Dr.

SHUBHRAJIT MANTRY
D.Pharm, B.Pharm, M.Pharm, Ph.D
Associate Professor,
Department of Pharmaceutics
Sharadchandra Pawar College of Pharmacy,
Otur, Pune
 INTRODUCTION
Target means specific organ or a cell or group of
cells, which in chronic or acute condition need
treatment.

Targeted drug delivery is a kind of smart drug

delivery system which is miraculous in delivering
the drug to a patient.
Most conventional dosage forms deliver
drug into the body that eventually
reaches the site of action by multiple
steps of diffusion and partitioning.

Targeted drug delivery system refer to

systems that place the drug at or near
the receptor site or site of action.
CONCEPTS OF TARGETING

The concept of designing specified delivery system to

achieve selective drug targeting has been originated

from the perception of Paul Ehrlich, who proposed

drug delivery to be as a 'magic bullet‘.

It was the very first report published on targeting

(Paul Ehrlich, 1902) describing targeted drug

delivery as an event where, a drug-carrier

complex/conjugate, delivers drug(s) exclusively to the

preselected target cells in a specific manner.

Bangham's observation on phospholipid hexagonal

liquid crystals, that they are permselective to the ions

in a manner similar to biomembrane, led to discovery

of artificial vesicular system based on phospholipid

amphiphiles (Bangham, 1965).

Gregoriadis, 1981 described drug targeting

using novel drug delivery systems as 'old

drugs in new cloths'.

Targeted therapy, as Ehrlich, 1902 proposed remains an

unachieved goal yet, however the idea stimulated a long

series of experiments that propounded the philosophy of

targeting of drugs and genes and attracted present

generation of researchers towards the problems and

prospects associated with the concept.

It is pertinent to discuss the concept and components, which are

utilized in the targeting of drug(s).

A number of essential aspects which should be considered for

the designing of drug delivery systems to achieve this goal

include target, carrier, ligand(s) and physically modulated

components.
Targeted drug delivery implies for selective and effective

localization of pharmacologically active moiety at preidentified

(preselected) target(s) in therapeutic concentration, while

restricting its access to non-target normal cellular linings, thus

minimizing toxic effects and maximizing therapeutic index

(Gregoriadis and Florence, 1993).

 CLASSIFICATIO
N
Drug targeting has been classified into three types:

A. First order targeting

It refers to DDS that delivers the drug to the capillary
bed or the active site or organ or tissue.
B. Second order targeting
It refers to DDS that delivers the drug to a special cell
type such as the tumor cells and not to the normal
cells.
C. Third order targeting
It refers to DDS that delivers the drug to specific
intracellular compartments in the target cells e.g.,
Lysosomes.
One of the key organelles involved in digestion and waste removal is the lysosome. Lysosomes are organelles that
contain digestive enzymes. They digest excess or worn out organelles, food particles, and engulfed viruses or bacteria.
Lysosomes are like the stomach of the cell.
(An organelle is a tiny cellular structure that performs specific functions within a cell)
 STRATEGIES
OF
TARGETED DRUG DELIVERY SYSTEM

Drug targeting to an area of interest within the body

increases the therapeutic effectiveness as well as it reduces
the toxicity.

Two strategies are widely used for drug targeting to the

desired organ/tissue.

1. PASSIVE TARGETING

2. ACTIVE TARGETING
1. PASSIVE TARGETING

It refers to natural or passive disposition of drug-carrier based on the physicochemical

characteristics of the system in relation to the body.

2. ACTIVE TARGETING

It refers to alteration of the natural disposition of the drug carrier, directing it to specific cells,
tissues or organs.
Example: Use of Ligands or monoclonal antibodies which can target specific sites.
 AR RI E RS
C
OF R Y
G D EL IV E
E T ED D R U
TAR G
SYSTEM
 Carriers
Carrier is one of the most important entities
essentially required for successful transportation
of the loaded drug.

They are drug vectors, which sequester, transport

and retain drug en route, which deliver it within or
in the vicinity of the target.
 TYPES OF CARRIER SYSTEMS USED FOR
TARGETED DRUG DELIVERY SYSTEM
1. COLLOIDAL CARRIERS
A) Vesicular Systems:
Liposomes, Niosomes, Pharmacosomes, Virosomes, Immunoliposomes.

B) Microparticulate Systems:
Microparticle, nanoparticle, Magnetic Microsphere, Albumin microsphere,
Nanocapsules.
2. CELLULAR CARRIERS
Resealed erythrocytes, Serum albumin, Antibodies, platelets, Leukocytes
3. SUPRAMOLECULAR DELIVERY SYSTEM

Micelles, Reverse micelles, Mixed micelles, Polymeric micelles, Liquid crystal,

lipoproteins (chylomicron, VLDL, LDL)

Synthetic LDL mimicking particlle (supramolecule biovector system)

4. POLYMER BASED SYSTEMS

Single sensitive, Mucoadhesive, Biodegradable, Bioerodible, Soluble synthetic

Polymeric carriers

5. MACROMOLECULAR CARRIERS

a) Proteins, Glycoproteins, Neo Glycoproteins and Artificial viral envelopes

(AVE)

b) Glycosylated water soluble polymers (Poly-L-lysine)

c) Mabs, Immunological Fab fragments, antibody enzyme complex and bispecific

Antibodies

d) Toxins, Immunotoxin & rCD4 toxin conjugates

e) Lectins, Polysaccharides
 VARIOUS CARRIERS USED IN
TARGETED DRUG DELIVERY SYSTEM

Carriers used in TDDS Size range

Liposomes 25nm-100μm

Niosomes 10 to 1000 nm

Aquasome 60-300nm

Resealed Erythrocytes 2.5-7.8μm

Nanoparticles 10-1000nm

Solid Lipid Nanoparticles 50-1000nm

(SLN)
 EVENTS
AND
L P RO CE SS
BIOLOGICA
N DRUG TARGE T ING
INVO L VED I
Order involved in Drug targeting
A.First order targeting
It refers to DDS that delivers the drug to the capillary bed or
the active site or organ or tissue.
B. Second order targeting
It refers to DDS that delivers the drug to a special cell type
such as the tumor cells and not to the normal cells.
C.Third order targeting
It refers to DDS that delivers the drug to specific
intracellular compartments in the target cells e.g., Lysosomes.
Process involved in Drug targeting

1.Cellular uptake and processing

2.Transport across the epithelial barrier

3.Extravasation

4.Lymphatic uptake
1. Cellular uptake and processing
2. Transport across the epithelial barrier

3. Extravasation

4. Lymphatic uptake
THA N K Y O U