2. 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
Reference
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3. 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.
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4. ADVANTAGES
Avoidance of first-pass effect,
Long duration of action,
No interference with gastric and intestinal fluids,
Suitable for administered of drug having-
Very short half-life, e.g. nitroglycerine.
Narrow therapeutic window.
Poor oral availability.
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5. DISADVANTAGES
Poor diffusion of large molecules,
Skin irritation,
Requires high drug load,
Unsuitable –If drug dose is large,
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6. COMPARISON BETWEEN IV,ORAL AND TDDS
ADVANTAGES IV ORAL TDDS
Avoid hepatic
first-pass effects
YES NO YES
Constant drug
levels
YES NO YES
Self-
administration
NO YES YES
Termination of
therapy
NO YES YES
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8. Skin is the part of Integrated system i.e. it helps to
maintain body temp and protect It from
surrounding environment.
Thickness is in range of 0.5mm (on eyelids ) to
4.0mm ( on heels ).
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10. 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.
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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11. 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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12. 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.
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13. PERMEATION OF DRUG MOLECULE THROUGH SKIN
It express by Fick’s first law of Diffusion-Drug
molecule diffuse from a region of higher conc. to one
of lower conc.
Fick’s First law of Diffusion-
dm/dt = J = D A K/h
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14. Fick’s 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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15. Percutaneous absorption done by 2-ways-
A. Transepidermal Absorption Date 17-03-2017
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Stratum Corneum
Intracellular Pathway Intercellular Pathway
Viable Epidermis
Dermis
Microcirculation
16. B. Transfollicular Absorption
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sebaceous unit Endocrine Gland
Hair Follicles Sebaceous Gland
Dermis
Microcirculation
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17. CLASSIFICATION OF TDDS
A. Rate-Programmed
Systems
Drug in Reservoir
Drug in Matrix
Drug in Adhesive
Drug in
Microreservoir
B. Physical Stimuli-
Activated Systems
Iontophoresis
Electroporation
Sonophoresis
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18. 1.Drug in Reservoir
2.Drug in Matrix
A.RATE-PROGRAMMED SYSTEMS-
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• In reservoir system the drug is enclosed between a rate
controlling micro porous or nonporous membrane and
an impermeable backing laminate. The release rate is
zero order process from reservoir system.
• In matrix diffusion system, drug is uniformly dispersed
in hydrophilic or lipophilic polymer material. The rate
of erosion of the polymer, thickness of the layer
&surface area of the film determines the release rate of
drug.
Date 17-03-2017
19. 3.Drug in Adhesive Date 17-03-2017
In this adhesive layer is surrounded by the liner. The
adhesive layer not only serve to adhere the components of
the patch with the skin but also controls the rate of drug
delivery to the skin.
This system can be divided into following parts:-
1.Prepration of individual matrix solution.
2.Coating the individual matrix layers.
4.Drug in Microreservoir
The micro reservoir system is the combination of the matrix and
reservoir system. In micro reservoir system the drug is the first
suspended in an aqueous solution of a hydrophilic polymer
(e.g. PEG)and then the above suspension is mixed with a
lipophilic polymer (e.g. Silicon)
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20. B. Physical Stimuli-Activated Systems-
Iontophoresis- is define as the permeation of ionized drug
molecules across biological membrane under the influence of
electric current.
Electoporation-
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21. 3. Sonophoresis- is a exponentially increase the
absorption of topical compounds(transdermal
delivery) into the epidermis, dermis and appendages
by ultrasonic energy.
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22. BASIC COMPONENTS OF TDDS
Polymer matrix / Drug reservoir
Drug
Backing laminate
Liner
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23. Polymer matrix / Drug reservoir-
Drug
Desirable properties of a drug for tdds
a . Physicochemical properties
b . Biological properties
Natural Polymer Synthetic Elastomer Synthetic Polymer
Gelatin Neoprene Polyethylene
Gum Arabic Silicone rubber Polystyrene
Starch Butyl rubber PVC
Shellac Chloroprene PVP
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24. 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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25. Liner-
Protects the patch during storage. The liner is removed
prior to use. Drug solution in direct contact with
release liner.
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26. FACTORS AFFECTING TRANSDERMAL
PERMEATION
Physicochemical property of Drug molecule,
Partition co-efficient,
pH Condition,
Drug Concentration,
Molecular weight.
Physicochemical property of Drug Delivery
System,
Enhancement of transdermal permeation
Composition of Drug Delivery System.
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27. Pathophysiological condition of Skin,
Hydration of skin,
Skin Temperature,
Pathological Injury to Skin,
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28. Evaluation of TDDS
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1.Determination of surface ph
2.Thickness of patch
3.Weight uniformity
4.Tack properties
a. Thumb tack test
b. Rolling ball tack testing
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29. 1.In-vitro drug release studies
a) paddle over disc method
2.In-vivo drug release
a)Animal model
b)Human model
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30. APPLICATIONS
For treatment of Angina Pectoris,
Smoking cessation(Nicotine Patch),
Contraceptive,
Antiemetic,
Anti-inflammatory,
Cosmetics.
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