Albuterol in situ Bioadhesive Nasal Inserts Mohamed Etman 1 , Ragwa Farid 2 , Aly Nada 3 , Abdelazim Ebian 1 1 Faculty of Pharmacy, Alexandria University, Alexandria, Egypt 2 Faculty of Pharmacy & Drug Manufacturing, Pharos University, Alexandria, Egypt 3 Faculty 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 0 C 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 0 C. 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 25 0 C 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 situ gelling mucoadhesive nasal inserts prepared from different polymers. The swelling indices ranged between 0.1 and 0.4 (Fig. 4). Objectives Methods RESULTS CONCLUSION