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000844248 1001_ $$0P:(DE-HGF)0$$aLucio, David$$b0$$eCorresponding author
000844248 245__ $$aCoencapsulation of cyclodextrins into poly(anhydride) nanoparticles to improve the oral administration of glibenclamide. A screening on C. elegans
000844248 260__ $$aAmsterdam [u.a.]$$bElsevier Science$$c2018
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000844248 520__ $$aThis work describes the feasibility of poly(anhydride) nanoparticles as carriers for the oral administration of glibenclamide (GB) as well as the in vivo evaluation of their hypolipidemic effect in a C. elegans model. For this purpose, and in order to increase the GB payload, the drug was encapsulated in nanoparticles in presence of cyclodextrins (either βCD or HPβCD). The optimized nanoparticles displayed a size of about 220 nm and a negative zeta potential (−40 mV), with a drug loading up to 52 μg/mg. Small-angle neutron scattering studies suggested an internal fractal-like structure, based on the repetition of spherical blocks of polymeric units (about 5 nm) grouped to form the nanoparticle. X-ray diffraction study confirmed the absence of crystalline GB molecules due to its dispersion into the nanoparticles, either entrapped in the polymer chains and/or included into cyclodextrin cavities. GB-loaded nanoparticles induced a significant reduction in the fat content of C. elegans. This hypolipidemic effect was slightly higher for the nanoparticles prepared with coencapsulated HPβCD (8.2%) than for those prepared with βCD (7.9%) or in the absence of cyclodextrins (7.0%). In summary, the coencapsulation of cyclodextrins into poly(anhydride) nanoparticles could be an interesting strategy to develop new oral formulations of glibenclamide.
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000844248 7001_ $$0P:(DE-HGF)0$$aMartínez-Ohárriz, María Cristina$$b1
000844248 7001_ $$0P:(DE-HGF)0$$aGonzález-Navarro, Carlos J.$$b2
000844248 7001_ $$0P:(DE-HGF)0$$aNavarro-Herrera, David$$b3
000844248 7001_ $$0P:(DE-HGF)0$$aGonzález-Gaitano, Gustavo$$b4
000844248 7001_ $$0P:(DE-Juel1)130905$$aRadulescu, Aurel$$b5
000844248 7001_ $$0P:(DE-HGF)0$$aIrache, Juan M.$$b6
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