Lipid-based nanoformulations of trifluralin analogs in the management of

To improve the potential of trifluralin (TFL) in the management of infections through the synthesis of analogs (TFLA) and incorporation in nanoparticulate drug delivery systems (NanoDDS), liposomes and solid lipid nanoparticles, for selective targeting to infection sites. screening of 18 TFLA was pe...

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Bibliographic Details
Published in:Nanomedicine (London, England) England), 2016-01, Vol.11 (2), p.153-170
Main Authors: Lopes, Rui M, Pereira, Joana, Esteves, M Alexandra, Gaspar, M Manuela, Carvalheiro, Manuela, Eleutério, Carla V, Gonçalves, Lídia, Jiménez-Ruiz, António, Almeida, António J, Cruz, M Eugénia M
Format: Article
Language:English
Subjects:
activity
dinitroanilines
drug delivery
drug development
leishmaniasis
liposomes
solid lipid nanoparticles
trifluralin
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Summary:To improve the potential of trifluralin (TFL) in the management of infections through the synthesis of analogs (TFLA) and incorporation in nanoparticulate drug delivery systems (NanoDDS), liposomes and solid lipid nanoparticles, for selective targeting to infection sites. screening of 18 TFLA was performed by flow cytometry. NanoDDS were loaded with active TFLA and evaluated for antileishmanial efficacy in mice through determination of parasite burden in liver and spleen. The testing revealed the most active and nontoxic TFLAs, which were selected for the studies based on high incorporation in liposomes and lipid nanoparticles (>90%). Selected TFLA nanoformulations showed superior antileishmanial activity in mice (parasite burden >80%), over free TFLA and Glucantime. The modification of TFL structure to obtain active TFLA, together with their incorporation in NanoDDS, improved their performance against infection.
ISSN:1743-5889
1748-6963
DOI:10.2217/nnm.15.190