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Department of Pharmaceutics
Presented by
MR. ANKIT L SHARMA
Roll No.-05
P.D.E.A’s S.G.R.S college of Pharmacy Saswad.
Date 17-03-2017
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
2
Date 17-03-2017
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
Date 17-03-2017
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.
4
Date 17-03-2017
DISADVANTAGES
 Poor diffusion of large molecules,
 Skin irritation,
 Requires high drug load,
 Unsuitable –If drug dose is large,
5
Date 17-03-2017
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
6
Date 17-03-2017
ANATOMY AND PHYSIOLOGY OF SKIN
7
Date 17-03-2017
 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 ).
8
Date 17-03-2017
 Skin has mainly 3 layers…
1)Epidermis
 Stratum Cornium
 Stratum Granulosm
 Stratum Spinosum
 Stratum Basal
2)Dermis
3)Subcutaneous layer
9
Date 17-03-2017
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.
10
Date 17-03-2017
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.
11
Date 17-03-2017
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.
12
Date 17-03-2017
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
13
Date 17-03-2017
 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
14
Date 17-03-2017
 Percutaneous absorption done by 2-ways-
A. Transepidermal Absorption Date 17-03-2017
15
Stratum Corneum
Intracellular Pathway Intercellular Pathway
Viable Epidermis
Dermis
Microcirculation
 B. Transfollicular Absorption
16
sebaceous unit Endocrine Gland
Hair Follicles Sebaceous Gland
Dermis
Microcirculation
Date 17-03-2017
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
17
Date 17-03-2017
1.Drug in Reservoir
2.Drug in Matrix
A.RATE-PROGRAMMED SYSTEMS-
18
• 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
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)
19
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-
20
Date 17-03-2017
3. Sonophoresis- is a exponentially increase the
absorption of topical compounds(transdermal
delivery) into the epidermis, dermis and appendages
by ultrasonic energy.
21
Date 17-03-2017
BASIC COMPONENTS OF TDDS
Polymer matrix / Drug reservoir
Drug
Backing laminate
Liner
22
Date 17-03-2017
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
23
Date 17-03-2017
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.
24
Date 17-03-2017
Liner-
Protects the patch during storage. The liner is removed
prior to use. Drug solution in direct contact with
release liner.
25
Date 17-03-2017
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.
26
Date 17-03-2017
 Pathophysiological condition of Skin,
 Hydration of skin,
 Skin Temperature,
 Pathological Injury to Skin,
27
Date 17-03-2017
Evaluation of TDDS
28
1.Determination of surface ph
2.Thickness of patch
3.Weight uniformity
4.Tack properties
a. Thumb tack test
b. Rolling ball tack testing
Date 17-03-2017
1.In-vitro drug release studies
a) paddle over disc method
2.In-vivo drug release
a)Animal model
b)Human model
29
Date 17-03-2017
APPLICATIONS
 For treatment of Angina Pectoris,
 Smoking cessation(Nicotine Patch),
 Contraceptive,
 Antiemetic,
 Anti-inflammatory,
 Cosmetics.
30
Date 17-03-2017
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 Zydus Cadilla
31
Date 17-03-2017
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.
32
Date 17-03-2017
THANK YOU………..
33
Date 17-03-2017

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Seminar on tdds

  • 1. Department of Pharmaceutics Presented by MR. ANKIT L SHARMA Roll No.-05 P.D.E.A’s S.G.R.S college of Pharmacy Saswad. Date 17-03-2017
  • 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 2 Date 17-03-2017
  • 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 Date 17-03-2017
  • 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. 4 Date 17-03-2017
  • 5. DISADVANTAGES  Poor diffusion of large molecules,  Skin irritation,  Requires high drug load,  Unsuitable –If drug dose is large, 5 Date 17-03-2017
  • 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 6 Date 17-03-2017
  • 7. ANATOMY AND PHYSIOLOGY OF SKIN 7 Date 17-03-2017
  • 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 ). 8 Date 17-03-2017
  • 9.  Skin has mainly 3 layers… 1)Epidermis  Stratum Cornium  Stratum Granulosm  Stratum Spinosum  Stratum Basal 2)Dermis 3)Subcutaneous layer 9 Date 17-03-2017
  • 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. 10 Date 17-03-2017
  • 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. 11 Date 17-03-2017
  • 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. 12 Date 17-03-2017
  • 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 13 Date 17-03-2017
  • 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 14 Date 17-03-2017
  • 15.  Percutaneous absorption done by 2-ways- A. Transepidermal Absorption Date 17-03-2017 15 Stratum Corneum Intracellular Pathway Intercellular Pathway Viable Epidermis Dermis Microcirculation
  • 16.  B. Transfollicular Absorption 16 sebaceous unit Endocrine Gland Hair Follicles Sebaceous Gland Dermis Microcirculation Date 17-03-2017
  • 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 17 Date 17-03-2017
  • 18. 1.Drug in Reservoir 2.Drug in Matrix A.RATE-PROGRAMMED SYSTEMS- 18 • 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) 19
  • 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- 20 Date 17-03-2017
  • 21. 3. Sonophoresis- is a exponentially increase the absorption of topical compounds(transdermal delivery) into the epidermis, dermis and appendages by ultrasonic energy. 21 Date 17-03-2017
  • 22. BASIC COMPONENTS OF TDDS Polymer matrix / Drug reservoir Drug Backing laminate Liner 22 Date 17-03-2017
  • 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 23 Date 17-03-2017
  • 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. 24 Date 17-03-2017
  • 25. Liner- Protects the patch during storage. The liner is removed prior to use. Drug solution in direct contact with release liner. 25 Date 17-03-2017
  • 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. 26 Date 17-03-2017
  • 27.  Pathophysiological condition of Skin,  Hydration of skin,  Skin Temperature,  Pathological Injury to Skin, 27 Date 17-03-2017
  • 28. Evaluation of TDDS 28 1.Determination of surface ph 2.Thickness of patch 3.Weight uniformity 4.Tack properties a. Thumb tack test b. Rolling ball tack testing Date 17-03-2017
  • 29. 1.In-vitro drug release studies a) paddle over disc method 2.In-vivo drug release a)Animal model b)Human model 29 Date 17-03-2017
  • 30. APPLICATIONS  For treatment of Angina Pectoris,  Smoking cessation(Nicotine Patch),  Contraceptive,  Antiemetic,  Anti-inflammatory,  Cosmetics. 30 Date 17-03-2017
  • 31. 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 Zydus Cadilla 31 Date 17-03-2017
  • 32. 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. 32 Date 17-03-2017