التفاصيل البيبلوغرافية
| العنوان: |
Oral Efficacy of a Diselenide Compound Loaded in Nanostructured Lipid Carriers in a Murine Model of Visceral Leishmaniasis |
| المؤلفون: |
Mikel Etxebeste-Mitxeltorena (8693244), Esther Moreno (8693250), Manuela Carvalheiro (11690240), Alba Calvo (11690243), Iñigo Navarro-Blasco (11690246), Elena González-Peñas (11690249), José I. Álvarez-Galindo (11690252), Daniel Plano (1443595), Juan M. Irache (2803504), Antonio J. Almeida (11500927), Carmen Sanmartín (4972318), Socorro Espuelas (8693247) |
| سنة النشر: |
2021 |
| المجموعة: |
Smithsonian Institution: Digital Repository |
| مصطلحات موضوعية: |
Biochemistry, Medicine, Pharmacology, Biotechnology, Cancer, Infectious Diseases, Environmental Sciences not elsewhere classified, Biological Sciences not elsewhere classified, Chemical Sciences not elsewhere classified, nanostructured lipid carriers, drug discovery pipeline, class iv compounds, biopharmaceutical classification system, poor aqueous solubility, demonstrating similar efficacy, nlc drastically enhanced, 2m , diselenide compound loaded, poor resources, oral efficacy, visceral leishmaniasis, trypanothione reductase, parasite burden, oral treatment, oral administration, murine model, least 95, intravenous fungizone, infected balb, infantum -< |
| الوصف: |
Leishmaniasis urgently needs new oral treatments, as it is one of the most important neglected tropical diseases that affects people with poor resources. The drug discovery pipeline for oral administration currently discards entities with poor aqueous solubility and permeability (class IV compounds in the Biopharmaceutical Classification System, BCS) such as the diselenide 2m , a trypanothione reductase (TR) inhibitor. This work was assisted by glyceryl palmitostearate and diethylene glycol monoethyl ether-based nanostructured lipid carriers (NLC) to render 2m bioavailable and effective after its oral administration. The loading of 2m in NLC drastically enhanced its intestinal permeability and provided plasmatic levels higher than its effective concentration (IC 50 ). In L. infantum- infected BALB/c mice, 2m -NLC reduced the parasite burden in the spleen, liver, and bone marrow by at least 95% after 5 doses, demonstrating similar efficacy as intravenous Fungizone. Overall, compound 2m and its formulation merit further investigation as an oral treatment for visceral leishmaniasis. |
| نوع الوثيقة: |
article in journal/newspaper |
| اللغة: |
unknown |
| العلاقة: |
https://figshare.com/articles/journal_contribution/Oral_Efficacy_of_a_Diselenide_Compound_Loaded_in_Nanostructured_Lipid_Carriers_in_a_Murine_Model_of_Visceral_Leishmaniasis/17003045Test |
| DOI: |
10.1021/acsinfecdis.1c00394.s001 |
| الإتاحة: |
https://doi.org/10.1021/acsinfecdis.1c00394.s001Test |
| حقوق: |
CC BY-NC 4.0 |
| رقم الانضمام: |
edsbas.6F0422AD |
| قاعدة البيانات: |
BASE |
