Lipid-based nanoformulations of trifluralin analogs in the management of Leishmania infantum infections

To improve the potential of trifluralin (TFL) in the management of Leishmania infantum infections through the synthesis of analogs (TFLA) and incorporation in nanoparticulate drug delivery systems (NanoDDS), liposomes and solid lipid nanoparticles, for selective targeting to leishmania infection sit...

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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:
Animals
Antiprotozoal Agents - administration & dosage
Antiprotozoal Agents - chemistry
Diffusion
Drug Compounding - methods
Drug delivery systems
Drug dosages
Flow cytometry
Infections
Leishmania infantum - drug effects
Leishmaniasis, Visceral - drug therapy
Leishmaniasis, Visceral - parasitology
Lipids
Liposomes - chemistry
Male
Mice
Mice, Inbred BALB C
Nanocapsules - chemistry
Nanocapsules - ultrastructure
Nanoparticles
Parasites
Parasitic diseases
Particle Size
Pharmaceuticals
Spleen
Treatment Outcome
Trifluralin - administration & dosage
Trifluralin - analogs & derivatives
Tropical diseases
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Summary:To improve the potential of trifluralin (TFL) in the management of Leishmania infantum infections through the synthesis of analogs (TFLA) and incorporation in nanoparticulate drug delivery systems (NanoDDS), liposomes and solid lipid nanoparticles, for selective targeting to leishmania infection sites. In vitro 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 in vitro testing revealed the most active and nontoxic TFLAs, which were selected for the in vivo 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 in vivo performance against L. infantum infection.
ISSN:1743-5889
1748-6963
DOI:10.2217/nnm.15.190