Therapeutic Activity of a Topical Formulation Containing 8-Hydroxyquinoline for Cutaneous Leishmaniasis

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Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorUniversidade de São Paulo (USP)-
Autor(es): dc.contributorUniversidad Complutense of Madrid-
Autor(es): dc.contributorUniversity of Strathclyde-
Autor(es): dc.contributorSanto André-
Autor(es): dc.creatorde Lima, Sarah Kymberly Santos-
Autor(es): dc.creatorCavallone, Ítalo Novaes-
Autor(es): dc.creatorSerrano, Dolores Remedios-
Autor(es): dc.creatorAnaya, Brayan J.-
Autor(es): dc.creatorLalatsa, Aikaterini-
Autor(es): dc.creatorLaurenti, Márcia Dalastra-
Autor(es): dc.creatorLago, João Henrique Ghilardi-
Autor(es): dc.creatorda Silva Souza, Dalete Christine-
Autor(es): dc.creatorMarinsek, Gabriela Pustiglione-
Autor(es): dc.creatorLopes, Beatriz Soares-
Autor(es): dc.creatorde Britto Mari, Renata-
Autor(es): dc.creatorPassero, Luiz Felipe Domingues-
Data de aceite: dc.date.accessioned2025-08-21T22:45:13Z-
Data de disponibilização: dc.date.available2025-08-21T22:45:13Z-
Data de envio: dc.date.issued2025-04-29-
Data de envio: dc.date.issued2023-10-31-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.3390/pharmaceutics15112602-
Fonte completa do material: dc.identifierhttps://hdl.handle.net/11449/308795-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/308795-
Descrição: dc.descriptionCutaneous leishmaniasis exhibits a wide spectrum of clinical manifestations; however, only a limited number of drugs are available and include Glucantime® and amphotericin B, which induce unacceptable side effects in patients, limiting their use. Thus, there is an urgent demand to develop a treatment for leishmaniasis. Recently, it was demonstrated that 8-hydroxyquinoline (8-HQ) showed significant leishmanicidal effects in vitro and in vivo. Based on that, this work aimed to develop a topical formulation containing 8-HQ and assess its activity in experimental cutaneous leishmaniasis. 8-HQ was formulated using a Beeler base at 1 and 2% and showed an emulsion size with a D50 of 25 and 51.3 µm, respectively, with a shear-thinning rheological behaviour. The creams were able to permeate artificial Strat-M membranes and excised porcine skin without causing any morphological changes in the porcine skin or murine skin tested. In BALB/c mice infected with L. (L.) amazonensis, topical treatment with creams containing 1 or 2% of 8-HQ was found to reduce the parasite burden and lesion size compared to infected controls with comparable efficacy to Glucantime® (50 mg/kg) administered at the site of the cutaneous lesion. In the histological section of the skin from infected controls, a diffuse inflammatory infiltrate with many heavily infected macrophages that were associated with areas of necrosis was observed. On the other hand, animals treated with both creams showed only moderate inflammatory infiltrate, characterised by few infected macrophages, while tissue necrosis was not observed. These histological characteristics in topically treated animals were associated with an increase in the amount of IFN-γ and a reduction in IL-4 levels. The topical use of 8-HQ was active in decreasing tissue parasitism and should therefore be considered an interesting alternative directed to the treatment of leishmaniasis, considering that this type of treatment is non-invasive, painless, and, importantly, does not require hospitalisation, improving patient compliance by allowing the treatment to be conducted.-
Descrição: dc.descriptionInstitute of Biosciences São Paulo State University (UNESP), Praça Infante Dom Henrique, s/n, SP-
Descrição: dc.descriptionLaboratory of Pathology of Infectious Diseases (LIM50) Department of Pathology Medical School São Paulo University, SP-
Descrição: dc.descriptionDepartment of Pharmaceutics and Food Science Faculty of Pharmacy Universidad Complutense of Madrid, Plaza Ramon y Cajal s/n-
Descrição: dc.descriptionCRUK Formulation Unit Institute of Pharmacy and Biomedical Sciences University of Strathclyde, 161 Cathedral Street-
Descrição: dc.descriptionCenter for Natural and Human Science (CCNH) Federal University of ABC Santo André, SP-
Descrição: dc.descriptionInstitute for Advanced Studies of Ocean São Paulo State University (UNESP), Rua João Francisco Bensdorp, 1178, SP-
Descrição: dc.descriptionInstitute of Biosciences São Paulo State University (UNESP), Praça Infante Dom Henrique, s/n, SP-
Descrição: dc.descriptionInstitute for Advanced Studies of Ocean São Paulo State University (UNESP), Rua João Francisco Bensdorp, 1178, SP-
Idioma: dc.languageen-
Relação: dc.relationPharmaceutics-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subject8-hydroxyquinoline-
Palavras-chave: dc.subjectcutaneous leishmaniasis-
Palavras-chave: dc.subjectL. (L.) amazonensis-
Palavras-chave: dc.subjectquinolines-
Palavras-chave: dc.subjecttopical treatment-
Título: dc.titleTherapeutic Activity of a Topical Formulation Containing 8-Hydroxyquinoline for Cutaneous Leishmaniasis-
Tipo de arquivo: dc.typelivro digital-
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