, 2018
Sarah Bekaert, Alison White, Kathy French, Kevin Miles
Miconazole is a synthetic imidazole antifungal agent with a broad spectrum of activity against pathogenic fungi (including yeasts and dermatophytes) and Gram-positive bacteria. There is little absorption through mucous membranes when miconazole is applied topically.
Polymeric versus lipid nanocapsules for miconazole nitrate enhanced topical delivery: in vitro and ex vivo evaluation
Published in Drug Delivery, 2022
Rania S. Abdel-Rashid, Doaa A. Helal, Ahmed Adel Alaa-Eldin, Raghda Abdel-Monem
Miconazole nitrate (MN) is a broad-spectrum antifungal drug of the azole derivatives extensively used for the treatment of dermatophytosis, cutaneous mycosis, and fungal infections affecting the vagina, mouth and skin, including candidiasis (Aljaeid & Hosny, 2016). Miconazole is a weak base (pKa = 6.7) with poor aqueous solubility (1.03 µg/mL) and rapid clearance hindered its systemic efficacy (Jain et al., 2010). MN acts by dual pathways: impedes the synthesis of ergosterol on fungal cell and causes accretion of reactive oxygen species (ROS) in the fungal cell, triggering oxidative damage, and cell death (Amaral et al., 2019). Currently, miconazole is available as conventional topical formulations such as cream, lotions, spray liquids, and suppository for vaginal use. Previously published reports stated that miconazole topical applications exhibited poor skin penetration and therefore higher doses are required to recompense low permeability (Qushawy et al., 2018). Moreover, it suffers from vast side effects on the application site like burning, redness, and swelling (Kenechukwu et al., 2018). Therefore, various approaches have been attempted to overcome these hitches and consequently improve the therapeutic efficacy of drugs such as SLNs (Aljaeid & Hosny, 2016), nano-suspensions (Cerdeira et al., 2010), transdermal films (Ofokansi et al., 2015), ethosomes, liposomes, and nanostructured lipid carriers (NLCs) (Firooz et al., 2016).
A nanocarrier system that potentiates the effect of miconazole within different interkingdom biofilms
Published in Journal of Oral Microbiology, 2020
Laís Salomão Arias, Jason L Brown, Mark C Butcher, Christopher Delaney, Douglas Roberto Monteiro, Gordon Ramage
The results of planktonic and sessile MICs of MCZ and IONPs-CS-MCZ against several C. albicans strains showed that the planktonic cells were equally affected by the tested drugs. However, according to the sMIC80 results, it was possible to obtain higher antimicrobial effect at lower concentrations of MCZ against biofilms, by using a nanocarrier. Miconazole has been used for over 30 years and is prescribed specifically against oral fungal infections for topical use [35,36]. Different from other azoles, MCZ has a dual mechanism of action; besides interfering with ergosterol synthesis by inhibition of lanosterol demethylase, it also inhibits fungal catalase and peroxidase, therefore increasing intracellular reactive oxygen species and leading to cell death [37]. As for CS, literature suggests that the interaction between the positively charged drug and the negatively charged bacterial cell membranes results in the leakage of intracellular constituents [38,39]. Therefore, the lower MIC values found for the IONPs-CS-MCZ could be explained by the synergistic action between CS and MCZ or that drug-delivery nanosystems are designed to break through physical barriers to target the cell of interest [21,40]. Additional data from this study showed that IONPs-CS-MCZ was able to act effectively against planktonic and sessile cells of most microbial species used in the three biofilm models, confirming that it has both antifungal and antibacterial activity. Indeed, literature data reports the antibacterial potential of topical use concentrations of MCZ, specially against Gram-positive bacteria [16].
Innovative nanocompounds for cutaneous administration of classical antifungal drugs: a systematic review
Published in Journal of Dermatological Treatment, 2019
Rafael Silva Santos, Kahynna Cavalcante Loureiro, Polyana Santos Rezende, Luciana Nalone Andrade, Raquel de Melo Barbosa, Antonello Santini, Ana Cláudia Santos, Classius Ferreira da Silva, Eliana Barbosa Souto, Damião Pergentino de Sousa, Ricardo Guimarães Amaral, Patrícia Severino
Commonly used classical formulations for topical administration of miconazole have not demonstrated efficiency for deep-seated fungal infections. In this context, Pandit et al. (53) prepared ultraflexible liposomes and compared them with conventional liposomes containing miconazole for topical application. The in vitro skin permeation using rat skin was evaluated and suggested liposomal formulations may contribute to the enhanced penetration of drug within the subcutaneous barrier. An in vivo study using albino rats with induced cutaneous candidiasis presented higher antifungal activity for ultraflexible liposomal (89%), compared to traditional liposomes (45%) and to plain drug solution (33%). The prepared ultraflexible liposomes were able to quickly improve the localized drug action in the skin. It offers a better option to manage the deep-seated fungal infections, due to the higher capacity of ultraflexible liposomal formulation to cross the skin, carry and deliver the therapeutic agents into the subcutaneous layers (53).