Preparation of surface multiple-coated polylactide acid drug-loaded nanoparticles for intranasal delivery and evaluation on its brain-targeting efficiency.
OBJECTIVE
To prepare a mixture of multiple-coated aniracetam nasal polylactic-acid nanoparticles (M-C-PLA-NP) and evaluate its stability preliminarily in vitro and its brain-targeting efficiency in vivo.


METHODS
The solvent diffusion-evaporation combined with magnetic stirring method has been chosen for the entrapment of aniracetam. The M-C-PLA-NP was characterized with respect to its morphology, particle size, size distribution and aniracetam entrapment efficiency. The in vivo distribution was studied in male SD rats after an intranasal administration.


RESULTS
In vitro release of M-C-PLA-NP showed two components with an initial rapid release due to the surface-associated drug and followed by a slower exponential release of aniracetam, which was dissolved in the core. The AUC0 → 30 min of M-C-PLA-NP in brain tissues resulted in a 5.19-fold increase compared with aniracetam solution. The ratios of AUC in brain to that in other tissues obtained after nasal application of M-C-PLA-NP were significantly higher than those of aniracetam solution.


CONCLUSIONS
Therefore, it can be concluded that M-C-PLA-NP demonstrated its potential on increasing the brain-targeting efficiency of drugs and will be used as novel brain-targeting agent for nasal drug delivery.
a College of Pharmacy , Chengdu University of Traditional Chinese Medicine , Chengdu , Sichuan , China .
Junjie
J
Bian
b Institute of Pharmacy , Sichuan Academy of Chinese Medicine Sciences , Chengdu , Sichuan , China , and.
Zhixiang
Z
Yuan
a College of Pharmacy , Chengdu University of Traditional Chinese Medicine , Chengdu , Sichuan , China .
Xiaoliang
X
Chen
a College of Pharmacy , Chengdu University of Traditional Chinese Medicine , Chengdu , Sichuan , China .
Yuan
Y
Gao
b Institute of Pharmacy , Sichuan Academy of Chinese Medicine Sciences , Chengdu , Sichuan , China , and.
Chaoqun
C
Xu
c Sichuan Academy of Medical Sciences, Sichuan Provincial People's Hospital , Chengdu , Sichuan , China.
Jianyou
J
Shi
D000281:Administration, Intranasal; D000818:Animals; D019540:Area Under Curve; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D016503:Drug Delivery Systems; D053758:Nanoparticles; D018697:Nootropic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011760:Pyrrolidinones / Q000008:administration & dosage / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley
D018697:Nootropic Agents; D011091:Polyesters; D011760:Pyrrolidinones; C033616:poly(lactide); C036466:aniracetam
Aniracetam; brain-targeting; intranasal delivery; surface multiple-coated nanoparticles