1. 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 1
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
Conclusion
References.
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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,
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 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,
Absorption efficiency is vary with different sites of
skin,
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6. COMPARISON BETWEEN IV,ORAL AND TDDS
ADVANTAGES IV ORAL TDD
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.
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 ).
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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. 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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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.
The dermis is the layer of tissue that is Deeper and
Thicker than epidermis.
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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. until equilibrium is attained.
The process of Diffusion of molecule is driven by
gradient between high concentration to low
concentration.
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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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17. B. Transfollicular Absorption
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Pilosebaceous unit Eccrine Gland
Hair Follicles Sebaceous Gland
Dermis
Microcirculation
18. CLASSIFICATION OF TDDS
A. Rate-Programmed
Systems
Drug in Reservoir
Drug in Matrix
Drug in Adhesive
Drug in
Microreservoir
B. Physical Stimuli-
Activated Systems
Structure-Based Systems
Electrically-Based Systems
Iontophoresis
Electroporation
Sonophoresis
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25. 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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26. Liner-
Protects the patch during storage. The liner is removed
prior to use. Drug – Drug solution in direct contact
with release liner.
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27. FACTORS AFFECTING TRANSDERMAL
PERMEATION
Physicochemical property of Drug molecule,
Partition co-efficient,
pH Condition,
Drug Concentration,
Molecular weight.
Physicochemical property of Drug Delivery
System,
Release characteristics,
Use of permeation enhancer,
Composition of Drug Delivery System.
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28. 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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29. 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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30. In vitro drug release evaluation
A. In vitro Permeation Studies-
In-Vitro skin Diffusion cells,
Skin-stripping,
Autoradiography.
B. In vitro Release Studies-
Paddle Over Disc Apparatus (USP Apparatus 5),
Reciprocating Disc (USP Apparatus 7).
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31. In vivo evaluation
Animal models,
Skin-Stripping In vivo,
Microdialysis,
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34. 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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35. REFERENCES
Brahmankar D. M., Jaiswal Sunil B.(2009)
Biopharmaceutics and Pharmacotherapeutics-A
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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36. Robert’s 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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