International Journal of Trend in Scientific Research and Development (IJTSRD)

Volume 6 Issue 1, November-December 2021 Available Online: www.ijtsrd.com e-ISSN: 2456 – 6470

A Basic Overview on Transdermal Drug Delivery System

Bachhav Rishikesh Shankar1, Kale Suvarna Bhausaheb2
1
Department of Pharmacology,
2
Department of Pharmaceutical Quality Assurance,
1,2
KCT’S R.G. Sapkal College of Pharmacy, Anjaneri, Nashik, Maharashtra, India

ABSTRACT How to cite this paper: Bachhav

Transdermal drug delivery system(TDDS) are topically administered Rishikesh Shankar | Kale Suvarna
medication. Transdermal drug delivery is the system in which the Bhausaheb "A Basic Overview on
delivery of one or more active ingredient of the drug to the system Transdermal Drug Delivery System"
circulation after passing through the skin. The Transdermal drug Published in
International Journal
delivery system has been one of the most innovative and
of Trend in
sophisticated approches of drug deliveries. Transdermal drug Scientific Research
delivery system has attracted considerable attention because of its and Development
many potential advantages, improve bioavailability, controlled (ijtsrd), ISSN: 2456-
absorption, flexibility of the terminating drug administration by 6470, Volume-6 | IJTSRD47975
simply removing patch to the body skin are many more potential Issue-1, December
advantages of Transdermal drug delivery, like better patient 2021, pp.1161-1169, URL:
compliance, hepatic first-pass metabolism and particularly for drugs www.ijtsrd.com/papers/ijtsrd47975.pdf
with short half-lives, reduction in systemic side effects, and sustained
delivery of drug to provide steady plasma profiles, and improve Copyright © 2021 by author(s) and
therapeutic efficacy. International Journal of Trend in
Scientific Research and Development
KEYWORDS: TDDS, Transdermal Patches, Anatomy and Physiology, Journal. This is an
Basic Components of TDDS, Types and Application of TDDS Open Access article
distributed under the
terms of the Creative Commons
Attribution License (CC BY 4.0)
(http://creativecommons.org/licenses/by/4.0)

INTRODUCTION:
Any drug delivery system is aim to provide a Transderm –scop for the treatment or prevention of
therapeutically effective amount of active ingredient nausea and vomiting.[3]
of drug to proper site in the skin and then maintained
ADVANTAGES OF TDDS:
or controlled desired drug concentration. Drug are
Self administration.
administered by various type of routes such as oral,
ocular, topical, transdermal, intramuscular, Improved patient compaliance.
intravaginal, rectal, parentral, nasal etc.[1] Among all Avoidance 1st pass metabolism.
of them, oral route is most common and popular but
this route of administration have some drawback like It reduces systemic drug interaction.
1st pass metabolism, enzymes, drug degradation in It is long duration of action.[4-9]
GIT tract due to PH etc. TDDS is also known as
“patches” or skin patch. TDDS is defined as the self– They are non-invasive, avoiding the
contained discreate dosage forms of patches which inconvenience of parentral therapy.
when applied to the skin deliver the drug, throught the They can avoide GIT drug absorption difficulties
skin portal to systemic circulation at a predetermined covered by GIT PH, drink, enzymatic activity,
and controlled rate over prolonged period of time in drug interaction with food and other orally
order to increase the therapeutic efficacy and reduced administration drug.[10]
side effect of drug.[2]
Avoidance of GIT incompatibility.
In 1965 stoughton 1st conceived of the percutaneous
Enhance therapeutic efficacy.
absorption of drug substance. In 1979 FDA 1st
approved the transdermal system (patches) i.e. End of therapy is easy at any point of time.

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DISADVANTAGES OF TDDS: Many problems such as like itching, edema,
The drug must have some desirable erythema etc. May be seen due to patches.
physicochemical properties for penetration Tdds is not compatible with ionic drugs
throught stratum corneum and if the drug dose
required for therapeutic value is more than It is not use in acute condition, only used in
10mg/day, the transdermal delivery will be very chronic conditions.
difficult. High drug level in blood cannot be attained.[12]
Some patient develop contact dermatitis at the site
The main disadvantages is that high cost, local
of application from one or more of the system
irritation, no rapid, variation in barrier function
components, necessitating discontinuation.[11]
(age, site) etc.[13-17]
Many drugs especially with hydrophilic drugs
cannot pass permeates the skin to slowly may not
achieve therapeutic level.

IDEAL PROPERTIES OF TRANSDERMAL DRUG DELIVERY SYSTEM

TABLE 1: SHOWING IDEAL PROPERTIES OF TRANSDERMAL DRUG DELIVRY SYSTEM.[18]

S. No Properties Comments
1. Shelf life Up to 2 yrs
2. Particle size <40cm2
3. Dose frequency Once in a day or once in a week
4. Aesthetic appeal Clear or white colour
5. Packaging Easy removal of release liner and min.no.of steps required to apply
6. Skin reaction Non irritating and non sensitizing
7. Release Consistent pharmacokinetic and pharmacodynamic profile over time
ANATOMY AND PHYSIOLOGY OF SKIN
Human skin comprises of three but mutually dependent tissues:
Epidermis
Dermis
Hypodermis and subcutaneous layer

Figure 1: Cross sectional view of various epidermal layers, dermis and the subcutaneous.
EPIDERMIS
Epidermis outer layer of the skin is made of stratified squamous epithelial cell.
Epidermis is a thickest area in the palms and soles[19].
Epidermis shows two main parts: 1) stratum corneum 2) stratum germinativum.
Stratum corneum forms the outer layer 10-15 micrometer thick which consist of many layers of compacted,
flattend, dehydrated keratinized cells in stratified layer.

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Keratin contains cells called as corneosites[20, 21].
Stratum corneum layer forms permeability obstacle for outer environment.
Water content of stratum corneum is around 20%.
The moisture required stratum corneum is around 10% (w/w) to maintained flexibility and softness[22].
It consist of cermides and neutral lipids such as sterols free fatty acids and triglyceride.
The stratum corneum is responsible for the barrier function of the skin and behaves as a primary to the
precutaneous absorption[23].
It is made up of three layers in thicker parts stratum granulosum, stratum lucidum, stratum spinousum
figure.1.
Removal of this layers results in increased skin permeability and water loss[24].
DERMIS
Dermis is composed of a regular network of robust collagen fiber and fairly uniform thickness with regularly
spaced cross-straiations.
This network or the gel structure is liable for the flexible properties of the skin.
It is supplied by blood to convery nutrients, remove waste and regulate body temperature.
Drug is well absorbed by this route.
Upper portion of the dermis is formed into ridges containing lymphatics and nerve endings.
HYPODERMIS OR SUBCUTANEOUS LAYER
This is a sheet of the fat containing areolar tissue, known as the superficial fascia, attaching the dermis to the
underlaying structures[20].
BASIC COMPONENTS OF TDDS
1. Polymer matrix or matrices
2. Drug
3. Permeation enhancers
4. Adhesive
5. Liners
6. Backing
7. Plasticizer
1. POLYMER MATRIX OR MATRICES
The polymer controls the drug loading, rate of drug release. The selection criteria should be satisfied for a to be
used in transdermal patches as following.
Chemical and molecular weight functionality of the polymer should be such that the specific drug diffuses
properly and gets released throught it.
The polymer should be stable.
The polymer should be nontoxic.
The polymer should be easily of manufactured.
The polymer should be inexpensive.
The polymer and its degration product must be non toxic or non-antagonistic to the host.
Big amounts of the active agent are incorporated into it.
Types of polymer
A. Natural polymers: Gelatin, shellac, waxes, chitosan, natural rubber, cellulose derivatives.
B. Synthetic polymers: PVA, PVC, polypropylene, polyacrylate, polyurea, polyamide, polypropylene.
C. Synthetic elastomers: Polybutadiene, silicon rubber, hydrine rubber, nitril, acrylonitril, neoprene.
2. DRUG :
The selection drug should have some desirable physiochemical and biological properties favorable for drug
transport across the skin.
Physiochemical properties:
A. The drug should have low mole. Weight (up to 1000 Daltons).

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B. The drug should have affinity for hydrophilic and lipophilic phases.
C. The drug should have a low melting point (less than 200 deg c).
Biological properties:
A. The drug should be potent with a daily dose of a few mg/day in order.
B. The half life (t½) of the drug should be short.
C. The drug must not produce allergic response.
D. Toleration to the drug must not develop under the near zero-order release profile of skin patches.
3. PERMEATION ENHANCER:
These are compounds which promote skin permeability by altering the skin as a obstacle to the flux of a desired
penetrant.
The flux J, can be given by - J = D dc/dx
J = The Flux
D = diffusion coefficient
C = Concentration of the diffusing species
Permeation enhance are hypothesized to affect one or more of these layers to achieve skin penetration
enhancement. A big number of compounds have been investigated for their ability to increaces stratum corneum
permeability. These may be conveniently be classified under the following headings.
A. Solvent: These compound enhance permeability possibly by swelling the polar pathway.
e.g. propylene glycol and Glycerol, water alcohols-methanol and ethanol, Dimethyl acetamide.
B. Surfactant: The ability of a surfactant to alter penetration is a function of both the hydrocarbon chain length
and polar head group.
Anionic surfactant : SLS, Decodecyl methyl sulfonamide, Diacetyl sulphosuccinate.
Nonionic surfactant: pluronic F68, pluronic F127.
Bile salt : sodium deoxycholate, sodium taurocholate.
C. Binary system: These systems apparently open up the heterogenous multilaminate pathway as well as the
continous pathways.
e.g. Propylene glycol-oleic acid and 1,4-butanediol- linoleic acid.
D. Miscellaneous chemicals: These include urea, a hydrating and keratolytics agent;
4. ADHESIVE:
Adhesive maintains the patch in continuous contact with the skin the selection criteria for patch include adhesive
properties e.g. polyisobutadine, polyacrylate.
It should not be irritant.
It should be easily removed.
It should be removable from the smooth surface without leaving a residue.
It should have excellent contact with the smooth surface.
Physical and chemical compatibility with the drug.
Permeation of drug should not effected[25,26].
5. Liner: Protect the patch from outside environment during storage. The linear is removed prior to use e.g.
PVC
6. Backing: It protect the polymeric drug reservoir from the external environment[27].
7. Plasticizers: plasticizer provides flexibility and improves the brittleness of the polymer.
e. g. PEG, PG, phthalic acid ester[28].
TRANSDERMAL PATCH:
Transdermal drug delivery system are tropically administered medicaments. TDDS is defined as medicated
adhesive patch which when applied to the skin to delivery the drug throught the skin at a predetermined and
controlled rate release to reach into the bloodstream. Today the most common transdermal system present in the
market mainly based on semipermiable membranes which were called as patches. TDDS patch shows different
component as following figure. 2[29-32].

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Figure 2: Transdermal patch showing its different components.

Figure 3: Transdermal patch (skin patch)

TYPES OF TRANSDERMAL PATCHES
1. Single-layer drug in-adhesive.
2. Multi-layer drug in-adhesive.
3. Drug reservoir-in-adhesive.
4. Drug matrix-in-adhesive.
SINGLE-LAYER DRUG IN-ADHESIVE
In this system drug is dispersed in the adhesive layer of the skin patch. In this type of patches the adhesive layer
serves to adhere the various layer together and also responsible for the releasing of the drug. The adhesive layer is
surrounded by a temporary backing and a liner.

Figure 4: Single-layer drug in-adhesive

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MULTI-LAYER DRUG IN-ADHESIVE
In this system drug is dispersed in the adhesive layers of the patch same as in single layer drug in adhesive. But
the only difference is that it contains multiple layers of drug in-adhesive separated by a membrane. This patch
also has a temporary liner-layer permanent backing.

Figure 5: Multi-Layer Drug In-Adhesive

DRUG RESERVOIR-IN-ADHESIVE
Reservoir transdermal system has a sepreate drug layer enclosed in a rate controlling microporous or nonporous
membrane and an impermeable backing laminate. The drug layer is a liquid mix compartment containing a drug
suspension or solution sepreated by the backing layer. The release rate of the drug is determined by the
permeability diffusion, abrasion rate and thickness of the membrane. In this type of system the rate of drug release
is zero order.

Figure 6: Drug reservoir in-adhesive

DRUG MATRIX-IN-ADHESIVE
In this approach, the reservoir is prepared by homogenously dispersing drug particles in a lipophilic or
hydrophilic polymer matrix. The adhesive layer in drug matrix patch surrounds the drug layer partially
overlaying it. It also has occlusive base plate, absorbent pad and backing laminate on the back[33-35].

Figure 7: Drug matrix-in-adhesive

APPLICATION OF TRANSDERMAL PATCHES
Nitroglycerine patches are also used in the treatment of angina pectoris.
Transdermal patches of nicotine, which releases nicotine in controlled doses is used in treatment of tobacco
smoking cessation.
Clonidine is antihypertensive drug and ketoprofen, the non-steroidal anti-inflamatory drug are also available
in the form of transdermal patches.
Transdermal delivery agent for the attention deficit hyperactivity disorder (ADHD), Antiemetic,
contraceptive.
Transdermal forms of the MAOI selegilline, became the 1st transdermal delivery agent for an
antidepressant[36-38].
Estrogen patches are sometimes prescribed to treat menopausal symptoms as well as post-menopausal
osteoporosis[39].
TDDS marketed product list as following Table. 2[40].

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TABLE 2: TDDS MARKETED PRODUCTS
Product Name Drug Manufacturer Indication
Alora Estradiol TheraTech/ Proctol and Gamble Postmenstrual Syndrome
Androderm Testosterone TheraTech/GlaxoSmithKline Hypogonadism in Males

Catapres –TTS Alza/ Boehinger Ingelheim Hypertension

Clonidine
Climaderm Estradiol Ethical Holdings/ Wyeth –Ayerest Postmenstrual Syndrome
Climara Estradiol 3M Pharmaceuticals/ Berlex Labs Postmenstrual syndrome
Estradiol/ Nore Hormone replacement
CombiPatch Noven, Inc./ Aventis
thindrone therapy
Deponit Nitroglycerin Schwarz –Pharma Angina pectoris
Duragesic Fentanyl Alza/ Janssen Pharmaceutical Moderate/ severe pain
Estraderm Estradiol Alza/ Norvatis Postmenstrual Syndrome
Ethical Holdings/ Solvay Healthcare
Fematrix Estrogen Postmenstrual Syndrome
Ltd.
FemPatch Estradiol Parke-Davis Postmenstrual Syndrome
Habitraol Nicotine Novartis Smoking Cessation
Minitran Nitroglycerin 3M Pharmaceuticals Angina pectoris
Nicoderm Nicotine Alza/ GlaxoSmithKline Smoking Cessation
Nitrodisc Nitroglycerin Roberts Pharmaceuticals Angina pectoris
Cygnus Inc./ McNeil Consumer
Nicotrol Nicotine Smoking cessation
Products, Ltd.

CONCLUSION Drug Delivery System - Simplified Medication

Transdermal drug delivery system have been used as Regimen - A Review. Research Journal of
safe and effective drug delivery devices since 1981. Pharmaceutical, Biological and Chemical
The purpose of this article was to give precious and Sciences, 2011; 2(4): 223-238.
basic information about the transdermal drug delivery [3] Patel Harunusman, Bhimani Bhavin, Patel Dr.
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Upendra, Patel Ghanshyam. Transdermal drug
convenient and self-administration, pain free for delivery system as prominent dosage forms for
patient. Many more drugs have been formulated in
the highly- Review Article. International
TDDS form, such as hypertention, chronic pain, journal of pharmaceutical research and
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bioscience, 2011; 1(3): 42- 65.
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