Development of praziquantel-loaded PLGA nanoparticles and evaluation of intestinal permeation by the everted gut sac model |
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Authors: | Mainardes Rubiana Mara Chaud Marco Vinícius Gremião Maria Palmira Daflon Evangelista Raul Cesar |
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Affiliation: | Programa de Pós-Gradua??o em Ciências Farmacêuticas, UNESP, Rod. Araraquara-Jaú km 1, CEP 14802-902, Araraquara, SP, Brazil. |
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Abstract: | Praziquantel has been shown to be highly effective against all known species of Schistosoma infecting humans. Spherical nanoparticles made of poly(D,L-lactide-co-glycolide) acid with controlled size were designed as drug carriers. Praziquantel, a hydrophobic drug, was entrapped into the polymeric nanoparticles with 30% (w/w) of theoretical loading. The nanoparticles size was approximately of 350 nm with 66% of encapsulation efficiency. The everted gut sac model shows to be efficient to evaluate the drug permeation through the intestinal membrane. The results show that free praziquantel presents 4-fold times more permeation than praziquantel-loaded PLGA nanoparticles and physical mixture. For this drug, in special, this result can be interesting, since the nanoparticulate system can behave as a drug reservoir and/or to have a more localized effect in intestinal membrane for a prolonged period of time, since great amounts of parasites can be usually found in the mesenteric veins. |
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