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dc.contributor.author
Imperiale, Julieta Celeste  
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Nejamkin, Pablo  
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del Sole, Maria Jose  
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Lanusse, Carlos Edmundo  
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Sosnik, Alejandro Dario  
dc.date.available
2018-03-06T20:07:47Z  
dc.date.issued
2015-01  
dc.identifier.citation
Imperiale, Julieta Celeste; Nejamkin, Pablo; del Sole, Maria Jose; Lanusse, Carlos Edmundo; Sosnik, Alejandro Dario; Novel protease inhibitor-loaded Nanoparticle-in-Microparticle Delivery System leads to a dramatic improvement of the oral pharmacokinetics in dogs; Elsevier; Biomaterials; 37; 1-2015; 383-394  
dc.identifier.issn
0142-9612  
dc.identifier.uri
http://hdl.handle.net/11336/38054  
dc.description.abstract
With the advent of the Highly Active Antiretroviral Therapy, the morbidity and the mortality associated to HIV have been considerably reduced. However, 35-40 million people bear the infection worldwide. One of the main causes of therapeutic failure is the frequent administration of several antiretrovirals that results in low patient compliance and treatment cessation. In this work, we have developed an innovative Nanoparticle-in-Microparticle Delivery System (NiMDS) comprised of pure drug nanocrystals of the potent protease inhibitor indinavir free base (used as poorly water-soluble model protease inhibitor) produced by nanoprecipitation that were encapsulated within mucoadhesive polymeric microparticles. Pure drug nanoparticles and microparticles were thoroughly characterized by diverse complementary techniques. NiMDSs displayed an encapsulation efficiency of approximately 100% and a drug loading capacity of up to 43%w/w. In addition, mucoadhesiveness assays exvivo conducted with bovine gut showed that film-coated microparticles were retained for more than 6h. Finally, pharmacokinetics studies in mongrel dogs showed a dramatic 47- and 95-fold increase of the drug oral bioavailability and half-life, respectively, with respect to the free unprocessed drug. These results support the outstanding performance of this platform to reduce the dose and the frequency of administration of protease inhibitors, a crucial step to overcome the current patient-incompliant therapy.  
dc.format
application/pdf  
dc.language.iso
eng  
dc.publisher
Elsevier  
dc.rights
info:eu-repo/semantics/openAccess  
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/  
dc.subject
Hiv Infection  
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Protease Inhibitors  
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Indinavir Free Base  
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Pure Drug Nanoparticle-In-Microparticle Delivery System  
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Mucoadhesion  
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Oral Bioavailability  
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Nano-materiales  
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Nanotecnología  
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INGENIERÍAS Y TECNOLOGÍAS  
dc.title
Novel protease inhibitor-loaded Nanoparticle-in-Microparticle Delivery System leads to a dramatic improvement of the oral pharmacokinetics in dogs  
dc.type
info:eu-repo/semantics/article  
dc.type
info:ar-repo/semantics/artículo  
dc.type
info:eu-repo/semantics/publishedVersion  
dc.date.updated
2018-03-02T13:58:12Z  
dc.journal.volume
37  
dc.journal.pagination
383-394  
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Países Bajos  
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Amsterdam  
dc.description.fil
Fil: Imperiale, Julieta Celeste. Universidad de Buenos Aires; Argentina  
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Fil: Nejamkin, Pablo. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina  
dc.description.fil
Fil: del Sole, Maria Jose. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina  
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Fil: Lanusse, Carlos Edmundo. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina  
dc.description.fil
Fil: Sosnik, Alejandro Dario. Technion-Israel Institute of Technology; Israel. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Nanobiotecnología. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Nanobiotecnología; Argentina  
dc.journal.title
Biomaterials  
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.biomaterials.2014.10.026