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Nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design.

de Mattos CB, Argenta DF, Melchiades Gde L, Cordeiro MN, Tonini ML, Moraes MH, Weber TB, Roman SS, Nunes RJ, Teixeira HF, Steindel M, Koester LS - Int J Nanomedicine (2015)

Bottom Line: Nanoemulsions are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect.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.

View Article: PubMed Central - PubMed

Affiliation: Faculdade de Farmácia, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil.

ABSTRACT
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.

No MeSH data available.


Related in: MedlinePlus

Pareto chart (A) and interaction graphs (B) to physicochemical characteristics.Notes: A: lipophilic surfactant; B: hydrophilic surfactant. Continuous line: sorbitan monooleate (−1); dotted line: soybean lecithin (+1).Abbreviation: PDI, polydispersity index.
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f2-ijn-10-5529: Pareto chart (A) and interaction graphs (B) to physicochemical characteristics.Notes: A: lipophilic surfactant; B: hydrophilic surfactant. Continuous line: sorbitan monooleate (−1); dotted line: soybean lecithin (+1).Abbreviation: PDI, polydispersity index.

Mentions: The Pareto chart (a) and interaction graphs (b) are shown in Figure 2. The variable A (lipophilic surfactant) presents a significant influence (P<0.05) on droplet size, PDI, zeta potential, viscosity, and pH, with a favorable effect on all parameters. This effect was observed when the lipophilic surfactant was present at its high level (soybean lecithin), resulting in nanoemulsions with smaller particle size, low PDI, higher zeta potential in module, and viscosity. The interactions between factors A and B present a significant influence only on droplet size. As can be observed in the interaction graphs, droplet sizes are reduced when both factors are at high level, that is, when soybean lecithin and polysorbate 20 are employed in the same formulation. The variable B (hydrophilic surfactant) did not influence nanoemulsions characteristics significantly. These findings suggest that the molecular geometry of the surfactants did not affect the properties of nanoemulsions, contrarily to what has been described in previous studies.31


Nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design.

de Mattos CB, Argenta DF, Melchiades Gde L, Cordeiro MN, Tonini ML, Moraes MH, Weber TB, Roman SS, Nunes RJ, Teixeira HF, Steindel M, Koester LS - Int J Nanomedicine (2015)

Pareto chart (A) and interaction graphs (B) to physicochemical characteristics.Notes: A: lipophilic surfactant; B: hydrophilic surfactant. Continuous line: sorbitan monooleate (−1); dotted line: soybean lecithin (+1).Abbreviation: PDI, polydispersity index.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4562752&req=5

f2-ijn-10-5529: Pareto chart (A) and interaction graphs (B) to physicochemical characteristics.Notes: A: lipophilic surfactant; B: hydrophilic surfactant. Continuous line: sorbitan monooleate (−1); dotted line: soybean lecithin (+1).Abbreviation: PDI, polydispersity index.
Mentions: The Pareto chart (a) and interaction graphs (b) are shown in Figure 2. The variable A (lipophilic surfactant) presents a significant influence (P<0.05) on droplet size, PDI, zeta potential, viscosity, and pH, with a favorable effect on all parameters. This effect was observed when the lipophilic surfactant was present at its high level (soybean lecithin), resulting in nanoemulsions with smaller particle size, low PDI, higher zeta potential in module, and viscosity. The interactions between factors A and B present a significant influence only on droplet size. As can be observed in the interaction graphs, droplet sizes are reduced when both factors are at high level, that is, when soybean lecithin and polysorbate 20 are employed in the same formulation. The variable B (hydrophilic surfactant) did not influence nanoemulsions characteristics significantly. These findings suggest that the molecular geometry of the surfactants did not affect the properties of nanoemulsions, contrarily to what has been described in previous studies.31

Bottom Line: Nanoemulsions are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect.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.

View Article: PubMed Central - PubMed

Affiliation: Faculdade de Farmácia, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil.

ABSTRACT
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.

No MeSH data available.


Related in: MedlinePlus