Acta Pharm. 66 (2016) 555-562
Short communication
Preparation and in vivo evaluation of
gel-based nasal delivery system for risperidone
FUGEN
GU, WEINA MA, GENDALAI MENG, CHUNZHI WU and YI WANG
1 Department of Pharmaceutics, Affiliated
Hospital, Inner Mongolia Medical University, Hohhot 010050, China
2
School of Pharmacy, Inner Mongolia Medical
University, Hohhot 010110, China
Accepted August 3, 2016
Published online September
6, 2016
The aim of this study was
to prepare a nasal gel of risperidone and to
investigate the pharmacokinetics and relative bioavailability of the drug in
rats. Compared with oral dosing, the risperidone
nasal gel exhibited very fast absorption and high bioavailability. Maximal
plasma concentration (cmax ) and the
time to reach cmax
(tmax)
were 15.2 µg mL–1 and 5min for the nasal gel, 3.6 µg mL–1and
30 min for the oral drug suspension, respectively. Pharmacokinetic parameters
such as tmax,
cmax
and AUC between oral and nasal routes
were significantly different (p ＜
0.01). Relative bioavailability of the drug nasal preparation
to the oral suspension was up to 1600.0%. Further, the in vitro effect of the risperidone nasal
gel on nasal mucociliary movement was also investigated
using a toad palate model. The risperidone nasal
formulation showed mild ciliotoxicity, but the
adverse effect was temporary and reversible.
Keywords: risperidone,
nasal gel, formulation, pharmacokinetics,
bioavailability, ciliotoxicity