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TRANSDERMAL DRUG
DELIVERY SYSTEM
PRESENTED BY:
SHIRODE RAHUL A.
M. Pharm.2nd sem.(2014-2015)
(Department of Pharmaceutics)
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,
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
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.
10
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,
12
13
dm/dt = J = D A K/h
Where,
the
Stratum
corneum and the vehicle
h
=
diffusional path length or
membrane
thickness
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PERCUTANEOUS ABSORPTION
15
Intracellular
Pathway
Intercellular
Pathway
Viable Epidermis
Dermis
Microcirculation
16
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
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2.Drug in Matrix
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3.Drug in Adhesive
4.Drug in Microreservoir
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2. Electoporation-
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3. Sonophoresis-
4.Microneedles-
22
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Synthetic Elastomer
Synthetic Polymer
Gelatin
Neoprene
Polyethylene
Gum Arabic
Silicone rubber
Polystyrene
Starch
Butyl rubber
PVC
Shellac
Chloroprene
PVP
zein
Polysiloxane
Polyster
Essential
oils,
terpenes,
organic
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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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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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
Quick-Stick test
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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.
32
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
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REFERENCES
Brahmankar D. M., Jaiswal Sunil B.(2009)
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