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Liposome-Based Delivery of Therapeutic Agents
Published in Emmanuel Opara, Controlled Drug Delivery Systems, 2020
Eneida de Paula, Juliana Damasceno Oliveira, Fernando Freitas de Lima, Lígia Nunes de Morais Ribeiro
The broadest spectrum agents of antifungal therapy worldwide in the last 50 years have been the polyene compounds (e.g. amphotericin, nystatin, hamycin, dermostatin, etc.). Amphotericin B (AMB) is the gold standard antifungal drug, but its use is still associated with severe adverse effects (mainly impairment of nephron function by cumulative doses, besides fever, chills, myalgia, and thrombophlebitis), low clinical response, and high mortality rates. Another class of antifungal, the azoles, include ketoconazole, fluconazole, and itraconazole (launched in the 80s), and later the second-generation triazoles voriconazole, ravuconazole, and posaconazole. Their good activity against molds brought some help to the antifungal therapy, although some of them are mostly used as topical agents. Allylamines, such as butenafine and naftifine, are the third class of antimycotic agents that are able to inhibit squalene epoxidase, restraining the synthesis of ergosterol.143 In the beginning of the 21st century, another class of drugs, the echinocandins–noncompetitive inhibitors of β-1-3-glucan synthase, blocking the synthesis of the fungal cell wall – appeared as a promise for the candidiasis and aspergillosis treatment.144,145
Green formulation, characterization, antifungal and biological safety evaluation of terbinafine HCl niosomes and niosomal gels manufactured by eco-friendly green method
Published in Journal of Biomaterials Science, Polymer Edition, 2022
Katayoun Morteza-Semnani, Majid Saeedi, Jafar Akbari, Shakiba Hedayati, Seyyed Mohammad Hassan Hashemi, Seyyed Mobin Rahimnia, Amirhossein Babaei, Mona Ghazanfari, Iman Haghani, Mohammad Taghi Hedayati
A total of 64 molecularly identified isolates of Aspergillus (n = 44), Fusarium (n = 10) and Trichophyton (n = 10) were obtained from the collection of Invasive Fungi Research Center (IFRC) of Mazandaran University of Medical Sciences were included in the study. Identification of Aspergillus and Fusarium at species level were done by applying of sequencing of the β-tubulin-encoding gene (benA) and partial translation elongation factor 1 alpha (TEF-1alpha) gene, respectively. Trichophyton mentagrophytes was identified by squalene epoxidase gene (SQLE) locus. The clinical source of Aspergillus species including A. fumigatus and A. niger were from Broncho-alveolar lavage (BAL) of patients with different underlying conditions and Fusarium species from patients with onychomycosis. All Trichophyton mentagrophytes were originated from patients with confirmed cases of dermatophytosis who were clinical TER resistant according to our previous study (unpublished data).
Norethisterone exposure alters the transcriptome of Marine Medaka (Oryzias melastigma) larvae
Published in Chemistry and Ecology, 2021
Xueyou Li, Xiaona Lin, Yuebi Chen, Zhongduo Wang, Yusong Guo, Gyamfua Afriyie, Ning Zhang, Zhongdian Dong
Many progestins have strong biological activity, even at ng/L, which poses a potential threat to aquatic organisms [35–37]. In addition, coexistence with other pollutants may cause more complex effects [35]. The role of synthetic progestins, such as NET, in fish, may be multifaceted, and the potential mechanisms are still uncertain. This may depend on the progestin type, exposure time, species, and developmental stage [6]. By changing gene expression and disrupting the normal signal transduction cascade, even low concentrations of NET continuously discharged into the aquatic environment may have numerous consequences for the health of aquatic vertebrates [27,37–39]. Studies have shown that progestins can regulate the expression of genes involved in steroid production [10,31,40,41]. In this study, even low-level NET exposure inhibited the synthesis of cholesterol-related genes, including 24-dehydrocholesterol reductase (dhcr24), 7-dehydrocholesterol reductase (dhcr7), 3-hydroxy-3-methyl Glutaryl-coenzyme a reductase (hmgcra), squalene epoxidase (sqle), and lanosterol 14-alpha demethylase (cyp51a1) (Figure S2). Of these, sqle can catalyze the oxidation of squalene to (S)-2,3-epoxyquinene, which is the rate-limiting enzyme in steroid synthesis [42]. Hmgcr is the rate-limiting enzyme gene in cholesterol synthesis and non-sterol isoprene synthesis [43]. These results suggest that a low concentration of NET may affect steroid synthesis by affecting the expression of steroid related genes in marine medaka.
Development of nanoemulsion gel based formulation of terbinafine for the synergistic antifungal activity: Dermatokinetic experiment for investigation of epidermal terbinafine deposition enhancement
Published in Inorganic and Nano-Metal Chemistry, 2021
Prabhu Raut, Shobhit Kumar, Babar Iqbal, Javed Ali, Sanjula Baboota
Terbinafine is an antifungal agent and it belongs to allylamine class. It shows antifungal activity by selectively inhibiting squalene epoxidase.[4] Terbinafine is commercially available as ointment, cream, and lotion. However, experiments carried out on ointment and cream have reported local side effects and limited penetrability hence defeating optimum topical drug delivery to the target site. In addition, terbinafine exhibits formulation-related issues of limited solubility. Therefore, it is highly challenging to overcome low penetration rate of terbinafine hydrochloride through the skin. Several lipid based formulations such as nanoemulsion, microemulsion, nanostructured lipid carrier (NLC), etc. have been used to enhance epidermal deposition of terbinafine hydrochloride. Karri and associates developed nanoemulsion gel for topical treatment of fungal infection.[3] Barot and associates formulated and optimized microemulsion based gel for the treatment of onycomycosis.[4] But to the best of our knowledge nanoemulsion of terbinafine hydrochloride using tea tree oil has not been investigated.