Acta Pharm. 57
(2007) 469-477
Original research paper
Chitosan inserts for periodontitis:
Influence of drug loading, plasticizer and crosslinking
on in vitro metronidazole
release
ROMI
BARAT, ANEGUNDHA SRINATHA, JAYANTA K. PANDIT, SHEMPA ANUPURBA and NEELAM MITTAL
jkpandit@gmail.com
1 Departments
of Pharmaceutics, Institute of Technology, Banaras
Hindu University, Varanasi-221005
2 Department
of Microbiology, Institute of Medical Sciences, Banaras
Hindu University, Varanasi-221005
3 Faculty
of Dental Sciences, Institute of Medical Sciences, Banaras
Hindu University, Varanasi-221005, India
Accepted September 10, 2007
Chitosan based metronidazole (MZ) inserts were fabricated by the casting
method and characterized with respect to mass and thickness uniformity, metronidazole loading and in vitro metronidazole release kinetics. The
fabricated inserts exhibited satisfactory physical characteristics. The mass of
inserts was in the range of 5.63 ± 0.42 to 6.04 ± 0.89 mg. The thickness ranged
from 0.46 ± 0.06 to 0.49 ± 0.08 mm. Metronidazole
loading was in the range of 0.98 ± 0.09 to 1.07 ± 0.07 mg except for batch CM3
with MZ loading of 2.01 ± 0.08 mg. The inserts exhibited an initial burst
release at the end of 24 h, irrespective of the drug to polymer ratio,
plasticizer content or cross-linking. However, further drug release was
sustained over the next 6 days. Cross-linking with 10% (m/m) of glutaraldehyde inhibited the
burst release by ~30% and increased the mean dissolution time (MDT) from 0.67
to 8.59 days. The decrease in drug release was a result of reduced permeability
of chitosan due to cross-linking.
Keywords: chitosan
inserts, cross-linking, metronidazole, periodontitis, sustained release