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Penetration enhencers

The presentation discusses penetration enhancers that can be used to promote the permeation of drugs through epithelial barriers and mucosa. It notes that chemical enhancers work by altering the properties of mucus, cell membranes, or enzymatic barriers. Specific chemical enhancers that have been used include chelators, surfactants, bile salts, fatty acids, and chitosan derivatives. The presentation provides tables listing examples of penetration enhancers and studies examining the effects of enhancers like sodium glycocholate and sodium taurocholate on permeation of various drugs in animal models.

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Presentation on Penetration enhancers Dr. Sanjula Baboota Abdul Muheem Deptt of pharmaceutics M.Pharma(pharmaceutics) JAMIA HAMDARD F/O PHARMACY JAMIA HAMDARD
Introduction • Permeation of drugs throughout epithelial barriers could be promoted by ‘penetration enhencers’capable of decreasing barrier properties of the mucosa by different mechanisms. • Enhancement is founded on different techniques that are usually divided in chemical or physical methods. Chemical methods- chemical enhancers are through to improve absorption without irritation or damage the mucosa by-
• Alteration the rheology of the mucus layer. • Transiently altering the lipid bilayer membrane. • Increasing cell membrane fluidity. • Extracting structural lipids. • Altering cellular proteins. • Increasing the thermodynamics activity of the permeate. • Overcoming the enzymatic barrier. -chemical enhancers could be added to a formulation, alone or in combination ;their efficacy depends on the physiochemical properties of both the drug & vehicle.
-various chelators ,surfactants, bile salts &fatty acids, have been used as permeation enhancers ;chitosan & its derivatives have been used as enhancers of small polar moiety & hydrophobic large molecules. recently lysalbinic acid ,a product of egg albumin ,hydrolysis ,has been successfully used as enhancers for protein & peptides. Enzymatic drug inactivation is neither rapid nor extensive as the enzymatic activity of buccal mucosa is relatively low . Nevertheless ,enzymes of the oral cavity could degrades some peptide & protein drugs Co- administration of enzyme inhibitors such as aprotinin ,could be effective as they reduce the activity of proteolytic enzymes.
S.No Penetration Enhancers S.No Penetration Enhancers 1 Aprotinin 8 Phosphotidyl choline 2 Azone 9 Polyoxyethylene 3 Lauric acids 10 Sod. Glycocholate 4 Glycol 11 Sod. Taurocholate 5 Cyclodextrin 12 Sod.glycodeoxycholate 6 Cetyltrimethyl ammonium 13 Sod.EDTA bromide 7 Polysrbate 80 14 Sod.taurodeoxycholine
S.N. Drug Enhancers results Methods 1 Insulin Sod.glycocholate F=0.5% Dog in-vivo 2 Glucose SLS, polysorbate 80 SLS increased the Rat in-vivo permeability, polysorbate 80 less effective 3 Insulin 5% sod. Glycocholate Increased F buccal Rat in vivo from 0.7% -26% 4 insulin 5% laureth-9,aprotinin, Increased F from 0.7- Rat in vivo sod.salicylate 3.6% ,laureth-9 ,other had no effect 5 Calcitonin Various bile salts Increased Rat in vivo pharmacologic effect, increased stability 6 Interferon 1-4% sod.taurocholate Increased F from Rat in vivo ,5% cyclodextrin 0.014% to 0.25% with sod.taurocholate, other have less effect
Penetration enhencers