The document discusses various methods for enhancing bioavailability of drugs. It begins by outlining common causes of low bioavailability such as first-pass metabolism and poor solubility. It then describes several methods for improving bioavailability including increasing drug solubility through techniques like micronization and use of surfactants, and enhancing permeability through lipid technologies and penetration enhancers. Specific technologies are also discussed like Optizorb which uses super-disintegrants to speed absorption and hot-melt extrusion which molecularly disperses drugs to increase dissolution. Nanoparticle systems are also proposed to increase permeability through physiological barriers like the blood-brain barrier to potentially treat diseases like Alzheimer's and Parkinson's.

1. BIOAVAILABILITY AND METHODS
OF ENHANCING BIOAVAILABILITY
Presented by
SHAHEEN BEGUM
Hallticket No:10S91R0035
UNDER THE GUIDANCE OF
Associate Professor. Syed Mohammed Kazim
Nizam Institute of Pharmacy & Research Centre
Deshmukhi (V), Nalgonda.
AFFILIATED TO JNTUH.

3. CAUSES OF LOW BIOAVAILABILITY
First pass metabolism
Poorly water soluble, slowly absorbing oral drugs
Insufficient time for absorption in GIT
Poor dissolution (highly ionized and polar)
Age,stress,disorders,surgery etc
Chemical reactions
Metabolism by luminal microflora

5. Methods of Enhancing Bioavailability
1.Enhancement of drug solibulity:
a. Micronization
b. Nanonization
c. SFR
d. SFL
e. EPAS
f. Use of surfactants
g. Molecular encapsulation with cyclodextrins
h. Eutectic mixtures

6. 2. Enhancement of drug permeability
a. Lipid technologies
b. Ion Pairing
c. Penetration enhancers
3. Enhancement of drug stability
d. Enteric coating
e. Complexation
f. Use of metabolism inhibitors
4. Enhancement of gastrointestinal retention
a. GRDDS

7. OPTIZORB TECHNOLOGY

8. •
Optizorb® technology is a combination of ingredients, which work together to speed up the
rate at which the paracetamol tablet disintegrates and dissolves in the stomach.
•
contains paracetamol 500mg along with super-disintegrants.
•
The new combination disperses five times faster and is absorbed 37% faster than standard
tablets.

9. HOT-MELT EXTRUSION TECHNOLOGY
The development of novel drugs with poor solubility and bioavailability brought
the application of HME into the realm of drug-delivery systems.
HME involves the application of heat, pressure and agitation through an
extrusion channel to mix materials together, and subsequently forcing them out
through a die.
HME extrusion has been shown to molecularly disperse poorly soluble drugs in a
polymer carrier, increasing dissolution rates and bioavailability.

10. ENHANCEMENT OF BIOAVAILABILITY BY
INCREASING PERMEABILITY THROUGH
PHYSIOLOGICAL BARRIERS
NANOPARTICLE SYSTEMS WITH CHELATION AGENTS:
Increased BBB permeability and lower toxicity
Nanoparticles made of natural or artificial polymers ranging in size from about
10–1000 nm and present a possible tool to transport drugs across the BBB
The advantages of nanoparticles include reduced drug toxicity, improved
biodistribution and therapeutic efficacy
The mechanism by which the nanoparticles deliver drugs into the brain may be
involved in the preferential absorption of ApoE and/or B.
The particles also appear to mimic LDL and interact with the LDL receptor,
resulting in their uptake by brain endothelial cells

11. BIOAVAILABILITY ENHANCEMENT BY BBB

12. Fighting Alzheimer's disease with nanotechnology
PLAQUE
FORMATION OF FIBRILS
BETA AMYLOID PEPTIDES

13. BREAKING THROUGH TO THE BRAIN, TO DELIVER A
CURE FOR PARKINSON’S
Nanotechnology uses a microscopic “bubble” transport system
it enables drugs to traverse the normally uncrossable blood brain barrier.
 Vesicles are one of the few things in the body that can permeate the BBB,
however, pathogens are able to break down the BBB, enabling substances such
as bacteria or other toxins to attack parts of the brain
The nanovesicles are highly stable and provide a controlled release mechanism
TIGHT JUNCTION
GLIAL CELLS
Nano bubble releasing drug

14. REFERENCES
•
D.M. BRAHMANKAR SUNIL B. JAISWAL Biopharmaceutics and pharmacokinetics a
Treatise,Second Edition..Page No:345-363
•
CVS SUBRAHMANYAM. Text book of Biopharmaceutics and pharmacokinetics .
•
shergill
•
http://archive.ispub.com/journal/the-internet-journal-of-aesthetic-and-antiaging-medicine/volume-2number-1/phytosomes-the-emerging-technology-for-enhancement-of-bioavailability-of-botanicals-andnutraceuticals
•
Wilson CG, Clarke CP, Starkey YY, Clarke GD. Comparison of a novel fast-dissolving acetaminophen
tablet
•
Martin physical pharmacy and pharmaceutical sciences 5th edition
•
Leon shargel.applied biopharmaceutics and pharmacokinetics
•
Pharmacokinetic and Bioequivalence Study Evaluating a New Paracetamol/Caffeine Formulation in
Healthy Human Volunteers Dongzhou J. Liu1 *, Mitchell Kotler1 and Scott Sharples2 1Medical Affairs
and New Products Research and Development, GlaxoSmithKline, Parsippany, NJ 07054, USA 2Celerion,
2420 W Baseline Rd, Tempe, AZ 85283, USA

15. REFERENCES
• Wilson CG, Clarke CP, Starkey YY, Clarke GD. Comparison of a novel fast-dissolving
acetaminophen tablet
• Martin physical pharmacy and pharmaceutical sciences 5th edition
• Leon shargel.applied biopharmaceutics and pharmacokinetics 4th Edition.
• Pharmacokinetic and Bioequivalence Study Evaluating a New Paracetamol/Caffeine
Formulation in Healthy Human Volunteers Dongzhou J. Liu1 *, Mitchell Kotler1 and
Scott Sharples2 1Medical Affairs and New Products Research and Development,
GlaxoSmithKline, Parsippany, NJ 07054, USA 2 Celerion, 2420 W Baseline Rd, Tempe,
AZ 85283, USA
• Milogibaldi, Biopharmaceutics and clinical pharmacokinetics 4th Edition Page no 146.
• Venkateshwarlu, Fundamentals of Biopharmaceutics and pharmacokinetics Page no 331.
• Remington’s Pharmaceuticals sciences volium 1 Page no 1037
• Remington’s Pharmaceuticals sciences volium 1 Page no 1041
• Robert E Notary, Biopharmaceutics and pharmacokinetics.
• Indian Journal of Pharmaceutical sciences.

16. Any Questions?