Presentation on Penetration enhancersDr. Sanjula Baboota Abdul MuheemDeptt 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 improveabsorption without irritation or damage themucosa 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 thephysiochemical properties of both the drug & vehicle.
-various chelators ,surfactants, bile salts &fatty acids,have been used as permeation enhancers ;chitosan & itsderivatives have been used as enhancers of small polarmoiety & hydrophobic large molecules. recently lysalbinic acid ,a product of egg albumin,hydrolysis ,has been successfully used as enhancers forprotein & peptides.Enzymatic drug inactivation is neither rapid nor extensiveas the enzymatic activity of buccal mucosa is relativelylow .Nevertheless ,enzymes of the oral cavity could degradessome peptide & protein drugsCo- administration of enzyme inhibitors such as aprotinin,could be effective as they reduce the activity ofproteolytic enzymes.
S.N. Drug Enhancers results Methods1 Insulin Sod.glycocholate F=0.5% Dog in-vivo2 Glucose SLS, polysorbate 80 SLS increased the Rat in-vivo permeability, polysorbate 80 less effective3 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 effect5 Calcitonin Various bile salts Increased Rat in vivo pharmacologic effect, increased stability6 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