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TRANSDERMAL DRUG
DELIVERY SYSTEM
PRESENTED BY-
MONIKA TARGHOTRA
Enroll no. - 00919601112
B.PHARM
1
CONTENTS:
 Introduction
 Advantages-Disadvantages
 Comparison between IV, Oral and TDDS
 Anatomy and Physiology of Skin
 Permeation of Drug Molecule through Skin
 Percutaneous Absorption
 Basic components of TDDS
 Factors affecting Transdermal Permeation
 Evaluation of TDDS
 Application
 Marketed Product
 Conclusion
 References.
2
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.
3
 INTRODUCTION-
 TDDS is a one in which:
 Drug is delieverd by skin portal to systemic circulation
 At a predetermined rate
 At maintained clinically effective conceration
 Over prolonged period of time
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.
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
 It cannot achieve high drug
level in blood or plasma.
 It cannot deliver ionic drugs.
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
7
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.
9
 Skin has mainly 3
layers…
1)Epidermis-
Stratum Cornium
Stratum Granulosm
Stratum Spinosum
Stratum Basal
2)Dermis
3)Subcutaneous layer
10
1.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.
11
2.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.
12
3.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.
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.
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
15
PERCUTANEOUS
ABSORPTION:
16
 Percutaneous absorption done by 2-ways-
A. Transepidermal Absorption
17
Stratum Corneum
Intracellular
Pathway
Intercellular Pathway
Dermis
Microcirculation
 B. Transfollicular Absorption
18
Pilosebaceous
unit
Eccrine Gland
Hair Follicles Sebaceous Gland
Dermis
Microcirculation
BASIC COMPONENTS
OF TDDS:
 Polymer matrix / Drug reservoir
 Drug
 Permeation enhancers
 Pressure sensitive adhesive (PSA)
 Backing laminate
 Liner
19
 Polymer matrix / Drug reservoir-
 Penetration Enhancers-
 Chemical Enhancers-eg.- Azone, Pyrrolidone, Fatty acids,
Essential oils, terpenes, organic solvents
 Physical Enhancers-eg.- Iontophoresis, electroporation,
Microneedles
20
Natural Polymer Synthetic Elastomer Synthetic Polymer
Gelatin Neoprene Polyethylene
Gum Arabic Silicone rubber Polystyrene
Starch Butyl rubber PVC
Shellac Chloroprene PVP
zein Polysiloxane Polyster
 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.
21
 Liner-
 Protects the patch during storage. The liner is removed prior
to use. Drug – Drug solution in direct contact with release
liner.
22
FACTORS AFFECTING
TRANSDERMAL
PERMEATION:
 Physicochemical property of Drug molecule,
 Partition co-efficient,
 pH Condition,
 Drug Concentration,
 Molecular weight.
23
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.
 Probe tack test
c. Shear Strength Properties- It is the measurement of the
cohesive strength of an adhesive polymer.
24
APPLICATIONS:
 For treatment of Angina Pectoris,
 Smoking cessation(Nicotine Patch),
 Contraceptive,
 Antiemetic,
 Anti-inflammatory,
 Cosmetics.
 Transdermal patch of nicotine, which releases nicotine in
controlled doses to help with cessation of tobacco smoking.
Nitroglycerine patches are also sometimes prescribed for the
treatment of Angina
 Clonidine, the antihypertensive drug and ketoprofen, the
non-steroidal anti-inflammatory drug are also available in the
form of transdermal patches
 Transdermal delivery agent for the Attention Deficit
Hyperactivity Disorder (ADHD).
25
MARKETED PRODUCT:
DRUG BRAND NAME MANUFACTURER
Nicotine Nicoderm gsk
Nicotine Habitraol Novartis
Nitroglycerine Transderm nitro Novartis
Insulin SonoDerm Imarx
Testosterone Testoderm Alza Corporation
26
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.
 Transdermal drug delivery system is useful for topical and
local action of the drug. Due to large advantages of the
Transdermal Drug Delivery System and various permeation
enhancers which would significantly increase the number of
drugs suitable for Transdermal drug delivery system, this
system interests a lot of researchers. Transdermal Drug
Delivery System a realistic practical application as the next
generation of drug delivery system.
27
REFERENCES
 Brahmankar D. M., Jaiswal Sunil B.(2009) Biopharmaceutics
and Pharmacotherapeutics-A Treatise, 2nd edition, pp-495-
501.
 Jain, N.K. (1997) Controlled and novel drug delivery. 1st ed.
New Delhi: CBS publishers and distributors, pp. 100- 127.
28

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Transdermal Drug Delivery: An Overview of Skin Permeation and Patches

  • 1. TRANSDERMAL DRUG DELIVERY SYSTEM PRESENTED BY- MONIKA TARGHOTRA Enroll no. - 00919601112 B.PHARM 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  Basic components of TDDS  Factors affecting Transdermal Permeation  Evaluation of TDDS  Application  Marketed Product  Conclusion  References. 2
  • 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. 3
  • 4.  INTRODUCTION-  TDDS is a one in which:  Drug is delieverd by skin portal to systemic circulation  At a predetermined rate  At maintained clinically effective conceration  Over prolonged period of time 4
  • 5. 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. 5
  • 6. 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  It cannot achieve high drug level in blood or plasma.  It cannot deliver ionic drugs. 6
  • 7. 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 7
  • 8. 8
  • 9.  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. 9
  • 10.  Skin has mainly 3 layers… 1)Epidermis- Stratum Cornium Stratum Granulosm Stratum Spinosum Stratum Basal 2)Dermis 3)Subcutaneous layer 10
  • 11. 1.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. 11
  • 12. 2.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. 12
  • 13. 3.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. 13
  • 14. 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. 14
  • 15.  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 15
  • 17.  Percutaneous absorption done by 2-ways- A. Transepidermal Absorption 17 Stratum Corneum Intracellular Pathway Intercellular Pathway Dermis Microcirculation
  • 18.  B. Transfollicular Absorption 18 Pilosebaceous unit Eccrine Gland Hair Follicles Sebaceous Gland Dermis Microcirculation
  • 19. BASIC COMPONENTS OF TDDS:  Polymer matrix / Drug reservoir  Drug  Permeation enhancers  Pressure sensitive adhesive (PSA)  Backing laminate  Liner 19
  • 20.  Polymer matrix / Drug reservoir-  Penetration Enhancers-  Chemical Enhancers-eg.- Azone, Pyrrolidone, Fatty acids, Essential oils, terpenes, organic solvents  Physical Enhancers-eg.- Iontophoresis, electroporation, Microneedles 20 Natural Polymer Synthetic Elastomer Synthetic Polymer Gelatin Neoprene Polyethylene Gum Arabic Silicone rubber Polystyrene Starch Butyl rubber PVC Shellac Chloroprene PVP zein Polysiloxane Polyster
  • 21.  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. 21
  • 22.  Liner-  Protects the patch during storage. The liner is removed prior to use. Drug – Drug solution in direct contact with release liner. 22
  • 23. FACTORS AFFECTING TRANSDERMAL PERMEATION:  Physicochemical property of Drug molecule,  Partition co-efficient,  pH Condition,  Drug Concentration,  Molecular weight. 23
  • 24. 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.  Probe tack test c. Shear Strength Properties- It is the measurement of the cohesive strength of an adhesive polymer. 24
  • 25. APPLICATIONS:  For treatment of Angina Pectoris,  Smoking cessation(Nicotine Patch),  Contraceptive,  Antiemetic,  Anti-inflammatory,  Cosmetics.  Transdermal patch of nicotine, which releases nicotine in controlled doses to help with cessation of tobacco smoking. Nitroglycerine patches are also sometimes prescribed for the treatment of Angina  Clonidine, the antihypertensive drug and ketoprofen, the non-steroidal anti-inflammatory drug are also available in the form of transdermal patches  Transdermal delivery agent for the Attention Deficit Hyperactivity Disorder (ADHD). 25
  • 26. MARKETED PRODUCT: DRUG BRAND NAME MANUFACTURER Nicotine Nicoderm gsk Nicotine Habitraol Novartis Nitroglycerine Transderm nitro Novartis Insulin SonoDerm Imarx Testosterone Testoderm Alza Corporation 26
  • 27. 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.  Transdermal drug delivery system is useful for topical and local action of the drug. Due to large advantages of the Transdermal Drug Delivery System and various permeation enhancers which would significantly increase the number of drugs suitable for Transdermal drug delivery system, this system interests a lot of researchers. Transdermal Drug Delivery System a realistic practical application as the next generation of drug delivery system. 27
  • 28. REFERENCES  Brahmankar D. M., Jaiswal Sunil B.(2009) Biopharmaceutics and Pharmacotherapeutics-A Treatise, 2nd edition, pp-495- 501.  Jain, N.K. (1997) Controlled and novel drug delivery. 1st ed. New Delhi: CBS publishers and distributors, pp. 100- 127. 28