title: Development of praziquantel-loaded PLGA nanoparticles and evaluation of intestinal permeation by the everted gut sac model.
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.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, UNESP, Rod. Araraquara-Jaú km 1, CEP 14802-902, Araraquara, SP, Brazil.
authors.forename: Rubiana Mara
authors.initials: RM
authors.lastname: Mainardes
authors.forename: Marco Vinícius
authors.initials: MV
authors.lastname: Chaud
authors.forename: Maria Palmira Daflon
authors.initials: MP
authors.lastname: Gremião
authors.forename: Raul Cesar
authors.initials: RC
authors.lastname: Evangelista
mesh_terms: D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry*; D066298:In Vitro Techniques; D007408:Intestinal Absorption / Q000502:physiology*; D007413:Intestinal Mucosa / Q000378:metabolism; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure*; D010316:Particle Size; D010539:Permeability; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry*; D011223:Praziquantel / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats
chemical_list: D000871:Anthelmintics; D004337:Drug Carriers; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011223:Praziquantel