ROUTES OF ADMINISTRATION

OF BIOTECH PRODUCTS:
PARENTERAL ROUTE
CONSIDERING LEPTOSOMES
AND MICROSPHERES

BY:

Pharmacist MD. ALIUL

ISLAM TANOY
GUIDED BY:
Mohammad Shahriar
(Assistant professor
of
University of Asia Pacific)

CONTENTS:
Routes of drug administration
Definition of Parenteral Route
Types of Parenteral Route
Advantages and Disadvantages of Parenteral
Route
Comparison of other route
Biotech example of Parenteral Route
Liposome & mechanism of drug delivery
Application of Liposomes
Microspheres & mechanism of drug delivery
Application of Microspheres

R O U T E O F A D M I N I S T R AT I O N

A route of administration in
pharmacology and toxicology is the
path by which a drug, fluid, poison,
or other substance is taken into
the body.

The pharmacokinetic properties,

such as absorption, distribution,
metabolism, and excretion, of a drug
are critically influenced by the route
of administration.

PARENTERAL ROUTE:
The term Parenteral comes from two Greek
words- Para (outside) & Enteron (intestine),
meaning outside the intestine.
Parenteral route of administration means the
medicine is generally directly administered by
injection such as SC, IV, IM, IA, IT, or IC or
through transdermal patches, which isn't
administered with an injection but is still
considered a parenteral route.

TYPES OF PARENTERAL ROUTES

Intravenousalso popularly known as I.V.which
is given directlyinto avein with injection.
Intra-arterialis giveninto anartery through
injection, e.g.vasodilatordrugs such as Sodium
Nitroproside, Methyl Dopa etc.
Intra-muscularinjection given to the muscular
part of the body.
Intrathecal:Drug is direcly administered in to
the spinal cord
Intraosseousinfusion: Into thebonemarrow


ADVANTAGESOFPARENTERALADMINISTRA
TION:
Rapid action of drug.
Can be employed in unconscious/ uncooperative
patients.
Drugs, which are not absorbed in small intestine or
irritate the stomach can be administered by this route.
Drugs, which are modified by alimentary juices and
liver can be given by this route.
can deliver drugs in large amounts, will have 100
percent bioavailability.
Does not have 1st pass metabolism.
Polor drug can be given as they are absorbed,
( eg.- Streptomycin)

DISADVANTAGEOFPARENTERAL
ADMINISTRATION
Less safe, more expensive.
Inconvenient (painful) for the patient.
Self medication is difficult.
Chances of local injury at the site of injection.
Itisdifficulttoreverseitsphysiologicaleffect.

COMPARISON:
Parenteral route

Enteral route

1. The term Parenteral comes

from two Greek words- Para
(outside) & Enteron (intestine),
meaning outside the intestine.
2. Its mechanism of drug
absorption is for most drugs is
passive transfer (eg.- Levodoa
follows
carrier
mediated
transport).
3. Drug can be directly enters
systemic circulation.

1. The term Enteral comes from

one Greed words- Enteros
(intestine), meaning the intestine.

4. Does not
metabolism.

Does
have
metabolism.

have

1st

2. Its mechanism of drug

absorption is for most drugs is
active transfer.
3. Drug cant directly enters
systemic circulation

pass 4.

1st

pass

5. Onset of action is faster.

5. Onset of action is slower.

6. Drug can be given unconscious &

uncooperative patients.

6. Drug cant be given unconscious

& uncooperative patients.

BIOTECHNO
LOGY:

Manipulation of living
organisms or their
components to produce useful
commercial products such as,
new bacterial strains, or novel
pharmaceuticals.

Therapeutic agents produced

by biotechnological processes
such as recombinant DNA
technology, fermentation,
tissue, cell culture technology
and genetic engineering.

BIOTECH EXAMPLES OF PARENTERAL

ROUTES OF DRUGS:
Name

Type

Molecular
target

Condition

Insulin

Systemic
Factor

Glucose
metabolism

Diabetes

G-CSF

Systemic
Factor

Neutrophils

Neutropenia

Erythropoietin Systemic
Factor

Erythropoiesis Renal failure

Omalizumab

IgE

Humanized
monoclonal
antibody

Asthma

BIOCOMPATIBILTY OF
PARENTERAL DOSAGE FORMS:

Biocompatibility "Refers to the ability of a

biomaterial to perform its desired function with
respect to a medical therapy, without eliciting
any undesirable local or systemic effects in the
recipient or beneficiary of that therapy, but
generating the most appropriate beneficial
cellular or tissue response in that specific
situation, and optimizing the clinically relevant
performance of that therapy"

BIOAVAILABILITY AND PARENTERAL DOSAGES

FORMS VS ORAL DOSAGE FORMS :

LIPOSOME
Aliposomeis a tiny bubble (vesicle), made
out of the same material as a cell membrane.
Liposomes can be filled with drugs, and used
to deliver drugs forcancerand other
diseases.
Membranes
are
usually
made
of
phospholipids, which are molecules that have
a head group and a tail group.
The head is attracted to water, and the tail,
which is made of a long hydrocarbon chain, is
repelled by water.

LIPOSOMES CONTT
When membrane phospholipids are disrupted,
they can reassemble themselves into tiny spheres,
smaller than a normal cell, either as bilayers or
monolayers. The bilayer structures are liposomes.
The monolayer structures are called micelles.
The name liposome is derived from two Greek
words: 'Lipos' meaning fat and 'Soma' meaning
body.
Liposomes
were first described by British
haematologist Dr Alec D Bangham FRS in 1961
(published 1964), at the Babraham Institute, in
Cambridge.

LIPOSOMES CONTT
They were discovered when Bangham and R. W.
Horne were testing the institute's new electron
microscope by adding negative stain to dry
phospholipids.
The resemblance to the plasmalemma was
obvious, and the microscope pictures served as
the first real evidence for the cell membrane
being a bilayer lipid structure.

MANUFECTURING:

The correct choice of liposome preparation

method depends on the following parameters:
The physicochemical characteristics of the
material to be entrapped and those of the
liposomal ingredients;
The nature of the medium in which the lipid
vesicles are dispersed
The effective concentration of the entrapped
substance and its potential toxicity;
Additional
processes
involved
during
application/delivery of the vesicles;
Optimum size, polydispersity and shelf-life of the
vesicles for the intended application; and,

MANUFECTURING CONTT.

Batch-to-batch reproducibility and possibility

of large-scale production of safe and efficient
liposomal products
Example:
Name

Trade name

Liposomal
amphotericin B
Liposomal
vaccine
Liposomal
vaccine
Liposomal
vincristine

IRIV
IRIV

Company

Indication

Ambisome

Gilead Sciences

Fungal
protozoal
infections

Epaxal

Crucell

Hepatitis A

Inflexal V

Berna Biotech

Influenza

Marqibo

Acute
Lymphoblastic
Spectrum Pharmac
Leukemia
(ALL)
euticals
and Melanoma

and

APPLICATION:
Applications
of
liposomes
in
the
sciences:
Use of liposomes in cosmetics
Use of liposomes in agro-food industry
Use of liposome in pharmaceutical industry:
Example:
Current Applications

Liposome Utility

Disease

States

Treated
Sustained-Release

Systemic

antineoplastic Cancer,

drugs,

hormones biotherapeutics
corticosteroids,
drug

Solubilization

depot in the lungs

Amphotericin B, minoxidil Fungal infections,

Accumolation

Prostaglandins

Cardiovascular
diseases

MICROSPHERES AS DRUG
DELIVERY SYSTEM

DEFINATION

Microspheres can be defined as solid, approximately

spherical particles ranging in size from 1 to 1000 m.

Made up of polymeric, waxy, or other protective

materials such as starches, gums, proteins, fats, and
waxes and used as drug carrier matrices for drug
delivery.
Microcapsules: micrometric reservoir systems
Microspheres: micrometric matrix systems.

Natural polymer can also be used:

Albumin
Gelatin

= Polymer Matrix
Drug Core
Polymer Coat
MICROCAPSULES

} = Entrapped Drug
MICROSPHERES

Microspheres are essentially spherical

in shape, whereas, microcapsules may be spherical or non-spherical
in shape.
Microparticles, either microcapsules
or microspheres, as the same: microcapsules.

ADVANTAGE OF MICROSPHERES

They facilitate accurate delivery of small quantities of potent drug and

reduced concentration of drug at site other than the target organ or tissue.

They provide protection for unstable drug before and after administration,
prior to their availability at the site of action.

They provide the ability to manipulate the in vivo action of the drug,
pharmacokinetic profile, tissue distribution and cellular interaction of the
drug.

They enable controlled release of drug.

Ex: narcotic, antagonist, steroid hormones

POLYMER USED FOR

MICROSPHERES PREPARATIONS
Biodegradable
Lactides &
Glycolides and
their copolymers
Polyanhydrides
Polycynoacrylates

Non-biodegradable
Poly methyl
methacrylate
Acrolein
Epoxy Polymer
Glycidyl
methacrylate

PARAMETERS THAT CAN BE

SATISFACTORILY
CONTROLLED

Taste and odour masking

Conversion of oil and other liquids,

facilitating ease of handling

Protection of the drug from the

environment

Delay of volatilisation

Freedom from incompatibilities between

drug and excipients, especially the buffers

Improvement of flow properties

Dispersion of water insoluble substance in

aqueous media

Production of sustained release, controlled

release and targeted medication

METHODS OF PREPARATIONS

Solvent evaporation method

Single emulsion technique
Double emulsion technique

Coacervation phase separation method

Spray drying and spray congealing method

Polymerization method

ROUT OF ADMINISTRATION
Oral delivery
Parenteral delivery

MECHANISMS OF DRUG RELEASE

1.

Degradation controlled monolithic system.

2.

Diffusion controlled monolithic system.

3.

Diffusion controlled reservoir system.

4.

Erodible poly agent system.

APPLICATIONS

Microspheres in vaccine delivery.

Eg ; diphtheria toxoid , tetanus toxoid.

Targeted drug delivery.

Eg ; ocular, eye (cornea).Etc

Controlled release.
Eg ; gi tumors, bone tumors.

Chemoembolization.

Immuno microspheres

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