Nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design.
Nanoemulsions are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect. Chalcones are compounds of low water solubility that have been described as promising molecules for the treatment of cutaneous leishmaniasis (CL). In this context, the aim of this work was to optimize the development of a nanoemulsion containing a synthetic chalcone for CL treatment using a 2(2) full factorial design. The formulations were prepared by spontaneous emulsification and the experimental design studied the influence of two independent variables (type of surfactant - soybean lecithin or sorbitan monooleate and type of co-surfactants - polysorbate 20 or polysorbate 80) on the physicochemical characteristics of the nanoemulsions, as well as on the skin permeation/retention of the synthetic chalcone in porcine skin. In order to evaluate the stability of the systems, the antileishmanial assay was performed against Leishmania amazonensis 24 hours and 60 days after the preparation of the nanoemulsions. The formulation composed of soybean lecithin and polysorbate 20 presented suitable physicochemical characteristics (droplet size 171.9 nm; polydispersity index 0.14; zeta potential -39.43 mV; pH 5.16; and viscosity 2.00 cP), drug content (91.09%) and the highest retention in dermis (3.03 µg·g(-1)) - the main response of interest - confirmed by confocal microscopy. This formulation also presented better stability of leishmanicidal activity in vitro against L. amazonensis amastigote forms (half maximal inhibitory concentration value 0.32±0.05 µM), which confirmed the potential of the nanoemulsion soybean lecithin and polysorbate 20 for CL treatment.
['de Mattos|Cristiane Bastos|CB|', 'Argenta|Débora Fretes|DF|', 'Melchiades|Gabriela de Lima|Gde L|', 'Cordeiro|Marlon Norberto Sechini|MN|', 'Tonini|Maiko Luis|ML|', 'Moraes|Milene Hoehr|MH|', 'Weber|Tanara Beatriz|TB|', 'Roman|Silvane Souza|SS|', 'Nunes|Ricardo José|RJ|', 'Teixeira|Helder Ferreira|HF|', 'Steindel|Mário|M|', 'Koester|Letícia Scherer|LS|']
D000279:Administration, Cutaneous D000977:Antiparasitic Agents D045744:Cell Line, Tumor D002599:Chalcone D055598:Chemical Phenomena D016503:Drug Delivery Systems D004655:Emulsions D006801:Humans D006863:Hydrogen-Ion Concentration D020128:Inhibitory Concentration 50 D054709:Lecithins D016773:Leishmaniasis, Cutaneous D049329:Nanostructures D010316:Particle Size D011136:Polysorbates D012867:Skin D012995:Solubility D013329:Structure-Activity Relationship D013501:Surface-Active Agents D014783:Viscosity
nanoemulsion chalcone full factorial leishmaniasis skin permeation