CELL MEMBRANE OF THE GASTROINTESTINAL TRACT

Cell Membrane
-a.k.a. Plasma Membrane
-is a thin semi-permeable membrane that surrounds the cytoplasm of a cell. Its function is to
protect the integrity of the interior of the cell by allowing certain substances into the cell, while
keeping other substances out.
-An important function of a biological membrane is to serve as a barrier to the outside world.
However, membranes are not impenetrable walls. Obviously, nutrients must enter the cell and
waste products have to leave in order for the cell to survive.

CHARACTERISTICS:
1.

Non-ciliated columnar epithelium- a single layer of non-ciliated column like cells

with oval nuclei near base of cells.

2.

Microvilli- finger like cytoplasmic projections, increase surface area of plasma

membrane thus increasing cells rate of absorption.

3.

Goblet cells- are modified columnar epithelial cells that secrete mucus, a slightly
sticky fl uid, at their apical surfaces. Before release, mucus accumulates in upper
portion of cell, causing it to bulge and making the whole cell resemble a goblet or
wine glass.

4.

Highly polarized- one side differs in structure and function from the other.
-

5.

Protein-mediated transport - In order to cross the hydrophobic interior of the

bilayer, water-soluble molecules (those that are either charged or have polar
groups) and large molecules require the action of membrane transport proteins.
These integral membrane proteins provide a continuous protein-lined pathway
through the bilayer.

3.

Endocytosis and Exocytosis -large macromolecules (e.g., proteins, viruses,

lipoprotein particles) require more complex mechanisms to traverse membranes and
are transported into and out of cells selectively via endocytosis and exocytosis
(secretion).

NATURE OF CELL MEMBRANE

Transcellular absorption is the process of drug movement across a cell. Some polar molecules
may not be able to traverse the cell membrane but, instead, go through gaps or tight junctions
between cells, a process known as paracellular drug diffusion.

its plasma membrane is organized into at least two discrete regions, each with
different sets of transport proteins.

A key determinant in the effectiveness of drug absorption, distribution, and

elimination. For example, a drug taken orally that targets cells in the central
nervous system must cross several membranes: first the barrier presented by
the intestinal epithelium, then the walls of the capillaries that perfuse the gut,
then the blood-brain barrier.

Lipid in nature

Anatomy
Cell Membrane

Composition
Proteins

Function
Hydrophilic layer

Triglycerides
Steroids (cholesterol)
Phospholipids(lecithin)

Lipophilic layer
biomolecular

Types of Functional or Anatomic membranes and their permeability for drugs in GIT
ORGAN
Stomach

TYPE OF MEMBRANE
Lipid membrane with few
pores

Small Intestines

There are several theories as to the structure of the cell membrane.

LIPID BILAYER OR UNIT MEMBRANE THEORY

Structure and Function of Membranes

Lipid membrane with few

pores

PERMEABILITY
For lipophilic, nonionized
acidic drugs, less for small
molecular size
nonelectrolytes
For lipophilic drugs (acidic
and basic), less for
hydrophilic drugs

Mechanism of transport
1.

2.

Selectively permeable- allows certain molecules or ions to pass through it by means

of active or passive transport.
-

6.

Carrier (integral) - Transports a specific substance across membrane by undergoing a

change in shape. For example, amino acids, needed to synthesize new proteins, enter body
cells via carriers. Carrier proteins are also known as transporters.
Receptor (integral)- Recognizes specific ligand and alters cell's function in some way. For
example, antidiuretic hormone binds to receptors in the kidneys and changes the water
permeability of certain plasma membranes.
Enzyme (integral and peripheral)- Catalyzes reaction inside or outside cell (depending on
which direction the active site faces). For example, lactase protruding from epithelial cells
lining your small intestine splits the disaccharide lactose in the milk you drink.
Linker (integral and peripheral) - Anchors filaments inside and outside the plasma
membrane, providing structural stability and shape for the cell. May also participate in
movement of the cell or link two cells together.
Cell identity marker (glycoprotein)- Distinguishes your cells from anyone else's (unless you
are an identical twin). An important class of such markers are the major histocompatibility
(MHC) proteins.
* Aquaporins- Water soluble drugs penetrate the cell membrane through aqueous channels
or pores.

Diffusion - This process allows molecules that are small and lipophilic (lipidsoluble), including most drugs, to easily enter and exit cells.

a. Passive diffusion
- drug moves from a region of high concentration to one of lower concentration
- does not involve a carrier.
b. Facilitated diffusion
- agents can enter the cell through specialized transmembrane carrier proteins
-does not require energy, can be saturated, and may be inhibited.
Types of transmembrane proteins
Ion channel (integral) - Forms a pore through which a specific ion can flow to get across
membrane. Most plasma membranes include specific channels for several common ions.

originally proposed by Davson and Danielli (1952)

considers the plasma membrane to be composed of two layers of phospholipid

between two surface layers of proteins

with the hydrophilic head groups of the phospholipids facing the protein layers and
the hydrophobic tail groups of the phospholipids aligned in the interior.

The lipid bilayer theory explains the observation that lipid-soluble drugs tend to
penetrate cell membranes more easily than polar molecules.

However, the bilayer cell membrane structure does not account for the diffusion of
water, small-molecular-weight molecules such as urea, and certain charged ions.
FLUID MOSAIC MODEL

proposed by Singer and Nicolson (1972),

explains the transcellular diffusion of polar molecules.

According to this model, the cell membrane consists of globular proteins embedded
in a dynamic fluid, lipid bilayer matrix.

These proteins provide a pathway for the selective transfer of certain polar
molecules and charged ions through the lipid barrier.

transmembrane proteins are interdispersed throughout the membrane.

Two types of pores of about 10 nm and 5070 nm were to be present in membranes

based on capillary membrane transport studies (Pratt and Taylor, 1990).

These small pores provide a channel through which water, ions, and dissolved
solutes such as urea may move across the membrane.

Membrane proteins embedded in the bilayer serve special purposes.

These membrane proteins function as structural anchors, receptors, ion channels,

or transporters to transducer electrical or chemical signalling pathways that facilitate or
prevent selective actions.