| Author | Santos, Quesia Nery dos | |
| Author | Teles, Daiane Caroline Santos | |
| Author | Araujo, Guilherme Rodolfo Souza de | |
| Author | Lima, Odeanny Vitória Azevedo | |
| Author | Silva, Luiz André Santos | |
| Author | Carvalho, Rita de Cássia Viana de | |
| Author | Sousa, Valéria Carlos de | |
| Author | Matos, Saulo Santos | |
| Author | Costa, Amanda Mendonça Barros | |
| Author | Andrade Neto, Valter Viana de | |
| Author | Santos, Eduardo Caio Torres dos | |
| Author | Araujo, Adriano Antunes de Souza | |
| Author | Sarmento, Victor Hugo Vitorino | |
| Author | Carvalho, Fernando Aécio de Amorim | |
| Author | Nunes, Rogéria de Souza | |
| Author | Lira, Ana Amélia Moreira | |
| Access date | 2024-08-06T12:42:13Z | |
| Available date | 2024-08-06T12:42:13Z | |
| Document date | 2024 | |
| Citation | SANTOS, Quesia Nery dos et al. Microemulsions strongly promoted the activity of α-bisabolol against different Leishmania species and its skin permeation. Experimental Parasitology, v. 265, p. 1-10, Oct. 2024. | |
| ISSN | 0014-4894 | |
| URI | https://www.arca.fiocruz.br/handle/icict/65262 | |
| Description | Produção científica do Laboratório de Bioquímica de Tripanossomatídeos. | pt_BR |
| Sponsorship | We thank the Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq, Brazil) for funding (grant number 405142/2021–8). | |
| Sponsorship | Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES, Brazil) for the scholarship. | |
| Language | eng | en_US |
| Publisher | Elsevier | |
| Rights | restricted access | |
| Title | Microemulsions strongly promoted the activity of α-bisabolol against different Leishmania species and its skin permeation | en_US |
| Type | Article | |
| DOI | 10.1016/j.exppara.2024.108808 | |
| Abstract | This study aimed to develop microemulsions (MEs) containing α-bisabolol for the topical treatment of cutaneous leishmaniasis (CL). Initially, pseudoternary phase diagrams were developed using α-bisabolol as the oil phase, Eumulgin® CO 40 as the surfactant, Polymol® HE as the co-surfactant, and distilled water as the aqueous phase. Two transparent liquid systems (TLS) containing 5% of α-bisabolol were selected and characterized (F5E25 and F5EP25). Next, skin permeation and retention assays were performed using Franz cells. The interaction of the formulation with the stratum corneum (SC) was evaluated using the FTIR technique. The cytotoxicity was evaluated in murine peritoneal macrophages. Finally, the antileishmanial activity of microemulsions was determined in promastigotes and amastigotes of L. amazonensis (strain MHOM/BR/77/LTB 0016). As a result, the selected formulations showed isotropy, nanometric size (below 25 nm), Newtonian behavior and pH ranging from 6.5 to 6.9. The MEs achieved a 2.5-fold increase in the flux and skin-permeated amount of α-bisabolol. ATR-FTIR results showed that microemulsions promoted fluidization and extraction of lipids and proteins of the stratum corneum, increasing the diffusion coefficient and partition coefficient of the drug in the skin. Additionally, F5E25 and F5EP25 showed higher activity against promastigotes (IC50 13.27 and 18.29, respectively) compared to unencapsulated α-bisabolol (IC50 53.8). Furthermore, F5E25 and F5EP25 also showed antileishmanial activity against intracellular amastigotes of L. amazonensis, with IC50 50 times lower than free α-bisabolol and high selectivity index (up to 15). Therefore, the systems obtained are favorable to topical administration, with significant antileishmanial activity against L. amazonensis promastigotes and amastigotes, being a promising system for future in vivo trials. | en_US |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Affilliation | Universidade Federal do Piauí. Núcleo de Pesquisa em Plantas Medicinais. Teresina, PI, Brasil. | |
| Affilliation | Universidade Federal do Piauí. Núcleo de Pesquisa em Plantas Medicinais. Teresina, PI, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanossomatídeos. Rio de Janeiro, RJ, Brasil. | |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanossomatídeos. Rio de Janeiro, RJ, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Exatas e Tecnologia. Departamento de Química. Itabaiana, SE, Brasil. | |
| Affilliation | Universidade Federal do Piauí. Núcleo de Pesquisa em Plantas Medicinais. Teresina, PI, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Affilliation | Universidade Federal de Sergipe. Centro de Ciências Biológicas e da Saúde. Departamento de Farmácia. São Cristóvão, SE, Brasil. | |
| Subject | Cutaneous leishmaniasis | en_US |
| Subject | Promastigotes | en_US |
| Subject | Amastigotes | en_US |
| Subject | Microemulsions | en_US |
| Subject | α-bisabolol | en_US |
