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

Volume 6 Issue 3, March-April 2022 Available Online: www.ijtsrd.com e-ISSN: 2456 – 6470

Transdermal Drug Delivery System: A Review

Akshay Kaware1, Prof. Santosh Waghmare2, Dr. Hemant Kamble3
1
Student, Department of Pharmaceutics, 2Professor, Department of Pharmacy, 3Principle,
1, 2, 3
Lokanete Shri Dada Patil Pharate College of Pharmacy, Mandavgan Pharate, Shirur, Maharashtra, India

ABSTRACT How to cite this paper: Akshay Kaware |

Although transdermal drug administration has made a significant Prof. Santosh Waghmare | Dr. Hemant
contribution to medical practise, it has yet to realise its full potential Kamble "Transdermal Drug Delivery
as an alternative to oral drug delivery and hypodermic injections. The System: A Review"
patch can essentially provide a controlled release of the medication Published in
International Journal
into the patient, usually through either a porous membrane covering a
of Trend in
reservoir of medication or through body heat melting thin layers of Scientific Research
medication embedded in the adhesive, which is an advantage of and Development
transdermal drug delivery over other types of delivery systems such (ijtsrd), ISSN: 2456- IJTSRD49639
as oral, topical, intravenous, intramuscular, and so on. The clinical 6470, Volume-6 |
usage of first-generation transdermal delivery systems for the Issue-3, April 2022, pp.857-862, URL:
delivery of tiny, lipophilic, low-dose medicines has increased www.ijtsrd.com/papers/ijtsrd49639.pdf
steadily. Chemical enhancers, non-cavitational ultrasound, and
iontophoresis have all been used in second-generation delivery Copyright © 2022 by author (s) and
methods. International Journal of Trend in
Scientific Research and Development
KEYWORDS: Study of Transdermal Drug Delivery System, Journal. This is an
Approches of Transdermal Patches, Recent Advances in Transdermal Open Access article
Patches distributed under the
terms of the Creative Commons
Attribution License (CC BY 4.0)
(http://creativecommons.org/licenses/by/4.0)

INTRODUCTION B. Can be used to replace oral pharmaceutical

TRANSDERMAL DRUG DELIVERY SYSTEM: delivery when the route is not suitable, such as
Transdermal delivery systems (TDS) or transdermal in the case of vomiting or diarrhoea.
therapeutic systems are topical formulations
C. To prevent the first-pass effect, such as with
comprising medicines with systemic effect (TTS).
Transdermal Nitroglycerin. When taken orally,
The distribution of a medicine through 'intact' skin so
it is rapidly metabolised by the liner.
that it reaches the systemic circulation in sufficient
quantity to be useful following administration of a D. Noninvasive, as opposed to parenteral therapy,
therapeutic dose is known as transdermal delivery. which is inconvenient.
Transdermal systems are appropriate for disorders E. They provided longer therapy with a single
that need to be treated on a long-term basis. As a application, resulting in better compliance than
result, anti-diabetic medicines used for both alternative dosage forms that required more
therapeutic and preventive purposes have been frequent dose administration, such as
investigated transdermally. transdermal clonidine 7 day.
Advantages: F. The activity of medications with a short half-
A. Prevents gastrointestinal medication absorption life is prolonged by the presence of a drug
problems caused by gut pH, enzymatic activity, reservoir in the therapeutic delivery system and
and drug interactions with food, drink, and its controlled release. g) Drug therapy may be
other orally administered drugs. necessary.

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Figure 1: Anatomy of Skin

Disadvantages: studies in the domain of penetration enhancement
A. Contact dermatitis from one or more of the have been done in recent years3. Slow penetration
system components causes contact dermatitis at rates, a lack of dosage flexibility, and a restriction to
the application site, prompting termination 1. relatively low dosage medicines are all drawbacks. 4.
B. Because of the natural limits of drug entrance Human skin is made up of three separate but
imposed by the skin's impermeability, only interdependent tissues.
powerful medicines are suitable candidates for
PRINCIPLES OF TRANSDERMAL
transdermal patch.
PERMEATION:
C. Some medications, such as the scopolamine
Previously, skin was thought to be an impenetrable
transdermal patch worn behind the ear, are
protective barrier, but subsequent research has
unpleasant.
demonstrated the value of skin as a route for systemic
D. It's difficult to stick to a long period of time.
administration. Because only a fraction of a
ANATOMY AND PHYSIOLOGY OF SKIN: millimetre of tissue separates the surface of the skin
The skin has evolved into a highly effective barrier from the underlying capillary network, it is the most
that inhibits both excessive water loss and xenobiotic intensive and easily accessible organ in the body. The
invasion. It gives us the ability to tolerate a wide following are the numerous processes involved in
range of environmental difficulties. The reasons drug transport from the patch to the systemic
behind this are numerous, but for the sake of this circulation: 5: 1. Drug diffusion from the drug
chapter, they can be stated briefly. Almost all reservoir to the rate-regulating membrane. 2. Drug
substances have a rate-controlling barrier in the diffusion from the rate-limiting membrane to the
stratum corneum, which is the outer layer of the skin. stratum corneum. 3. Sorption through the stratum
Corneocytes, which are dead, flattened, keratin-rich corneum and penetration through the epidermis that is
cells, make up this structure. still alive. 4. Drug uptake by the dermal papillary
These packed cells are surrounded by a complicated layer's capillary network. 5. Impact on the organ of
intercellular lipid combination. Ceramides, free fatty interest
acids, cholesterol, and cholesterol sulphate are among KINETICS OF TRANSDERMAL
them. The fact that they are organised into categories PERMEATION:
is the most crucial characteristic. The ability to understand skin penetration dynamics is
(1.4 g/cm2 in dry state) and low moisture of 15 to 20 critical for the creation of successful transdermal
percent, the skin, particularly the stratum corneum, medicinal devices. The steps involved in transdermal
acts as a barrier to medication penetration. The barrier penetration of a medication are as follows:
function is aided further by the replacement of the 1. Sorption through the stratum corneum 2. Drug
stratum corneum on a regular basis, lowering topical penetration through the epidermis. 3. Drug uptake in
and transdermal absorption. As a result, various the dermal papillary layer via the capillary network.

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Only if the medicine has specific physiochemical generally constant over the period of skin permeation,
qualities will it be able to permeate the body. The rate the rate of skin permeation is constant. The drug
of permeation across the skin is calculated as follows: should be released from the device at a rate Rr, which
dQ/dt = Ps (Cd– Cr), where Cd and Cr are the is either constant or greater than the rate of skin
concentrations of the skin penetrant in the donor uptake Ra, i.e. Rr >> Ra, to keep Cd constant. Since
compartment, i.e. the stratum corneum surface, and Rr > Ra, the drug concentration on the skin is higher.
the receptor compartment, i.e. the body, respectively.
BIOPHARMACEUTICA L PARAMETERS IN
Ps is the skin tissue's total permeability coefficient to
TRANSDERMAL PATCH 7 DRUG
the penetrant. The permeability coefficient is
SELECTION:
calculated using the
The dose should be kept modest, around 20mg per
For a skin penetrant, the coefficient Ps can be day. The half-life should be shorter than 10 hours.
assumed constant. It is obvious from the preceding The molecular weight of the compound should be
equation that a constant rate of drug permeation can 400. The partition coefficient should be between 1.0
be achieved only when Cd >> Cr, that is, when the and 4 Log P (octanolwater). The permeability
drug concentration at the stratum corneum's surface coefficient of the skin should be 0.5 X 103cm/h. The
Cd is continuously and significantly more than the drug should not irritate or sensitise the skin in any
drug concentration in the body Cr. dQ /dt= Ps Cd way. Bioavailability in the mouth should be low. The
becomes the equation. If the magnitude of Cd is therapeutic index should be as low as possible.
APPROACHES USED IN DEVELOPMENT OF TRANSDERMAL PATCH5:

Figure 2 Types of TDDS

A. Membrane moderated systems:
In this, the drug reservoir is totally encapsulated in a
shallow compartment molded from a drug
impermeable metallic plastic laminate and a rate
controlling polymeric membrane. In the drug
reservoir compartment, the drug solids are either
dispersed in a solid polymer matrix or suspended in
an unleachable, viscous liquid medium e.g. silicon
fluid. The rate controlling membrane can be micro
Figure 3 Representation of Membrane
moderated systems

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A skin layer of medication, suitable hypo allergic The absence of dosage dumping, direct exposure of
sticky polymer, or a porous or nonporous polymeric polymeric matrix to the skin, and lack of adhesive
membrane e.g. ethylene vinyl acetate copolymer on interference are all advantages of matrix patches.
the external surface of the polymeric membrane may
D. Microreservoir system
be applied to produce an intimate contact of TDDS
with the skin surface. TransdermNitro is a once-daily
system; TransdermScop is a three-day medicine
system; Catapres TTS is a weekly treatment system.
B. Adhesive diffusion controlled system:

Figure 6 Representation of microreservoir

system
These are classified as a mix of reservoir and matrix
dispersion. The drug reservoir is created by
Figure 4 Representation of adhesive diffusion
suspending the drug particles in an aqueous solution
controlled system
of a water soluble polymer and then homogeneously
It's the most basic version of membrane-moderated dispersing the drug suspension in a lipophilic polymer
drug delivery devices. The drug reservoir is created in using high shear mechanical force to form
this technique by dispersing the drug directly in an unleachable microscopic spheres of drug reservoir.
adhesive polymer and then solvent casting the This dispersion is quickly stabilised by cross linking
medicated adhesive onto a flat sheet of drug the polymer chains, resulting in a medicated disc with
impermeable metallic plastic backing to generate a a consistent surface area and thickness. System that is
thin drug reservoir layer. Layers of nonmedicated rate marketed: Nitrodisc®
regulating sticky polymer of consistent thickness are
ADVANCES IN THE FIELD OF
put on top of the reservoir layer. Single-layer or
TRANSDERMAL PATCHES RECENTLY:
multi-layer drug-in-adhesive patches are available.
There have been several research projects in this
The multi layer system differs from the single layer
sector, and just a few are now underway.
method in that it includes an additional layer of drug-
in-adhesive, normally separated by a membrane. Due The following are some of the most recent studies in
of the convenience of remembering once weekly, the realm of transdermal patches:
pharmacological characteristics in adhesive patches Protein delivery via patch technology:
may account for increased patient compliance. Large amounts of medication can be delivered
C. Matrix dispersion: through the skin. The skin's living tissues, diffusing
across a strong concentration gradient8.
Pain-free diabetic monitoring using transdermal
patches:
The initial prototype patch is around 1cm in diameter
and is constructed of polymers and thin metallic
sheets. The 55 sampling array, as well as their
metallic connectors, can be seen clearly. When the
skin's seal is broken, the interstitial fluid and the
Figure 5 Representation of matrix dispersion biomolecules it contains become visible on the skin's
The drug reservoir is created by dispersing the drug surface. A high-temperature heat pulse can be applied
particles uniformly in a hydrophilic or lipophilic locally, breaching the stratum corneum, using
polymer matrix, and then moulding the medicated microheating devices embedded into the structural
polymer into a disc with a predetermined area and layer of the patch nearest to the skin surface. The skin
thickness. The adhesive polymer is dispersed along surface is exposed to temperatures of 130°C for 30
the circumference of the disc to produce a stripe of milliseconds during this ablation procedure. The
adhesive rim around it, and it is attached onto an temperature rapidly drops from the skin's surface, yet
occlusive base plate on the disc's surface. neither the live tissue nor the nerve endings are
impacted. This painless and bloodless procedure

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causes a 40–50m diameter section of the brain to be lidocaine 5 percent patch used to treat postherpetic
disrupted. neuralgia. The ETrans fentanyl HCl patch is another
promising innovation in pain management. This
Testosterone transdermal patch system in young
credit card-sized patch is an active delivery system
women with spontaneous premature ovarian
with a self-contained battery that administers fentanyl
failure:
HCl, a powerful narcotic, in pulses. This is similar to
In premenopausal women, daily testosterone
the use of intravenous self-controlled analgesia
production is around 300 g, with half coming from
systems, which are expensive, inconvenient, and
the ovaries and half from the adrenal glands. When
require a lot of nursing care11.
compared to normal ovulatory women, young women
with spontaneous premature ovarian failure (sPOF) Absorption enhancers, or chemicals:
may have lower testosterone levels. The Testosterone that help medications pass through the stratum
Transdermal Patch (TTP) was created to mimic the corneum, have been the subject of extensive
normal ovarian testosterone production rate. In investigation. Terpene derivatives, as well as terpenes
women with sPOF, adding TTP to cyclic E2/MPA themselves Some phenols appear to help with
treatment resulted in mean free testosterone levels transdermal absorption. Linalool, alpha terpineol, and
that were close to the upper limit of normal10 carvacrol, for example, have been examined in
Transdermal patch of oxybutynin used in combination with haloperidol (a commonly
prescribed neuroleptic drug). Although all three
overactive bladder:
improved haloperidol absorption, only linalool
The product is a transdermal patch containing
elevated it to a therapeutic level. Limonene,
Oxybutynin HCl that is approved in the United States
and Europe under the brand names Oxytrol and menthone, and eugenol were reported to improve
Kentera. OXYTROL is a thin, flexible, clear patch tamoxifen transdermal absorption. The polyphenol
that is applied twice weekly to the belly, hip, or phloretin improved the absorption of lignocaine.
buttock and delivers oxybutynin in a continuous and Absorption enhancement research has generally been
regular manner over a three to four day period. conducted on excised animal skin (pig or rabbit) or
OXYTROL provides OAB. Patient's continued human skin derived from cadavers or plastic surgery
effective bladder control while avoiding some of the procedures12
oral formulation's adverse effects, such as dry mouth Technologies and approaches for the future:
and constipation. However, for the majority of Thermal poration is the process of creating water
patients, these side effects are not bothersome9. channels through the stratum corneum using pulsed
Nanotechnology gaining hold: heat. This method has been utilised to administer
Microneedles are another enhancement that is gaining conventional medications and to extract intestinal
popularity. This method combines the benefits of a fluid glucose from human subjects. 8,13.
needle and a transdermal patch in one device. The Jet injectors are getting a lot of attention these
gadgets are dime-sized polymer chunks with days, which is leading to better device design for
hundreds of hollow microneedles ranging in length controlled, needle-free injection of medication
from 100 to 1,000 micrometres. These tiny needles solutions across the skin and into deeper tissue.
pierce the top layers of skin, allowing the medication Morphine has been delivered to humans using this
to easily pass through. This technology can be used in
method. A small needle is placed a few
conjunction with an electrically controlled
millimetres into skin, and drug solution is
micropump that distributes the medicine at
pumped via the needle into the skin at controlled
predetermined intervals or on demand. These devices,
rates using a microinfusion pump contained
once approved by the FDA, would allow the patient
within a big patch fastened to skin.
or physician to manage the time and dose of the drug
being given. These devices have the ability to Several explanations have been proposed
precisely deliver medications in the area where throughout the last decade. nonpainful, safe and
particular immune cells reside, allowing these effective alternative to current intramuscular or
treatments to modulate the immune system. subcutaneous vaccination methods
Pain treatment: Altea Therapeutics is currently in clinical
Transdermal patch technology is frequently used for development of a transdermal patch designed to
pain relief. The Duragesic patch is well-known to the address a major unmet need by preventing ‘off’
majority of readers. There are a slew of others on the periods and provide an improved therapeutic
market right now. One of these is Lidoderm, a option for managing Parkinson’s disease.

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Conclusion: Parameters in Drug Selection and Loading of
In above study we studied principles, kinetics of Transdermal Drug Delivery. Indian Journal of
Transdermal Permeation. Also, we studied Pharmaceutical Sciences. 2008; 70(1): 94‐96.
parameters, approaches used, development and recent
[8] Levin G, Kornfeld J, Patel Y R, Damon S.
advances in Transdermal patches.
Transdermal Delivery: Success through a Deep
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