| Autor: |
Stecanella, Luciano Aparecido, Taveira, Stephânia Fleury, Marreto, Ricardo Neves, Valadares, Marize C., Vieira, Marcelo de Sousa, Kato, Massuo Jorge, Lima, Eliana Martins |
| Zdroj: |
Revista Brasileira de Farmacognosia; January-February 2013, Vol. 23 Issue: 1 p153-159, 7p |
| Abstrakt: |
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 vivoinvestigations are challenged by the difficulties 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 efi cacy of grandisin as an antitumoral drug, with high drug loading and efi ciency, prolonged drug release and increased physical-chemical stability. Mean diameter of the nanocapsules was lower than 200 nm, with very low polydispersity. Encapsulation efi ciency was above 90%. A sustained in vitrodrug release was achieved for up to twenty days and cytotoxicity was markedly increased (IC50 for grandisin-NC and grandisin were 0.005μM and 0.078μM, respectively), indicating that polymeric nanocapsules are a potential drug delivery system for grandisin allowing the preparation of formulations viable for further in vivostudies. |
| Databáze: |
Supplemental Index |
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