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Buccal and sublingual administration
Tablets to be placed under the tongue or in the cheek pouch and retained in the mouth Highly vascular epithelium Ideal for: lipid soluble drugs, high metabolism in the GIT or liver after oral administration Oral mucosa resembles the skin more than the GIT Oral mucosa: two areas: Non keratinized area: floor of the mouth, buccal mucosa Keratinized mucosa: gum, hard palate, inner side of the lips
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Cohesion is by lipids and glycolipids
Buccal mucosa is composed of 2 components: epithelium and connective tissue Rapid turnover of the cells Non keratinized squamous cells with different degrees of maturity Cohesion is by lipids and glycolipids
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Absorption is mainly by passive diffusion and it obeys pH partition hypothesis
Lipid solubility and absorption Nitroglycerine tablets Nicotine chewing gum
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Buccal mucosa is composed of 2 components: epithelium and connective tissue
Rapid turnover of the cells Non keratinized squamous cells with different degrees of maturity
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Absorption of peptides and proteins
Barriers ? Transport: intracellular, intercellular Buccal mucosa and enzymes: low levels of membrane associated enzymes
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Approaches to improve permeation
Increase the lipophilicity of the peptide Lipophilic carriers Absorption enhancers In vitro models for testing Cell lines Animal models
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Penetration enhancers used in Buccal Delivery Chelators: EDTA, citric acid, sodium salicylate, methoxy salicylates. Surfactants: sodium lauryl sulphate, polyoxyethylene, Polyoxyethylene-9-laurylether, Polyoxythylene-20-cetylethe. Benzalkonium chloride, 23-lauryl ether, Bile salts: sodium glycocholate, sodium deoxycholate, sodium taurocholate, sodium glycodeoxycholate, Fatty acids: oleic acid, capric acid, lauric acid, lauric acid/propylene glycol. Inclusion complexes: cyclodextrins. Thiolated polymers: chitosan-4-thiobutylamide, chitosan-4-thiobutylamide/GSH, chitosan-cysteine, Poly (acrylicacid)-homocysteine Mechanisms of enhancing permeation Changing mucus rheology Increasing the fluidity of lipid bilayer membrane Acting on the components at tight junctions By overcoming the enzymatic barrier
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