bioenhancer and its mechanism

1. BIOENHANCER
Supervisor: Dr. Shamsher Singh
Department of Pharmacology
ISF College of Pharmacy, Moga
Presented by: Shakshi Sharma
M. Pharm: Pharmacology (3rd semester)
1

2. Contents
• Introduction
• Benefits of adding bioenhancer
• Ideal properties
• Mechanism of action
• Classification on the basis of MOA
• Piperine: Most commonly used bioenhancer
• Clinically used bioenhancer
• References
2

3. Introduction
• Bioenhancers are the agents capable of enhancing bioavailability and
bioefficacy of a particular drug with which it is combined, with or without
any typical pharmacological activity.
• The concept of bioenhancer was first time reported in 1929 by Bose [1].
• Piperine, aloe vera, allicin, quercetin, etc are commonly used as
bioenhancer.
• The commonly used marketed formulation is Risorine (200 mg of
rifampicin, 300 mg of isoniazid (INH) and 10 mg of Piperine). Piperine
increases bioavailability of rifampicin by about 60% [1].
3

4. Benefits of adding bioenhancer
• Reduced dosage.
• Reduces the drug cost.
• Reduces the drug resistance.
• Reduces the drug adverse effects.
• Increases the efficacy of drug.
4

5. Ideal Properties
• Non toxic to human/animal.
• Should be effective at a very low concentration in a
combination.
• Should be easy to formulate.
• Should enhances absorption and activity of the drug
molecules.
• Should be extracted in its pure form.
• Should be stable with time and environment.
• Should be cost effective.
5

6. Mechanism of action2
BIOENHANCER
Inhibition of drug
metabolizing enzymes
Stimulation of gut amino
acid transporter
Inhibition of cell pump
responsible for drug elimination
from cells
Increases the blood supply and
reduces HCl secretion
Inhibition of intestinal
production of glucuronic
acid
Increases the absorption in GIT
6

7. Classification on the basis of MOA
Bioenhancer
Inhibitors of Pgp
efflux pump:-
Caraway, Naringin,
Quercetin, Cumin.
Suppressors of
CYP-450 enzyme
and its iso enzyme:-
Gallic acid and its
esters.
Regulators of GIT
function to
facilitate better
absorption:- Aloe
vera, Glycyrrhizin,
Zingiber officinale.
7

8. Piperine: Most commonly used bioenhancer2
• Piperine is extracted from black pepper and
long pepper Piper longum and Piper nigrum .
• Piperine enhances the metabolism, raises the
serotonin and dopamine level, and also
enhances the memory functions.
• It shows anti oxidant, anti inflammatory, anti
allergic properties.
8

9. How does piperine increase the bioavailability
of other drugs?
• Piperine inhibits the detox enzyme which breaks the CYP3A4
and increases the drug absorption in the gut resulted into
increase in the blood supply. Thus, piperine increases the
bioavailability of other drugs such as quercetin.
• It increases the absorption of drugs by increasing the length of
intestinal villi several folds.
• It also inhibits the efflux pump- P glycoprotein in the gut and
liver so that drug is not thrown out from the body and backs
into the GIT lumen.
9

10. Clinically used bioenhancers
Plant origin3:-
• Carum Carvi (enhance the bioavailability of antibiotics, anti-
fungals, etc)
• Garlic (enhance the fungicidal activity of Amphotericin B against
pathogenic fungi)
• Naringin (inhibits intestinal CYP3A4, CYP3A1, CYP3A2, P-gp)
• Ginger (acts on GIT mucous membrane to facilitate absorption)
• Indian aloe (improves the absorption of Vitamins C and E)
Animal origin3:-
• Cow urine distillate (enhances the transport of antibiotics like
rifampicin across the gut)
10

11. Contd…
• Seeds of caraway (enhances the Cmax and AUC of rifampicin)
• Glycyrrhizin (inhibition of cell growth)
• Tea leaves and buds (promotes oxidation and decreases the
oxidation rate)
• Stevia leaves (stimulation of insulin secretion)
• Gallic acid (increases drug absorption and inhibits drug
metabolizing enzymes)
• Niaziridin (isolated from Moringa oleifera, acts on GIT
mucous membrane to facilitate absorption)
11

12. References
1) Randhawa GK, Kullar JS, Rajkumar. Bioenhancers from Mother Natural
and their applicability in modern medicine. Int J App Basic Med Res
2011; 1(1):5-10.
2) Atal N, Bedi KL. Bioenhancers: Revolutionary concept to market. J Ayur
Integ Med 2010; 1(2):96-99.
3) Kumar-Sarangi M, Chandra-Joshi B, Ritchie B. Natural Bioenhancers in
Drug Delivery: An Overview. Puerto Rico health sciences journal. 2018
Mar 14;37(1):12-8.
4) Gerber W, Steyn J, Kotzé A, Hamman J. Beneficial pharmacokinetic drug
interactions: a tool to improve the bioavailability of poorly permeable
drugs. Pharmaceutics. 2018 Jul 26;10(3):106-121.
12

13. THANK YOU
13