Nanopartículas lipídicas sólidas contendo genisteína para uso tópico
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Data
2012-02-28
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Universidade Federal de Goiás
Resumo
Genistein (GEN), isoflavone contained in soybeans, shows activity against a
large number of cancers, including skin cancer. However, to be used topically it is
essential the association of GEN in an appropriate formulation. The aim of this study
was the development and characterization of solid lipid nanoparticles (SLN) contends
genistein for topical application. A bioanalytical method was developed and validated
for GEN quantification in skin layers with High Performance Liquid Chromatographer
(HPLC) with UV detection. The SLN was obtained with glyceryl behenate,
polysorbate 80, sorbitan trioleate and different amounts of cetylpyridinium chloride
(CPC) (0.5 - 0.05%). The characteristics in terms of particle size, size distribution,
zeta potential, entrapment efficiency and drug recovery were evaluated. In vitro
release, passive and iontophoretic, skin permeation studies were performed.
Cytotoxicity studies were carried out in melanoma cells (B16F10) with free drug and
SLN with and without GEN. The analytical method was linear in the concentration
range of 0.1 to 60 mg/mL. Limit of quantification was 100 ng/mL for both skin
layers. Recovery of the drug ranged from 95.57 to 97.57%. The method was able to
analyze the GEN without suffering interference from endogenous skin
components. SLN loaded with GEN showed positive surface (+ 23 mV) and average
size of 343 nm. Particles were obtained with high entrapment efficiency (93%) and
drug load was 5.45%. In vitro release studies demonstrated that the release of GEN
from SLN occurs in two stages with a large amount of drug released within the first
six hours, followed by a slow release of the remaining drug in the lipid matrix of SLN
in the following hours. When administered in the skin, during in vitro passive
permeation studies, the SLN increased retention of GEN in stratum corneum and
remaining skin compared with free GEN. After iontophoresis application in
formulation of SLN containing GEN thirteen times more GEN was retained on stratum
corneum and three times more drug was retained on remaining skin. In cellular
cytotoxicity studies SLN favored the increase of interaction of drug with the cells and
the cytotoxicity was concentration-dependent. Thus, GEN loaded SLN increased drug
skin permeation and retention and shows to be a potential formulation for topical
application.
Descrição
Citação
SILVA, Lorena Maione. Nanopartículas lipídicas sólidas contendo genisteína para uso tópico. 2012. 37 f. Dissertação (Mestrado em Ciências Farmacêuticas (FF)) - Universidade Federal de Goiás, Goiânia, 2012.