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Transdermal Delivery Systems2011

This document discusses transdermal drug delivery systems, including advantages over oral administration, types of patches like drug-in-adhesive and reservoir patches, limitations on drug types, and newer technologies like iontophoresis and microneedles.

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Imam Adi
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68 views

Transdermal Delivery Systems2011

This document discusses transdermal drug delivery systems, including advantages over oral administration, types of patches like drug-in-adhesive and reservoir patches, limitations on drug types, and newer technologies like iontophoresis and microneedles.

Uploaded by

Imam Adi
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPT, PDF, TXT or read online on Scribd
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Transdermal Delivery

Systems
Advantages of Transdermal
Delivery Systems
Reasonably constant dosage can be maintained
(as opposed to peaks and valleys associated
with oral dosage)
First pass metabolism in the liver and GI tract is
avoided
Reduced need for active administration (some
patches can last 7 days)
The patch is noninvasive and dosage can be
stopped by removal
Easy to apply and to monitor
Oral versus Transdermal

EE = Ethinyl Estradiol
Limitations of Transdermal Delivery
Systems

Skin structure poses a barrier on the mw of the drug (< 500


Da)

Usually reserved for drugs which are extremely potent (thus


requiring a dosage of only a few mg).
The largest daily dose of a drug from a patch is the
nicotine patch, with delivers a daily dose of only 21 mg.
The drug must traverse three layers, the stratum cornium, the epidermis, and
the dermis.
Of these, the toughest barrier is the stratum corneum, which consists of 10-25
layers of keratinized cells.
The stratum corneum is the outermost layer of the epidermis and is composed
mainly of dead cells that lack nuclei.
These are sloughed off during the day and replaced by new cells from the
stratum germinativum.
In the stratum corneum is a high proportion of keratin, an
insoluble protein, with a high proportion of disulfide bridges
(from cysteine), and also a high level of glycine and alanine
residues that allow strong H-bonds to neighboring amino
acids.
Types of patches: definitions
Liner: Protects the drug during storage and is
removed prior to use
Drug
Adhesive: Serves to bind the components of the
patch to the skin
Membrane: Controls the release of the drug
from the reservoir in certain types of patches
Backing: Protects the patch from the outer
environment.
Drug in Adhesive
Patches

A system in which the drug is incorporated


directly into the adhesive, rather than into
a separate layer. Usually used for smaller
molecular weight compounds.
These can be either a single layer or multi-
layer.
Sometimes referred to as the matrix type
patch
Schematic Drawing of the Matrix (Drug-in-Adhesive) type
of patch.

Film Backing

Drug/Adhesive Layer

Protective Liner (removed prior to use)

skin
Drug in Adhesive Patches Can Also Have
Additional Layers to Regulate Rate of Drug
Delivery

Link
Reservoir Patches

The reservoir system has a drug layer that


is separate from the adhesive.
Schematic Drawing of the Reservoir type of patch.

Film Backing

Drug Layer

Rate-controlling Membrane

Contact Adhesive

Protective Peel Strip (removed prior to use)

skin
Article illustrating two types of patches can be found at:

http://molinterv.aspetjournals.org/cgi/reprin
t/4/6/308
What kind of drugs can be
incorporated into a patch?
Compounds with low logP will not diffuse
into skin lipids
However, compounds with high logP also
have difficulties, this time associated with
their diffusion out of the stratum corneum.
The accepted range of logP values is
between 1 and 3.
Products on the market, or in development include:

Clonidine
Works as an agonist of adrenaline at the
presynaptic 2 adrenergic
Product name = Catapres-TTS
used to treat hypertension
Ethinylestradiol (EO) and norelgestromin (N)
Product name = Ortho-Evra
Used for Contraception
Type of patch = Drug-in-Adhesive
Frequency of application = weekly
Fentanyl
Product Name = Duragesic
Used for: Analgesia
Type of Patch = Drug-in-Adhesive
Frequency of Application = Weekly
Lidocaine
Product Name = Lidoderm
Used for: analgesia of postherpetic neuralgia
(PHN), a painful condition caused by the
varicella zoster virus (herpes zoster = shingles)
Lidoderm Patch

Type of Patch = Reservoir


Frequency of Application = Daily
Nicotine
Product name = Habitrol, Nicoderm
CQ, Nicotrol, Prostep
Used for: Smoking cessation
Frequency of administration = Daily
Nitroglycerin
Works by producing nitric oxide (NO), which then acts as
a vasodilator
Product Names = Nitro-Dur, Transderm-Nitro
Used for: Angina
Type of Patch = Nitro-Dur is Drug-in-adhesive
Nitrodisc is reservoir
Frequency of administration = Daily
Estradiol
Product Name = Alora, Climara, Esclim,
Estraderm, FemPatch, Vivelle, Vivelle-DOT
Used for: Hormone replacement
Type of Patch: Drug-in-adhesive
Frequency of application = weekly
Estradiol + Norethindrone
Product name = CombiPatch
Used for: Hormone Replacement
Oxybutynin
Works as competitive antagonist of the
muscarinic acetycholine receptor
Product name = Oxytrol
Used for: Overactive bladder (antispasmodic)
Type of Patch: Drug-in-adhesive
Frequency of application = twice a week
Scopolamine
Works as competitive antagonist of acetylcholine
at the muscarinic receptor
Product Name = Transderm Scop
Used for: Motion Sickness
Testosterone
Product Names = Androderm, Testoderm TTS,
Testoderm
Used for: Hypogonadism
Lidocaine + Epinephrine
Product name = Lidosite
Used for: Dermal anesthesia
Type of Patch = Reservoir,
iontophoretic.

Epinephrine acts as vasoconstrictor, thus prolonging the


duration of action of lidocaine (by delaying resorption) at the site
Iontophoretic Patches

Iontophoretic patches use a tiny electrical


current to promote flow of the drug
(usually charged) through the skin.
Iontophoretic Patches
Iontophoretic Patches
Microneedles Patches

Microneedles patches are currently being


explored as mechanisms to deliver
vaccines and larger macromolecules.
Transdermal Vaccine Technology

LINK
The microneedle technology can result in more effective contact of the vaccine
with the antigen-presenting Langerhans cells

The needles can be fabricated to be long enough to penetrate the stratum


corneum, but short enough to not come into contact with nerve endings.

LINK
Assigned Reading
Scheindlin Stanley Transdermal drug delivery: PAST,
PRESENT, FUTURE. Molecular interventions (2004), 4(6),
308-12 (see link in presentation).
Prausnitz, Mark R.; Langer, Robert. Transdermal drug
delivery. Nature Biotechnology (2008), 26(11), 1261-1268
Link
Sieg, A.; Wascotte, V. Diagnostic and therapeutic applications
of iontophoresis. Journal of Drug Targeting, (2009); 17(9):
690-700.
Graduate Students Only: Subedi, R. K. et al. Recent
Advances in Transdermal Drug Delivery. Archives of Pharmal
Research (2010), 33(3): 339-351.
Homework Questions
1. List the advantages of administering drugs via trandermal drug delivery
systems, over administering medications orally.
2. Use diagrams to illustrate the differences between a drug-in-adhesive patch
and a reservoir patch
3. List the limitations on the types of drugs which can be administered by first-
generation transdermal delivery systems. Explain why much of the drug is
wasted, and how this is commercially feasible.
4. Draw the structures of the following drugs and circle the functionalities
capable of ionization at biological pH. Redraw each structure, showing the
predominant charge state at pH = 7.4 (blood pH): Fentanyl, Lidocaine.
5. Explain how second and third generation transdermal devices differ from
first generation and provide examples of each that are in clinical trials.
6. Explain how transdermal delivery of vaccines might elucidate a greater
immune response than conventional methods.

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