Efficacy of topical risedronate and risedronate – Eudragit E complex in a model of cutaneous leishmaniasis induced by Leishmania (Leishmania) amazonensis
An efficacious topical treatment for cutaneous leishmaniasis (CL) is highly desirable but still an ongoing challenge. Systemic risedronate (Ris) has been reported to have anti-leishmanial properties and Eudragit EPO (EuE) has shown in vitro activity against L. (L.) amazonensis. The aim of this work was to investigate the in vivo efficacy of topical Ris and EuE-Ris complexes on CL. Surface charge and Ris release kinetics from the different dispersions were analyzed. BALB/c mice were infected intradermally with promastigotes of L. (L.) amazonensis. Ulcers were treated with Ris or EuE-Ris hydrogels. All the lesions that received topical Ris or EuE-Ris showed an improvement with respect to control: reduction of ulcer average size, cicatrization, flattened edges and no signs of necrosis. In addition, a marked parasitic inhibition of 69.5 and 73.7% was observed in the groups treated with Ris and EuE-Ris, respectively, with the IgG2a levels indicating a tendency towards cure. The results are promising and the system should now be enhanced to achieve total parasite elimination.
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or continue reading here: Ma. Florencia Peralta, Ma. Laura Guzman, Ma. Estefanía Bracamonte, J. Diego Marco, Ma. Eugenia Olivera, Dolores C. Carrer, Paola A. Barroso, Efficacy of topical risedronate and risedronate – Eudragit E complex in a model of cutaneous leishmaniasis induced by Leishmania (Leishmania) amazonensis, Heliyon, Volume 7, Issue 5,
2021, e07136, ISSN 2405-8440, https://doi.org/10.1016/j.heliyon.2021.e07136. (https://www.sciencedirect.com/science/article/pii/S2405844021012391)
The development of novel chemotherapeutic approaches for CL is of great importance. The use of bisphosphonates is of interest as they have already been used for other clinical indications. Ris produced moderately encouraging results in the treatment of CL caused by L. (L.) amazonensis in an experimental animal model. The EuE-Ris-HPMC complex led to lesion cicatrization and a slightly higher reduction in the parasitic burden. Future work should be aimed at optimizing the concentration, dose frequency, drug or excipient combinations and system characteristics in order to attain total parasite elimination. To the best of our knowledge, this is the first report on the efficacy of bisphosphonates against CL as a topical treatment.