Presentation on Penetration enhancers

Abdul MuheemM.Pharma(pharmaceutics)F/O PHARMACYJAMIA HAMDARD

Dr. Sanjula BabootaDeptt of pharmaceuticsJAMIA 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 drugsCo- 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 bromide

13 Sod.EDTA

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 permeability, polysorbate 80 less effective

Rat in-vivo

3 Insulin 5% sod. Glycocholate Increased F buccal from 0.7% -26%

Rat in vivo

4 insulin 5% laureth-9,aprotinin, sod.salicylate

Increased F from 0.7-3.6% ,laureth-9 ,other had no effect

Rat in vivo

5 Calcitonin Various bile salts Increased pharmacologic effect, increased stability

Rat in vivo

6 Interferon 1-4% sod.taurocholate ,5% cyclodextrin

Increased F from 0.014% to 0.25% with sod.taurocholate, other have less effect

Rat in vivo