Research and reports in tropical medicine · 2026
Enhanced Topical Treatment of Cutaneous Leishmaniasis Using Niosomal Gel of Tioxolone-Benzoxonium Chloride: In silico, in vitro, and in vivo Evaluation.
СтатьяНазвание и аннотация: Перевод в очереди
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Hakimi Parizi Maryam, Sharifi Iraj, Molaakbari Elaheh, Salarkia Ehsan, Mostafavi Mahshid, Daie Parizi Mohammad Hossein, Pardakhty Abbas, Khamesipour Ali, Ghaffari Daryoush
Аннотация
BACKGROUND: Cutaneous leishmaniasis (CL) is a neglected tropical disease that poses significant therapeutic challenges owing to its toxicity and low compliance with existing treatments. In this study, we formulated and evaluated niosomal gels containing tioxolone (NT), benzoxonium chloride (NB), and their combination (NTB) for topical application against CL.
METHODS: Various in silico methods, including homology modeling and molecular docking, were used to assess pharmacological potential. In vitro anti-leishmanial activity was tested against Leishmania major promastigotes and amastigotes, whereas in vivo efficacy was evaluated in a BALB/c mouse model.
RESULTS: Docking studies showed strong interactions between NT, NB, and NTB and the target proteins. The ADMET analysis indicated that NTB had favorable aqueous solubility (LogS = -3.71) and low toxicity (2.88 mol/kg). In vitro, NTB demonstrated the lowest IC5 0 values (79.0±3.2 μg/mL for promastigotes and 44.4±0.8 μg/mL for amastigotes) against both parasite forms and the highest selectivity index (9.8), outperforming the standard drug meglumine antimoniate (MA). In vivo tests revealed that NTB significantly reduced lesion size and splenic parasite burden compared with placebo, drug-blank niosome, and MA (p < 0.05).
CONCLUSION: Overall, these findings suggest that the NTB formulation exhibits enhanced pharmacological properties and effective antileishmanial activity, indicating the potential for further clinical research.
METHODS: Various in silico methods, including homology modeling and molecular docking, were used to assess pharmacological potential. In vitro anti-leishmanial activity was tested against Leishmania major promastigotes and amastigotes, whereas in vivo efficacy was evaluated in a BALB/c mouse model.
RESULTS: Docking studies showed strong interactions between NT, NB, and NTB and the target proteins. The ADMET analysis indicated that NTB had favorable aqueous solubility (LogS = -3.71) and low toxicity (2.88 mol/kg). In vitro, NTB demonstrated the lowest IC5 0 values (79.0±3.2 μg/mL for promastigotes and 44.4±0.8 μg/mL for amastigotes) against both parasite forms and the highest selectivity index (9.8), outperforming the standard drug meglumine antimoniate (MA). In vivo tests revealed that NTB significantly reduced lesion size and splenic parasite burden compared with placebo, drug-blank niosome, and MA (p < 0.05).
CONCLUSION: Overall, these findings suggest that the NTB formulation exhibits enhanced pharmacological properties and effective antileishmanial activity, indicating the potential for further clinical research.