3. ABSORPTION MECHANISM
•The main categories of drug transport
mechanisms involved in absorption are:
1. Transcellular/Intracellular transport
2. Paracellular/Intercellular transport
3. Vesicular transport
4. TRANSCELLULAR TRANSPORT
Transcellular transport is defined as
the passage of drugs across the GI
epithelium
Most common pathway for drug
transport
•Types:
•Passive transport
•Active transport
5. MECHANISM OF TRANSCELLULAR
TRANSPORT
•3 steps are involved in transcellular transport of
drugs:
i. Permeation of GI epithelial cell membrane
ii. Movement across the intracellular space(cytosol)
iii. Permeation of the lateral or basolateral
membrane
6. TYPES OF TRANSCELLULAR TRANSPORT
1.PASSIVE TRANSPORT
• These transport process do not require energy other than that of
molecular motion to pass through the lipid bilayer.
• Movement of molecules take place from higher conc to lower
conc.
• Types of passive transport:
a) Passive diffusion
b) Pore transport
c) Ion-pair transport
d) Facilitated diffusion
7. PASSIVE DIFFUSION
• It is defined as the difference in the
drug concentration on either side of
the membrane.
• Also called as non-ionic diffusion.
• Drug movement is a result of kinetic
energy of molecules.
• Eg of drugs undergoing passive
diffusion: most of the drugs
8. PORE TRANSPORT
• Pore transport involves the
transport of molecules into the cell
through the protein channels
present in the cell membrane.
• Also called as convective transport
,bulk flow or filtration.
• Eg of drugs undergoing pore
transport are : Very small
molecules (less than 100 daltons),
such as urea, water and sugars are
able to rapidly cross the cell
membrane through pores.
9. ION-PAIR TRANSPORT
• Absorption of drugs taking place by
ionizing under all PH conditions is termed
as ion-pair transport.
• The agents penetrate the membrane by
forming reversible neutral complexes with
endogenous ions of the GIT like mucin.
• Such neutral complexes have both
required lipophilicity as well as aqueous
solubility for passive diffusion. such a
phenomenan is called as ion-pair
transport.
• Eg of drugs: propranolol, a basic drug
forms an ion-pair with oleic acid and
quinine which forms ion-pair with
hexylsalicylate.
10. FACILITATED DIFFUSION
• It is a carrier mediated transport
systemthat operates down the
concentration gradient.
• It is the process of spontaneous
passive transport of molecules or
ions across a biological membrane
via specific transmembrane
integral proteins
• The drug moves along a conc
gradient.
• Eg: entry of glucose into molecules
and fat cells by GLUT4,vitaminB12
11. ACTIVE TRANSPORT
• These transport processes require
energy from ATP to move drug
molecules from extracellular to
intracellular.
• Movement of molecules take
place from lower conc to
highconc.
• Types of active transport:
• Primary transport
• Secondary transport
12. PRIMARY ACTIVE TRANSPORT
• Involves direct ATP requirement
• The process transfers only one ion or molecule and in only one
direction, hence called as uniporter.
• Carrier proteins involved are:
• Ion transporters
• ABC(ATP-binding cassette) transporters.
• Eg: muscle cells contain Ca2+ uniporters
13. SECONDARY ACTIVE TRANSPORT
• In this process there is no direct requirement of ATP.
• The transport of ion or molecule (coupled or co-transport)occurs either
in same or opposite direction.
• Types:
i. Symport (co-transport)
ii. Antiport (counter transport)
14. SYMPORT
• Involves movement of molecules
of both the molecules in the
same direction.
• Eg:
i. Na+ - glucose symporter,
H+coupled peptide transporter
16. ANTIPORT
• Involves movement of molecules in
the opposite direction
• Eg: expulsion of H+ ions using the
Na+ gradient in the kidneys.
17. PARACELLULAR TRANSPORT
• Paracellular transport is defined as the transport of drugs
through the junctions between the GI epithelial cells.
• Mechanisms involved are:
1. Permeation through tight junctions of epithelial cells.
2. persorption
18. PERMEATION
• This process basically occurs
through openings which are little
bigger than the aqueous pores.
• Eg: insulin,cardiac glycosides.
19. PERSORPTION
• Persorption is the permeation of
drug through temporary
openings formed by shedding of
two neighbouring epithelial cells
into the lumen.
20. VESICULAR TRANSPORT
• It is the minor transport mechanism which involves engulfing
extracellular materials within a segment of the cell membrane to
form a vesicle.
• This is the only transport mechanism where by a drug or compound
does not have to be in an aqueous solution in order to be absorbed.
• Also called as endocytosis.
21. TYPES OF ENDOCYTOSIS:
• Endocytosis includes 2 types of processes:
1. Phagocytosis
2. Pinocytosis
• Eg :sabin polio vaccine, botulism toxin etc: