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Original Research Article
Development of
Mucoadhesive Nanoparticulate System of Ebastine for
Nasal Drug Delivery
Tashi Chhojom Khom, Hemant
KS Yadav*, Abhay Raizaday, Navya Manne, Hemant S Kumar
and Sankeerth N Kumar
Department of
Pharmaceutics, JSS College of Pharmacy, JSS University,
Mysore, Karnataka –570015, India
*For correspondence:
Email:
haisunny2@yahoo.co.in; Tel:
+91-9886112637; Fax: +9-0821-2548359
Received: 13 May 2013
Revised accepted: 26 April
2014
Tropical
Journal of Pharmaceutical Research, July 2014;
13(7): 1013-1019
http://dx.doi.org/10.4314/tjpr.v13i7.2
Abstract
Purpose: To
prepare and evaluate mucoadhesive nanoparticulate system
of ebastine for nasal drug delivery.
Methods: The
nanoparticles were prepared by ionic gelation method
using drug-chitosan weight ratios 1:1, 1:2 and 1:3, and
incorporating 0.5 or 0.7 % w/v sodium tripolyphosphate (STPP)
and poloxamer 407. The mucoadhesive nanoparticles were
characterized by scanning electron microscope (SEM),
transmission electron microscope (TEM), differential
scanning colorimetry (DSC) and Fourier transform
infrared spectroscopy (FTIR) and evaluated for drug
loading, entrapment efficiency, in vitro mucoadhesion,
in vitro drug release and ex-vivo permeation.
Results:
FTIR and DSC studies indicate that no chemical
interaction occurred between the drug and polymer.
Nanoparticle size ranged from 169 to 500 nm. Drug
loading and entrapment efficiency increased with
increase in chitosan concentration and decreased with
increase in poloxamer 407 concentration. The highest
drug loading obtained for the nanoparticles was 19.5 %.
With increase in polymer (chitosan) concentration (1:1
to 1:3), production yield was unchanged (73.2 to 74.4 %
(F6)). Mucoadhesion increased with increase in the
concentration of chitosan. In vitro drug release from
all the formulations was biphasic, being characterized
by a slight ‘burst’ followed by slow release. At the end
of 8 h F6 (1:3) showed drug release of only 86.9 %,
indicating sustained release. Ex-vivo permeation of pure
ebastine was more rapid than from F6, thus indicating
the capability of chitosan to control drug permeation
rate through sheep nasal mucosa.
Conclusion: The results indicate that a mucoadhesive
nanoparticulate system can be used effectively for the
nasal delivery of the antihistamine, ebastine.
Keywords: Chitosan, Ebastine, Mucoadhesive,
Nanoparticles, Ionotropic gelation, Permeation, Drug
release, Poloxamer |
