Desenvolvimento, caracterização e avaliação da permeação cutânea da isoflavona genisteína em nanocápsulas poliméricas
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Data
2009-12-16
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Universidade Federal de Goiás
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Isoflavones are phytoestrogens that have biological activities such as estrogenic and inhibiting enzymes that regulate the cell cycle, and for topic application it is highlighted antioxidant and anticancer activities. Amongst isoflavones, genistein shows the greatest biological activity, however, its low hydrosolubility damages incorporation in topic vehicles and passive permeation. Therefore, development of
particulated nanocarrier systems, such as nanocapsules, aiming to increase genistein biological activities and make topic administration possible, became this work s objective. To do so, PLA nanocapsules containing genistein were prepared by interfacial polymer deposition method, then characterized, and their 90 days stability was evaluated. Later, free and nanoencapsulated genistein were incorporated into semi-solid formulations (gel and emulsion) and evaluated by in vitro models using classical Franz-type diffusion cells, to measure its ability to modulate swine skin and synthetic membranes penetration. Nanocapsules average diameter was 138,5 nm (DP± 2,95) and PDI found was 0,126 (DP± 0.03). After separation of free genistein, the drug was quantified by HPLC and showed 89,63% (DP±2,27) encapsulation efficiency, followed by loss by leaking to 63,80% (DP±11,26) in 90 days. Permeation tests demonstrated that gel formulation containing nanoencapsulated genistein presented the greatest permeated concentration, and there was significant difference for all tested formulations and similarity only between genistein quantity reminiscent in the dosage form of formulations containing gel and emulsion, as well as drug quantities retained in the skin of gel and emulsion formulations containing genistein. Nanoencapsulated forms kinetic parameters showed the greatest correlation coefficient for kinetic of zero order model, indicating that flow didn t depend on its concentration. Nanoencapsulated genistein concentrations permeation across synthetic and swine skin presented significant difference depending on time. Thus, the study performed showed that the polymeric system developed presents great potential for application as genistein nanocarrier in biological systems
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ZAMPIERI, Ana Lúcia Teixeira de Carvalho. Development, characterization and evaluation of the permeation of isoflavone genistein in polymeric nanocapsules. 2009. 114 f. Tese (Doutorado em Ciencias da Saude) - Universidade Federal de Goiás, Goiânia, 2009.