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

ROUTE OF ADMINISTRATION

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

Intravenous also popularly known as I.V. which is given directly into a vein with injection.

Intra-arterial is given into an artery through injection, e.g. vasodilator drugs such as Sodium Nitroproside, Methyl Dopa etc.

Intra-muscular injection given to the muscular part of the body.

Intrathecal: Drug is direcly administered in to the spinal cord

 Intraosseous infusion: Into the bone marrow

 ADVANTAGES OF PARENTERAL ADMINISTRATION: 

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) 

DISADVANTAGE OF PARENTERAL ADMINISTRATION

Less safe, more expensive. Inconvenient (painful) for the patient. Self medication is difficult. Chances of local injury at the site of injection. It is difficult to reverse its physiological effect

.

COMPARISON:Parenteral route Enteral route

1. The term “Parenteral” comes from two Greek words-‘ Para’ (outside) & ‘Enteron’ (intestine), meaning outside the intestine.

1. The term’ Enteral’ comes from one Greed words- ‘Enteros’ (intestine), meaning the intestine.

2. It’s mechanism of drug absorption is for most drugs is passive transfer (eg.- ‘Levodoa’ follows carrier mediated transport).

2. It’s mechanism of drug absorption is for most drugs is active transfer.

3. Drug can be directly enters systemic circulation.

3. Drug can’t directly enters systemic circulation

4. Does not have 1st pass metabolism.

4. Does have 1st pass metabolism.

5. Onset of action is faster. 5. Onset of action is slower.

6. Drug can be given unconscious & uncooperative patients.

6. Drug can’t be given unconscious & uncooperative patients.

7. Polor drug can be given as they are absorbed ( eg.- Streptomycin)

7. Polor drug can’t be given as they are absorbed ( eg.- Streptomycin)

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.

BIOTECHNOLOGY:

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 Humanized monoclonal antibody

IgE Asthma

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"

BIOCOMPATIBILTY OF PARENTERAL DOSAGE FORMS:

BIOAVAILABILITY AND PARENTERAL DOSAGES FORMS VS ORAL DOSAGE FORMS :

LIPOSOME

A liposome is 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 for cancer and 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 Company Indication

Liposomal amphotericin B

Ambisome Gilead SciencesFungal and protozoal infections

Liposomal IRIV vaccine

Epaxal Crucell Hepatitis A

Liposomal IRIV vaccine

Inflexal V Berna Biotech Influenza

Liposomal vincristine

Marqibo Spectrum Pharmaceuticals

Acute Lymphoblastic Leukemia (ALL) and Melanoma

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: Liposome Utility Current Applications Disease States

Treated

Sustained-Release Systemic antineoplastic

drugs, hormones

corticosteroids, drug

depot in the lungs

Cancer,

biotherapeutics

Solubilization 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 μm.

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

.

Drug CorePolymer Coat

= Polymer Matrix

} = Entrapped Drug

MICROCAPSULES 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• Polycynoacrylate

s

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

Thank

you……