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Sertaconazole
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Sertaconazole is a synthetic imidazole derivative with antifungal, antibacterial, anti-inflammatory and anti-pruritic activity. Besides its ability to inhibit the synthesis of ergosterol, the benzothiophene ring of sertaconazole is able to insert into the fungal cell wall instead of tryptophan. This increases the permeability of the cell wall. In addition, sertaconazole suppresses the release of cytokines. This drug is indicated for the topical treatment of interdigital tinea pedis caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum. In pharmaceutical products, sertaconazole is employed as sertaconazole nitrate (CAS number 99592-39-9, EC number not available, molecular formula C20H16C13N3O4S) (1).
Topical Azoles
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Joanne L. Sharp, Michael A. Pfaller
Sertaconazole demonstrates a second effect on cell function—it binds directly to non-sterol lipids in the membrane, which interferes with regulation of the permeability of the fungal cell membranes. Inhibition of sterol synthesis interferes with fungal cell growth, whereas direct interaction with the membrane produces subsequent leakage of intracellular components, particularly adenosine triphosphate (ATP), thereby contributing to immediate cell death. As a result, sertaconazole is an effective fungicidal and fungistatic agent (Agut et al., 1992; Croxtal and Plosker, 2009).
Solutol HS15 based binary mixed micelles with penetration enhancers for augmented corneal delivery of sertaconazole nitrate: optimization, in vitro, ex vivo and in vivo characterization
Published in Drug Delivery, 2018
Nihal Farid Younes, Sally Adel Abdel-Halim, Abdelhalim I. Elassasy
Sertaconazole nitrate (STZ) is a new antifungal agent of the imidazole class with antifungal activity against wide range of pathogenic fungi, some of which are Fusarium, Aspergillus, and yeasts (Croxtall and Plosker, 2009), which are the most common contributory factors for fungal ocular diseases (He et al., 2016). STZ is reported to have good ocular tolerance (Romero et al., 1996), which makes it an excellent candidate for the treatment of keratomycosis. However, the extreme poor aqueous solubility of STZ acts as an obstacle that limits its ocular clinical efficacy (Albet et al., 1992), and urges for the development of new delivery systems capable of enhancing its aqueous solubility, and improving its ocular penetration and retention.
Lipid liquid-crystalline nanoparticles sustained teicoplanin delivery for treatment of chronic osteomyelitis: in vitro and in vivo studies
Published in Journal of Microencapsulation, 2022
Cubosomes are prepared by melt emulsification and sonication technique using lipid (glycerol monooleate or phytantriol) and non-ionic surfactants (Shabbir et al.2020). The application of cubosomes has the advantage of sustained drug release, and their topical use has drawn the attention of several formulators (Pan et al.2013; Duttagupta et al.2016). Elakkad et al. (2021) used tenoxicam loaded hyalcubosomes and noted high drug permeation and deposition to treat osteoarthritis for 8 weeks (Elakkad et al.2021). Liu et al. (2013) showed the potential of cubosomes to deliver earthworm fibrinolytic enzyme for inner ear treatment (Liu et al.2013). Kapoor et al. (2020) developed methotrexate loaded cubosomes for effective treatment of rheumatoid arthritis (Kapoor et al.2020). Morsi et al. noted the application of silver sulfadiazine loaded cubosomes to treat deep second degree burns (Morsi et al.2014). Li et al. prepared paeonol-loaded cubosomes for sustained drug delivery and noted high drug permeation and retention in the skin tissue without local irritation (Li et al.2015). Marilisa Guimaraes Lara et al. noted sustained celecoxib release, improved permeation and drug retention in skin tissue using a cubic phase system of monolein (Estracanholli et al.2014). Flak et al. formulated AT101 R-(-)-enantiomer of cottonseed-derived polyphenol gossypol loaded cubosomes for effective therapy of glioblastoma multiforme (Flak et al.2020). Boge et al. loaded antimicrobial peptide LL-37 in cubosomes for skin infection and noted improved efficacy against Staphylococcus aureus (Boge et al.2019). Younes et al. showed an improved permeation profile of sertaconazole using cubosomes in ex vivo and in vivo studies (Younes et al.2018). Researchers have observed comprehensive advantages of cubosomes over liposomes, microemulsions and nano-emulsions.