Albuterol in situ Bioadhesive Nasal Inserts
Mohamed Etman1, Ragwa Farid2, Aly Nada3, Abdelazim Ebian1
1Faculty of Pharmacy, Alexandria University, Alexandria, Egypt2Faculty of Pharmacy & Drug Manufacturing, Pharos University, Alexandria, Egypt
3Faculty of Pharmacy, Kuwait University, Kuwait ([email protected])
�In situ gelling inserts of AL (1.4%)
were prepared by film casting method
using aqueous solutions of AL and
different bioadhesive polymers (2%):
�Carboxymethyl cellulose sodium
(CMC-Na, FI), hydroxypropyl-
methylcellulose (HPMC, FII), Na
alginate (FIII), chitosan (FIV) and 1:1 mixture of FI and FII (FV).
�The inserts were investigated for:
content uniformity, thickness, surface
pH, weight uniformity, water uptake
and in vitro drug release.
�Bioadhesion was tested In vitro by
modified balance method and
displacement method:
�The inserts were placed on a hydrated surface of agar/mucin and the
displacement on the vertical surface
due to gravity was taken as an inverse
measure of the bioadhesion potential.
The drug release from CMC-Na and
sodium alginate inserts followed zero-
order kinetics while HPMC and
chitosan inserts showed non-Fickian
diffusion mechanism. The inserts
exhibited high water uptake with the
smallest values for chitosan (Fig. 2).
Fig.( 2): Water uptake profiles of the in situ
gelling mucoadhesive nasal inserts
prepared from different polymers at 25 0C
�The bioadhesive in situ gelling inserts
have shown satisfactory bioadhesive characteristics, water uptake and
extended drug release.
�The inserts could be used for nasal
delivery of AL over about 12 hours;
bypassing the hepatic first-pass
metabolism without potential
irritation.
Cumulative drug released exhibited
extended release for more than 10
hours with the order of chitosan>
Na alginate >CMC Na >HPMC (Fig. 1).
Fig. (1): Albuterol sulphate release from
the nasal inserts from different polymers
in simulated nasal fluid at 37 0C.
The bioadhesion force was in the
rank of sodium alginate = CMC-Na>HPMC > chitosan (Fig 3).
Fig.( 3): Adhesion force profiles of the
prepared insitu gelling mucoadhesive
nasal inserts from different polymers.
To formulate albuterol sulphate (AL)
bioadhesive nasal inserts, based on in situ gel release-controlling
polymers, having a high potential as
nasal drug delivery system.
Fig.( 4): Swelling index profiles of the
prepared in situ gelling mucoadhesive
nasal inserts at 250C in simulated nasal
fluid after 8 hours.
No displacement was observed for
all formulae except for FII (Fig. 5).
Fig.( 5 ): Adhesion profiles of the in situgelling mucoadhesive nasal inserts
prepared from different polymers.
The swelling indices ranged
between 0.1 and 0.4 (Fig. 4).
Objectives
Methods
RESULTS
CONCLUSION