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A SEMINAR ON

TRANSDERMAL DRUG
DELIVERY SYSTEM
PRESENTED BY:

SHIRODE RAHUL A.
M. Pharm.2nd sem.(2014-2015)

(Department of Pharmaceutics)

R. C. Patel Institute of Pharmaceutical


Education and Research, Shirpur
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CONTENTS
Introduction
Advantages-Disadvantages
Comparison between IV, Oral and TDDS
Anatomy and Physiology of Skin
Permeation of Drug Molecule through Skin
Percutaneous Absorption
Classification of TDDS
Basic components of TDDS
Factors affecting Transdermal Permeation
Evaluation of TDDS
Application
Marketed Product
Conclusion
References.

INTRODUCTION
TDDS

are
topically
administered
medicaments in the form of patches that
deliver drugs for systemic effects at
predetermined and controlled rate.
Transdermal patch is an adhesive patch, that
has a coating of medicine (drug), that is
placed on the skin to deliver specific dose of
the medicine, into the blood over a period of
time.

ADVANTAGES
Avoidance of first-pass effect,
Long duration of action,
Comparable characteristics with IV infusion,
Ease of termination of drug action,

if

necessary,
No interference with gastric and intestinal
fluids,
Suitable for administered of drug havingVery short half-life, e.g. nitroglycerine.
Narrow therapeutic window.
Poor oral availability.
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DISADVANTAGES
Poor diffusion of large molecules,
Skin irritation,
Requires high drug load,
Unsuitable If drug dose is large,
Absorption efficiency is vary with different

sites of skin,

COMPARISON BETWEEN IV,ORAL AND TDDS


ADVANTAG
ES

IV

ORAL

TDD

Avoid hepatic
first-pass
effects

YES

NO

YES

Constant drug
levels

YES

NO

YES

Selfadministration

NO

YES

YES

Termination of
therapy

NO

YES

YES

ANATOMY AND PHYSIOLOGY OF SKIN

Skin is the part of Integrated system i.e.

it helps to maintain body temp and protect


It from surrounding environment.
It covers an area of about 2m2 and 4.5-5
kg i.e. about 16% of total body weight in
adults.
Thickness is in range of 0.5mm (on
eyelids ) to 4.0mm ( on heels ).

Skin has mainly 3 layers


1)Epidermis
Stratum
Stratum
Stratum
Stratum

Cornium
Granulosm
Spinosum
Basal

2)Dermis
3)Subcutaneous layer

EPIDERMIS
Stratum Cornium- consists of 25 to 30
layers of flattened dead keratinocytes. Which
makes it water repellent.
Stratum Granulosm- consists of 3 to 5
layers and under goes Apoptosis. It contains
granules known as Keratohyalin. These
granules release Lipid rich secretion, which
acts as the water repellent.
Stratum Spinosum- contains 8 to 10 layers
of cells and it is closely arranged.
Stratum Basal- consists of single layer of
cubical or columnar keratinocytes.

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DERMIS
Composed of strong connective

tissue
containing collagen and elastic fibres, hence it
can easily stretch and recoil easily.
Blood vessel, nerves gland and hair
follicles are embedded in this layer.

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SUBCUTANEOUS LAYER
It is also called as Hypodermis.
It is made up of loose connective tissue,

including Adipose tissue.


This helps to insulate the body by monitoring
heat gain and heat loss.
The dermis is the layer of tissue that is
Deeper and Thicker than epidermis.

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PERMEATION OF DRUG MOLECULE THROUGH


SKIN

It express by Ficks first law of Diffusion-Drug

molecule diffuse from a region of higher conc.


to one of lower conc. until equilibrium is
attained.
The process of Diffusion of molecule is driven

by gradient between high concentration to


low concentration.

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Ficks First law of Diffusion-

dm/dt = J = D A K/h
Where,

dm / dt =J= study state flux


D = diffusion coefficient
A = surface area
K = partial coefficient between

the
Stratum
corneum and the vehicle
h
=
diffusional path length or
membrane
thickness

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PERCUTANEOUS ABSORPTION

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Percutaneous absorption done by 2-

waysA. Transepidermal Absorption


Stratum
Corneum

Intracellular
Pathway

Intercellular
Pathway
Viable Epidermis
Dermis
Microcirculation

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B. Transfollicular Absorption

Pilosebaceous
unit
Hair Follicles

Eccrine Gland

Sebaceous
Gland

Dermis

Microcirculation

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CLASSIFICATION OF TDDS
A. Rate-

.
.
.
.

Programmed
Systems
Drug in Reservoir
Drug in Matrix
Drug in Adhesive
Drug in
Microreservoir

B. Physical StimuliActivated Systems


Structure-Based
Systems
Electrically-Based
Systems
Iontophoresis
Electroporation
Sonophoresis

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A.RATE-PROGRAMMED SYSTEMS1.Drug in Reservoir

2.Drug in Matrix

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3.Drug in Adhesive

4.Drug in Microreservoir

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B. Physical Stimuli-Activated Systems1. Iontophoresis-

2. Electoporation-

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3. Sonophoresis-

4.Microneedles-

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BASIC COMPONENTS OF TDDS


Polymer matrix / Drug reservoir
Drug
Permeation enhancers
Pressure sensitive adhesive (PSA)
Backing laminate
Liner

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Polymer matrix / Drug reservoirNatural Polymer

Synthetic Elastomer

Synthetic Polymer

Gelatin

Neoprene

Polyethylene

Gum Arabic

Silicone rubber

Polystyrene

Starch

Butyl rubber

PVC

Shellac

Chloroprene

PVP

zein

Polysiloxane

Polyster

Penetration EnhancersChemical Enhancers-eg.- Azone, Pyrrolidone,


Fatty acids,
solvents

Essential

oils,

terpenes,

organic

Physical Enhancers-eg.- Iontophoresis,


electroporation, Microneedles
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Pressure Sensitive Adhesives (PSA) A PSA is a material that helps in maintaining an

intimate contact between transdermal system and


the skin surface.
Some widely used pressure sensitive adhesives
are Eg- Polyisobutylenes, Polyacrylates, Silicones.

Backing Laminate:
Hold and protect the drug reservoir from exposure

to atmosphere.
Avoid loss of drug
Accept printing
High flexibility
Eg- vinyl, polyethylene and polyester films, aluminium
foil,
foam pad, metallic plastic laminate.
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LinerProtects the patch during storage. The liner is

removed prior to use. Drug Drug solution in


direct contact with release liner.

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FACTORS AFFECTING
TRANSDERMAL PERMEATION
Physicochemical

property

of

Drug

of

Drug

molecule,

Partition co-efficient,
pH Condition,
Drug Concentration,
Molecular weight.

Physicochemical

property

Delivery System,
Release

characteristics,
Use of permeation enhancer,
Composition of Drug Delivery System.

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Pathophysiological condition of Skin,


Reservoir effect of Horney Layer,
Hydration of skin,
Lipid Film,
Skin Temperature,
Pathological Injury to Skin,
Regional variation.

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Evaluation of TDDS
1. Evaluation of Adhesive
a. Peel Adhesion Properties- It is the force
required to remove coating from a test substrate.
b. Tack Properties- It is the ability of polymer to
adhere to a substrate with little contact pressure.
Thumb tack test

Rolling ball tack test

Quick-Stick test

Probe tack test


c. Shear Strength Properties- It is the
measurement of the cohesive strength of an
adhesive polymer.
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In vitro drug release evaluation


A. In vitro Permeation StudiesIn-Vitro skin Diffusion cells,
Skin-stripping,
Autoradiography.

B. In vitro Release StudiesPaddle Over Disc Apparatus (USP Apparatus 5),


Reciprocating Disc (USP Apparatus 7).

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In vivo evaluation
Animal models,
Skin-Stripping In vivo,
Microdialysis,

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APPLICATIONS
For treatment of Angina Pectoris,
Smoking cessation(Nicotine Patch),
Contraceptive,
Antiemetic,
Anti-inflammatory,
Cosmetics.

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MARKETED PRODUCT
DRUG

BRAND NAME

MANUFACTURER

Nicotine

Nicoderm

gsk

Nicotine

Habitraol

Novartis

Nitroglycerine

Transderm nitro

Novartis

Insulin

SonoDerm

Imarx

Testosterone

Testoderm

Alza Corporation

Diclofenac diethyl
amine

NuPatch 100

Zudus Cadilla

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CONCLUSION
As we know, the basic functions of the skin is

protection and hence it is difficult to target


the skin for drug delivery. Because skin having
numerous layers. But using novel techniques
in TDDS we have successfully penetrate the
drug into systemic circulation.

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REFERENCES
Brahmankar D. M., Jaiswal Sunil B.(2009)

Biopharmaceutics and PharmacotherapeuticsA Treatise, 2nd edition, pp-495-501.


Chien

Yie W.(2002), Novel Drug Delivery


Systems, Marcel Dekkar, Inc Publication,
volume-50, 2nd edition, pp-301.

Walters Kenneth A.(2002), Dermatological and

Transdermal Formulations, Marcel Dekkar, Inc


Publications, volume-119, pp-1,319.
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Roberts Michael s., Walters Kenneth A.(2002),

Dermal Absorption and Toxicity Assessment,


Marcel Dekker, Inc Publications, volume-91, pp-1,
189.
Dr.

Patel Upendra, Bhavin Bhimani(2012)


Transdermal Drug Delivery System As Prominent
Dosage Form For The Highly Lipophilic Drugs.
International Journal Of Pharmaceutical Research
And Bio-Science. Volume 1(3)42:65. pp- 1-6.

Jain, N.K. (1997) Controlled and novel drug

delivery. 1st ed. New Delhi: CBS publishers and


distributors, pp. 100- 127.
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