FOR ENHANCED BUCCAL

1. Presentation on Penetration
enhancers
Dr. Sanjula Baboota Abdul Muheem
Deptt of pharmaceutics M.Pharma(pharmaceutics)
JAMIA HAMDARD F/O PHARMACY
JAMIA HAMDARD

2. 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-

3. • 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.

5. -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.

6. 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

7. 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