TY  - JOUR
AU  - Lucio, David
AU  - Martínez-Ohárriz, María Cristina
AU  - González-Navarro, Carlos J.
AU  - Navarro-Herrera, David
AU  - González-Gaitano, Gustavo
AU  - Radulescu, Aurel
AU  - Irache, Juan M.
TI  - Coencapsulation of cyclodextrins into poly(anhydride) nanoparticles to improve the oral administration of glibenclamide. A screening on C. elegans
JO  - Colloids and surfaces / B
VL  - 163
SN  - 0927-7765
CY  - Amsterdam [u.a.]
PB  - Elsevier Science
M1  - FZJ-2018-01689
SP  - 64 - 72
PY  - 2018
AB  - This 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.
LB  - PUB:(DE-HGF)16
C6  - pmid:29277019
UR  - <Go to ISI:>//WOS:000427217300008
DO  - DOI:10.1016/j.colsurfb.2017.12.038
UR  - https://juser.fz-juelich.de/record/844248
ER  -