Development and characterization of PLGA nanocapsules of grandisin isolated from Virola surinamensis: in vitro release and cytotoxicity studies
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2013-02
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Resumo
The most studied phyto constituent isolated from Virola surinamensis
(Rol. ex Rottb.) Warb., Myristicaceae, is the tetrahydrofuran neolignan grandisin,
which exhibits a series of biological activities, including trypanocidal, larvicidal and
antitumoral. Due to its extremely low solubility, additional studies, including in vivo
investigations are challenged by the diffi culties in the development of an effective
drug delivery system for grandisin. The encapsulation in polymeric nanoparticles is
a very attractive alternative for overcoming some of these limitations. In this work,
PLGA nanocapsules loaded with grandisin were developed in an attempt to optimize
the effi cacy of grandisin as an antitumoral drug, with high drug loading and effi ciency,
prolonged drug release and increased physical-chemical stability. Mean diameter of
the nanocapsules was lower than 200 nm, with very low polydispersity. Encapsulation
effi ciency was above 90%. A sustained in vitro drug release was achieved for up to
twenty days and cytotoxicity was markedly increased (IC50 for grandisin-NC and
grandisin were 0.005 μM and 0.078 μM, respectively), indicating that polymeric
nanocapsules are a potential drug delivery system for grandisin allowing the preparation
of formulations viable for further in vivo studies.
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Cytotoxicity, Grandisin, PLGA nanocapsules, Sustained release
Citação
STECANELLA, Luciano Aparecido et al. Development and characterization of PLGA nanocapsules of grandisinisolatedfrom Virolasurinamensis: in vitro release and cytotoxicity studies. Revista Brasileira de Farmacognosia, Curitiba, v. 23, n. 1, p. 153-159, 2012.