Purpose. The aim of this work was the formulation and characterization of new kynurenic acid (KA) loaded polymeric nanoparticles (NP) destined to a brain targeting purpose. Methods. Several batches of KA loaded poly(lactide-co-glycolide) (PLGA) NP were prepared by two different new methods. The first uses direct injection of a solution of N-methyl pyrrolidone into a solution of 1% tween 80 or PVA. The second consisted in injecting a solution of N-methyl pyrrolidone-acetone into a 1% PVA solution upon combined homogenisation/sonication. The MS were characterized in terms of size, morphology, drug content. Spectrophotometry, HPLC, TEM, and photocorrelation spectroscopy were employed. Particle size, polydispersity index (P.I.), and zeta potential were taken as indicators of formulation quality. Results. KA was successfully entrapped in PLGA NP (4-5% content). The NP obtained by using the first method had size was about 170 nm with tween 80 and 250 nm with PVA and resulted mainly spherical. In addition, P.I. was 0.179 and 0.352 respectively. Zeta potential resulted higher with tween 80 (15 mV) and lowered by PVA (-0.4 mV) indicating a possible attitude to aggregation. The second method provided mean diameters around 290-300 nm, P.I. between 0.107 and 0.072 and zeta potential of 23.3 mV. Conclusions. KA loaded PLGA NP size were suitable for a possible drug targeting application. Although a further characterization and formulation assessment is needed the NP prepared using the homogenisation/sonication combined method showed a fairly good dispersion and stability.
New kynurenic acid containing polymeric nanoparticles for brain targeting
GIOVAGNOLI, Stefano;BLASI, PAOLO;SCHOUBBEN, Aurelie Marie Madeleine;RICCI, Maurizio;ROSSI, Carlo
2007
Abstract
Purpose. The aim of this work was the formulation and characterization of new kynurenic acid (KA) loaded polymeric nanoparticles (NP) destined to a brain targeting purpose. Methods. Several batches of KA loaded poly(lactide-co-glycolide) (PLGA) NP were prepared by two different new methods. The first uses direct injection of a solution of N-methyl pyrrolidone into a solution of 1% tween 80 or PVA. The second consisted in injecting a solution of N-methyl pyrrolidone-acetone into a 1% PVA solution upon combined homogenisation/sonication. The MS were characterized in terms of size, morphology, drug content. Spectrophotometry, HPLC, TEM, and photocorrelation spectroscopy were employed. Particle size, polydispersity index (P.I.), and zeta potential were taken as indicators of formulation quality. Results. KA was successfully entrapped in PLGA NP (4-5% content). The NP obtained by using the first method had size was about 170 nm with tween 80 and 250 nm with PVA and resulted mainly spherical. In addition, P.I. was 0.179 and 0.352 respectively. Zeta potential resulted higher with tween 80 (15 mV) and lowered by PVA (-0.4 mV) indicating a possible attitude to aggregation. The second method provided mean diameters around 290-300 nm, P.I. between 0.107 and 0.072 and zeta potential of 23.3 mV. Conclusions. KA loaded PLGA NP size were suitable for a possible drug targeting application. Although a further characterization and formulation assessment is needed the NP prepared using the homogenisation/sonication combined method showed a fairly good dispersion and stability.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
