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TRANSDERMAL DRUG
DELIVERY SYSTEM
BY MANSOORI MOHAMMAD SHOAIB
REVIEW
LITERATURE
Guidance by Sunil ojha
• CONTENT.
 Introduction
 History
 Advantages and disadvantages
 Classification of tdds
 Types of transdermal patches
 Material employed /Formulation /Components of transdermal patch
 Factors influencing dermal penetration of drugs
 Some fda approved drugs
 Marketed transdermal products
 Transdermal patches available
 Applications
 Conclusion
• INTRODUCTION
 Definition – Transdermal therapeutic systems are
defined as self contained,self discrete dosage
forms ,which when applied to the intact skin
deliver the drug at a controlled rate to the
systemic circulation. A simple patch that you
stick onto your skin like an adhesive bandage,
which utilize passive diffusion of drugs across
the skin as the delivery mechanism.
• HISTORY

 The first Transdermal patch was approved in 1981 to prevent
the nausea and vomiting associated with motion sickness.
 The FDA has approved, till 2003, more than 35 transdermal
patch products, spanning 13 molecules.
 The US Transdermal market approached $1.2 billion in 2001.
It was based on 11 drug molecules: fentanyl, nitroglycerin,
ethinylestradiol, estradiol, nor ethindroneacetate, testosterone,
clonidine, nicotine, lidocaine, prilocaine, and scopolamine.
 Two new, recently approved Transdermal treat products (a
contraceptive patch containing etreat estradiol and nor-
elgestromin, and a patch to treat overactive bladder containing
oxybutynin.)
ADVANTAGES
 Avoids first pass hepatic metabolism.
 Maintains constant blood levels for long
period of time.
 Decrease the dose of administration.
 Decrease unwanted/ side effects.
 Decreases gastro-intestinal side effects.
 Easy to discontinue in case of toxic effects.
 Increased patient compliance.
 Great advantage for patients who are unconscious.
 Provides an ability to modify the properties of biological.
 barriers to improve absorption.
 Relatively large area of application in comparison to buccal/ nasal cavity.

 Drug must have some desirable physico-chemical properties to
penetrate through stratum conium.
 Local irritation at the site of administration may be caused by drug,
adhesive/ other excipients in patch.
 Clinical need must be clearly established.
 The barrier function of skin changes form one site to another, from
person to person and with age.
 Poor skin permeability limits the number of drug that can be delivered in
this route.
 TDD can not deliver ionic drug.
 TDD can not achieve high drug levels in Blood/ plasma.
 Drugs of large molecular size can not be formulated as TDD.
DISADVANTAGES
• 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
 1.lontophoresis
 2.Electroporation
 3.Sonophoresis
• TYPES OF TRANSDERMAL PATCHES
1.Single layer drug in adhesive.
2.Multi layer drug in adhesive.
3.Reservoir.
4.Matrix.
1. Single layer drug in adhesive.
 In this type of patch
the adhesive layer
serves to adhere the
various layers
together, along with
the entire system to
the skin, contain the
drug, and is
responsible for the
releasing of the drug.
The adhesive layer is
surrounded by a
temporary liner and a
backing.
Drug in adhesive
Backing
Drug in adhesive
Liner/Skin
2. Multi layer drug in adhesive.
 The multi-layer drug-in-
adhesive patch is similar to
the single-layer system but it
differs in that it adds another
layer of drug-in-adhesive,
usually separated by a
membrane. One layer is for
immediate release of the drug
and the other is for control
release of drug from the
reservoir. This patch also has
a temporary liner-layer and a
permanent backing. The drug
release from this depends on
membrane permeability and
diffusion of drug molecules.
Backing
Drug in adhesive
Membrane
Drug in adhesive
Liner/Skin
Multi laminate
3. Reservoir.
 Unlike the single-layer and multi-
layer drug-in-adhesive systems, the
reservoir transdermal system has a
separate drug layer. The drug layer
is a liquid compartment containing a
drug solution or suspension that is
separated by the adhesive layer.
The drug reservoir is completely
encapsulated in a shallow
compartment molded from a drug-
impermeable metallic-plastic
laminate, with a rate-controlling
membrane made of a polymer (like
vinyl acetate) on one surface. This
patch is also backed by the backing
layer.
Backing
Drug
Membrane
Adhesive
Liner/Skin
Reservoir
4. Matrix.
 Also known as a
monolithic device, the
matrix system has a
drug layer of a
semisolid matrix
containing a drug
solution or
suspension. The
adhesive layer in this
patch surrounds the
drug layer, partially
overlaying it.
Backing
Adhesive
Drug
Liner/Skin
Matrix
• Materials employed/ Formulation/ Component of
transdermal patch
 1. Polymer matrix/ matrices
 2. The drug
 3. Pressure sensitive adhesives
 4. Permeation enhancers
• 1. Polymer matrix : The polymer is formulated either as a matrix/
reservoir to controls the release of the drug from the device.
• The polymers used in the transdermal drug delivery systems
are:
• 1. Natural polymers
• Cellulose derivatives ,zein, gelatin , shellac ,waxes, proteins
,gums and their derivatives, natural rubber starch etc.
• 2. Synthetic elastomers-
• Poly butadiene, hydrin rubber, poly siloxane siliconerubber,
nitrile, acrylonitrile ,butyl rubber, butadiene Neoprene etc.
• 3. Synthetic polymers-
• Polyvinyl chloride, polyethylene, poly propylene, polyacrylate
,polyamide,polyurea, polyvinyl pyrrolidone, poly methyl
methaacrylate
• 2. Drug:
• For successful development of a transdermal drug delivery, the
following are the desirable properties of a drug.
• Physicochemical properties :
• It is generally accepted that the best drug candidates for
passive adhesive Transdermal patches must be Non-ionic.
• Low molecular weight (less than 1000 Daltons),
• Adequate solubility in oil and water.
Biological properties :
• The half life of the drug should be short.
• Drugs degraded in the GIT or inactivated by the hepatic
first pass are suitable candidates for transdermal drug
delivery.
• Tolerance of drug must not be developed.
• Drugs which are to be administered for long period of
time or which cause adverse effects are suitable.
• 3. Pressure sensitive adhesives:
• These provide good adherence characteristics &
help to secure the transdermal device on the skin
over long period of time.
• The major classes of pressure sensitive adhesives
are :
1. Polyisobutylene based adhesives.
2. Acrylic adhesives.
3. Silicone based adhesives.
• 4. Permeation enhancers:These are the
compounds which promote skinpermeability by
altering the skin as a barrier to the fluxof a desired
penetrant (drug).These are also known as
accelerants.
• Factors influencing dermal penetration
of drugs.
 I.Biological factors:
 1. Skin condition
 2. Skin age
 3. Blood flow
 4. Regional skin site
 5. Skin metabolism
 6. Species difference.
 II.Physicochemical factors:
 1. Skin hydration
 2. Temperature and pH
 3 Diffusion coefficient
 4. Drug concentration
 5. Partition coefficient
 6. Molecular size and
shape.
 7. Solubility, ionization,
M.pt.
• SOME FDA APPROVED
DRUGS
• MARKETED TRANSDERMAL PRODUCTS
• TRANSDERMAL PATCHES AVAILABLE.
1. TRANSDERMAL NICOTINE PATCH
Nicotine Patch helps to give up smoking by relieving the desire to
smoke, and some of the unpleasant effects which smokers
experience when they stop smoking.To successfully become a non-
smoker it is important to understand how Nicorette Patch works.
2. TRANSDERMAL ANALGESIC PATCH
A transdermal analgesic or pain relief patch is a medicated adhesive patch
used to relieve minor to severe pain. There are two primary types of analgesic
patches: patches containing counter irritants, which are used to treat mild to
moderate pain,and patches containing fentanyl.a narcotic used to relieve
moderate to severe pain inopioid-tolerant patients.
3. TRANSDERMAL ANTI DEPRESSANT PATCH
Is a transdermal patch containing the Selegiline, in
smalldoses, is most commonly used in the
treatmentof Parkinson's disease. It is also effective
in higher dosesfor the treatment of major
depressive disorder.The patch "is a matrix
containing three layers consistingof a backing,
an... adhesive drug layer, and a release linerthat is
placed against the skin.
4. TRANSDERMAL VITAMIN B12
PATCH
• APPLICATION OF TDDS.
• For treatment of Angina Pectoris,
• Smoking cessation (Nicotine Patch),
• Contraceptive,
• Antiemetic,
• Anti-inflammatory,
• Cosmetics.
• CONCLUSION
• As we know, the basic functions of the skin is As 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.
• References :
1.] https://biotextiles2017blog.wordpress.com/transdermal-patch/
2]https://www.google.com/url?sa=t&source=web&rct=j&url=http
s://www.slideshare.net/mobile/ArshadKhan63/transdermal-drug-
delivery-system
3]https://www.slideshare.net/mobile/binujass1/transd
ermal-drug-delivery-system-149052116
4]https://www.slideshare.net/mobile/RahulShirode2/tdds-by-
rahul-shirode
5]https://www.slideshare.net/mobile/DanishKurien/transde
rmal-drug-delivery-system-13541191
Thank you

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Transdermal drug delivery system by MANSOORI MOHAMMAD SHOAIB.

  • 1. TRANSDERMAL DRUG DELIVERY SYSTEM BY MANSOORI MOHAMMAD SHOAIB REVIEW LITERATURE Guidance by Sunil ojha
  • 2. • CONTENT.  Introduction  History  Advantages and disadvantages  Classification of tdds  Types of transdermal patches  Material employed /Formulation /Components of transdermal patch  Factors influencing dermal penetration of drugs  Some fda approved drugs  Marketed transdermal products  Transdermal patches available  Applications  Conclusion
  • 3. • INTRODUCTION  Definition – Transdermal therapeutic systems are defined as self contained,self discrete dosage forms ,which when applied to the intact skin deliver the drug at a controlled rate to the systemic circulation. A simple patch that you stick onto your skin like an adhesive bandage, which utilize passive diffusion of drugs across the skin as the delivery mechanism.
  • 4. • HISTORY   The first Transdermal patch was approved in 1981 to prevent the nausea and vomiting associated with motion sickness.  The FDA has approved, till 2003, more than 35 transdermal patch products, spanning 13 molecules.  The US Transdermal market approached $1.2 billion in 2001. It was based on 11 drug molecules: fentanyl, nitroglycerin, ethinylestradiol, estradiol, nor ethindroneacetate, testosterone, clonidine, nicotine, lidocaine, prilocaine, and scopolamine.  Two new, recently approved Transdermal treat products (a contraceptive patch containing etreat estradiol and nor- elgestromin, and a patch to treat overactive bladder containing oxybutynin.)
  • 5. ADVANTAGES  Avoids first pass hepatic metabolism.  Maintains constant blood levels for long period of time.  Decrease the dose of administration.  Decrease unwanted/ side effects.  Decreases gastro-intestinal side effects.  Easy to discontinue in case of toxic effects.  Increased patient compliance.  Great advantage for patients who are unconscious.  Provides an ability to modify the properties of biological.  barriers to improve absorption.  Relatively large area of application in comparison to buccal/ nasal cavity.
  • 6.   Drug must have some desirable physico-chemical properties to penetrate through stratum conium.  Local irritation at the site of administration may be caused by drug, adhesive/ other excipients in patch.  Clinical need must be clearly established.  The barrier function of skin changes form one site to another, from person to person and with age.  Poor skin permeability limits the number of drug that can be delivered in this route.  TDD can not deliver ionic drug.  TDD can not achieve high drug levels in Blood/ plasma.  Drugs of large molecular size can not be formulated as TDD. DISADVANTAGES
  • 7. • 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  1.lontophoresis  2.Electroporation  3.Sonophoresis
  • 8. • TYPES OF TRANSDERMAL PATCHES 1.Single layer drug in adhesive. 2.Multi layer drug in adhesive. 3.Reservoir. 4.Matrix.
  • 9. 1. Single layer drug in adhesive.  In this type of patch the adhesive layer serves to adhere the various layers together, along with the entire system to the skin, contain the drug, and is responsible for the releasing of the drug. The adhesive layer is surrounded by a temporary liner and a backing. Drug in adhesive Backing Drug in adhesive Liner/Skin
  • 10. 2. Multi layer drug in adhesive.  The multi-layer drug-in- adhesive patch is similar to the single-layer system but it differs in that it adds another layer of drug-in-adhesive, usually separated by a membrane. One layer is for immediate release of the drug and the other is for control release of drug from the reservoir. This patch also has a temporary liner-layer and a permanent backing. The drug release from this depends on membrane permeability and diffusion of drug molecules. Backing Drug in adhesive Membrane Drug in adhesive Liner/Skin Multi laminate
  • 11. 3. Reservoir.  Unlike the single-layer and multi- layer drug-in-adhesive systems, the reservoir transdermal system has a separate drug layer. The drug layer is a liquid compartment containing a drug solution or suspension that is separated by the adhesive layer. The drug reservoir is completely encapsulated in a shallow compartment molded from a drug- impermeable metallic-plastic laminate, with a rate-controlling membrane made of a polymer (like vinyl acetate) on one surface. This patch is also backed by the backing layer. Backing Drug Membrane Adhesive Liner/Skin Reservoir
  • 12. 4. Matrix.  Also known as a monolithic device, the matrix system has a drug layer of a semisolid matrix containing a drug solution or suspension. The adhesive layer in this patch surrounds the drug layer, partially overlaying it. Backing Adhesive Drug Liner/Skin Matrix
  • 13. • Materials employed/ Formulation/ Component of transdermal patch  1. Polymer matrix/ matrices  2. The drug  3. Pressure sensitive adhesives  4. Permeation enhancers • 1. Polymer matrix : The polymer is formulated either as a matrix/ reservoir to controls the release of the drug from the device. • The polymers used in the transdermal drug delivery systems are: • 1. Natural polymers • Cellulose derivatives ,zein, gelatin , shellac ,waxes, proteins ,gums and their derivatives, natural rubber starch etc.
  • 14. • 2. Synthetic elastomers- • Poly butadiene, hydrin rubber, poly siloxane siliconerubber, nitrile, acrylonitrile ,butyl rubber, butadiene Neoprene etc. • 3. Synthetic polymers- • Polyvinyl chloride, polyethylene, poly propylene, polyacrylate ,polyamide,polyurea, polyvinyl pyrrolidone, poly methyl methaacrylate • 2. Drug: • For successful development of a transdermal drug delivery, the following are the desirable properties of a drug. • Physicochemical properties : • It is generally accepted that the best drug candidates for passive adhesive Transdermal patches must be Non-ionic. • Low molecular weight (less than 1000 Daltons), • Adequate solubility in oil and water.
  • 15. Biological properties : • The half life of the drug should be short. • Drugs degraded in the GIT or inactivated by the hepatic first pass are suitable candidates for transdermal drug delivery. • Tolerance of drug must not be developed. • Drugs which are to be administered for long period of time or which cause adverse effects are suitable. • 3. Pressure sensitive adhesives: • These provide good adherence characteristics & help to secure the transdermal device on the skin over long period of time.
  • 16. • The major classes of pressure sensitive adhesives are : 1. Polyisobutylene based adhesives. 2. Acrylic adhesives. 3. Silicone based adhesives. • 4. Permeation enhancers:These are the compounds which promote skinpermeability by altering the skin as a barrier to the fluxof a desired penetrant (drug).These are also known as accelerants.
  • 17. • Factors influencing dermal penetration of drugs.  I.Biological factors:  1. Skin condition  2. Skin age  3. Blood flow  4. Regional skin site  5. Skin metabolism  6. Species difference.  II.Physicochemical factors:  1. Skin hydration  2. Temperature and pH  3 Diffusion coefficient  4. Drug concentration  5. Partition coefficient  6. Molecular size and shape.  7. Solubility, ionization, M.pt.
  • 18. • SOME FDA APPROVED DRUGS
  • 19.
  • 21. • TRANSDERMAL PATCHES AVAILABLE. 1. TRANSDERMAL NICOTINE PATCH Nicotine Patch helps to give up smoking by relieving the desire to smoke, and some of the unpleasant effects which smokers experience when they stop smoking.To successfully become a non- smoker it is important to understand how Nicorette Patch works.
  • 22. 2. TRANSDERMAL ANALGESIC PATCH A transdermal analgesic or pain relief patch is a medicated adhesive patch used to relieve minor to severe pain. There are two primary types of analgesic patches: patches containing counter irritants, which are used to treat mild to moderate pain,and patches containing fentanyl.a narcotic used to relieve moderate to severe pain inopioid-tolerant patients.
  • 23. 3. TRANSDERMAL ANTI DEPRESSANT PATCH Is a transdermal patch containing the Selegiline, in smalldoses, is most commonly used in the treatmentof Parkinson's disease. It is also effective in higher dosesfor the treatment of major depressive disorder.The patch "is a matrix containing three layers consistingof a backing, an... adhesive drug layer, and a release linerthat is placed against the skin. 4. TRANSDERMAL VITAMIN B12 PATCH
  • 24. • APPLICATION OF TDDS. • For treatment of Angina Pectoris, • Smoking cessation (Nicotine Patch), • Contraceptive, • Antiemetic, • Anti-inflammatory, • Cosmetics. • CONCLUSION • As we know, the basic functions of the skin is As 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.
  • 25. • References : 1.] https://biotextiles2017blog.wordpress.com/transdermal-patch/ 2]https://www.google.com/url?sa=t&source=web&rct=j&url=http s://www.slideshare.net/mobile/ArshadKhan63/transdermal-drug- delivery-system 3]https://www.slideshare.net/mobile/binujass1/transd ermal-drug-delivery-system-149052116 4]https://www.slideshare.net/mobile/RahulShirode2/tdds-by- rahul-shirode 5]https://www.slideshare.net/mobile/DanishKurien/transde rmal-drug-delivery-system-13541191