Transdermal Drug

Delivery System

Ankit Keshari
Pharm d 3rd Year
TRANSDERMAL DRUG DELIVERY
SYSTEM
Transdermal Drug Delivery Systems are self contained, discrete
dosage from which when applied to the intact skin, deliver
the drug through skin at a controlled rate to systemic circulation.
 Advantages of Transdermal Drug Delivery System
• Avoids first pass metabolism.

• Reduced inter and intra-patient variability.

• Drug levels can be maintained in the systemic circulation, within the
therapeutic window for prolonged periods of time. So, frequency of dosing
can be reduced.
• Improved patient compliance and acceptability of drug therapy.
• Drug input can be terminated simply by removal of the patch.
• Allow utilisation of drugs with short half lives.
 Disadvantages of Transdermal Drug Delivery
System

• Can be used only for drugs those which requires small plasma concentration
for action (<5mg/day).
• Skin irritation, contact dermatitis may happen due to formulation.

• Enzymes in the epidermis may denature the drugs.

• Expensive
• Toxicity due to dose dumping.
Drug Component
Ideal properties of drug for transdermal drug delivery systems are

Physicohemical properties
⯈The drug should have a molecular weight less than approximately 1000 daltons.
⯈The drug should have affinity for both-lipophilic and hydrophilic phases.
⯈The drug should have a low melting point.

Biological properties
⯈The drug should be potent with a daily dose of the order of a few mg/day.
⯈The half life (t1/2) of the drug should be short.
⯈The drug must not induce a cutaneous irritant or allergic response.
⯈Drugs which degrade in the GI tract or are inactivated by hepatic first-pass effect are
suitable candidates for transdermal delivery.
⯈Drugs which have to be administered for a long period of time.
Excipients of Transdermal Drug Delivery System

The excipients of transdermal devices include:

1. Polymer matrix or matrices

2. Permeation enhancers
3. Other excipients
Polymer matrix or matrices

• The polymer controls the release of the drug from the device.

• Molecular weight, glass transition temperature and chemical functionality of the

polymer should be such that the specific drug diffuses properly and gets released
through it.

• The polymer should be stable, non-reactive with the drug.

• The mechanical properties of the polymer should not deteriorate when large amounts of
active agent are incorporated into it.

• Natural polymers: Cellulose derivatives, Gelatin.

• Synthetic polymers: Polyvinyl alcohol, Polyurea.
Permeation Enhancers
These are compounds which promote skin permeability by altering the skin as a
barrier to the flux of a desired penetrant.

• These may conveniently be classified under the following main headings

a) Solvents
• These compounds increase penetration by swallowing the polar pathway
and/or by fluidizing lipids.
• Examples include Ethanol, Glycerol.

b) Surfactants
• These compounds are proposed to enhance the transport of hydrophilic
drugs.
• It comprises of a polar head group and the hydrocarbon chain length.
• Anionic surfactants: Sodium lauryl sulphate, Dioactyl sulphosuccinate.
• Nonionic surfactants: Pluronic F127, Pluronic F68.
Other
Excipients
a) Adhesives:

• The fastening of all Transdermal devices to the skin has so far been done by using
a pressure sensitive adhesive which can be positioned on the face of the device
or in the back of the device and extending peripherally.

b) Backing membrane:

• These are flexible and they provide a good bond to the drug reservoir.
• It is impermeable substance that protects the product from leaving the dosage
form through the top.
• Eg. Metallic plastic laminate plate, Aluminium foil disc.
APPROACHES USED IN DEVELOPMENT OF TDDS

1. Membrane permeation controlled system

2. Adhesive dispersion type system
3. Matrix diffusion controlled system
4. Micro reservoir type controlled system.
1. Membrane permeation controlled system.

 In this type of system, the drug reservoir is 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 such as silicon fluid to form a paste like
suspension.

 Polymeric membrane may be microporous or non porous with a defined drug permeability property.

 A thin layer of drug compatible, hypoallergenic adhesive polymer eg. Silicon or polyacrylate adhesive
may be applied to the external surface of the polymer membrane to achieve a contact of the skin
surface.

 Major advantage of this system is controlled release rate of drug.

2. Adhesive dispersion type system
 In this system, the drug reservoir is formulated by directly dispersing the drug in a adhesive polymer.
 The medicated adhesive is then spread by solvent casting or hot melt, on to a flat sheet of drug
impermeable metallic plastic backing.
 Thin layers of non medicated, rate controlling adhesive of specific permeability and constant thickness are
applied to produce an adhesive diffusion controlled delivery system
 3. Matrix diffusion controlled system
 In this type the drug is dispersed homogeneously in a hydrophilic or lipophilic polymer matrix.
 This drug containing polymer disc is fixed onto an occlusive base plate in a compartment fabricated from a drug
impermeable backing layer.
 Instead of applying the adhesive on the face of the drug reservoir, it is spread along with the circumference to
form a strip of adhesive rim.
 Homogeneously mixing the finely ground drug particles with a liquid polymer or a highly viscous base polymer
followed by cross linking of polymer chains.
 Now the drug and polymer are dissolved in a common solvent followed by solvent evaporation in a mould at high
temperature and vaccum.
 4. Microreservoir type system
 In this type the drug delivery system is a combination of reservoir and matrix dispersion type system
 The drug reservoir is formed by first suspending the drug in an aq. Sol of water soluble polymer and then
dispersing the solution homogeneously in a lipophilic polymer to form thousands of unreachable, microscopic
spheres of drug reservoirs.
 This thermodynamically unstable dispersion is stabalized quickly by immediately cross linking the polymer in
situ by using cross linking agents.
 So formed medicated disc is positioned at centre of the aluminium backing and is surrounded by adhesive rim.
Examples of formulations using Transdermal Drug Delivery System
THANK YOU