2

3
 Transdermal drug delivery system is defined as self
containing, discrete dosage forms which when applied
to the intact skin,deliver the drugs through the skin at a
controlled rate to the systemic circulation.

 Transdermal delivery represents an attractive alternative

to oral delivery of drugs and is poised to provide an
alternative to hypodermic injection too.

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 Avoid gastrointestinal drug absorption difficulties caused
by gasrtointestinal pH, enzymatic activity, drug
interaction.
 Substitute for oral administration of medication.
 Avoid first pass effect.
 Noninvasive in nature.
 Extended therapy with a single application.
 Improving compliance.
 May be terminated rapidly.
 Easily and rapidly identified in emergencies.

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 Many drugs especially drugs with hydrophilic structures
permeate the skin too slowly may not achieve therapeutic
level.
 The drug, the adhesive or other excipients in the patch
formulation can cause erythema, itching and local
edema.
 The barrier function of the skin changes from one site to
another on the same person, from person to person and
also with age.
 Drug that require high blood levels cannot be
administered
 Adhesive may not adhere well to all types of skin
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Bioactivity of drug

Skin characteristics

Formulation

Adhesion

System design

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 Release of the medicament from the vehicle.
 Penetration through the skin barrier.
› Skin structure and its properties
› The penetrating molecule and its physical-chemical
relationship to skin and the delivery platform
› The platform or delivery system carrying the
penetrant
› The combination of skin, penetrant, and delivery
system
 Activation of pharmacological response.

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o Biological factors –

o Skin condition

o Skin age

o Blood flow

o Regional skin sites

o Skin metabolism

o Species differences

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 Physicochemical factors –
 Skin hydration
 Temperature and pH
 Diffusion coefficient
 Drug concentration
 Partition coefficient
 Molecular shape and size

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11
1.Through stratum
corneum

2.Transfollicular

3.Through sweat
gland

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 The drug

 Polymer matrix

 Permeation enhancers

 Adhesive

 Backing layer.
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The drug is in direct contact with release liner.
 Ex: Nicotine, Methotrexate, and Oestrogen.

 Some of the desirable properties of a drug for

transdermal delivery:

 Should possess an adequate solubility in oil and water.

 Should have a molecular weight less than approximately
1000 daltons.
 Require a balanced partition coefficient to penetrate the
stratum corneum.
 Should have low melting point.
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These polymers control the release of the drug from the
drug reservoir.

 Natural polymers: shellac, gelatin, waxes, gums, starch

etc.

 Synthetic polymers: polyvinyl alcohol, polyamide,

polyethylene, polypropylene, Polyurea, polymethyl
methacrylate.

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 Substances exist which temporarily diminish the
impermeability of the skin are known as accelarants or
sorption promoters or penetration enhancers.

 These include water, pyrolidones, fatty acids and

alcohols, azone and its derivatives, alcohols and glycols,
essential oils, terpenes and derivatives, sulfoxides like
dimethyl sulfoximide and their derivatives, urea and
surfactants

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 Serves to adhere the patch to the skin for systemic drug
delivery of the drug

 Ex: Silicones, Polyisobutylene

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 Backing layer protects patch from outer environment.

 Ex: Cellulose derivatives, Polypropylene silicon rubber

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19
There are main four types of TDDS

 Membrane moderated system

 Adhesive diffusion controlled system

 Matrix dispersion system

 Micro reservoir system.

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21
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Drug Trade Name Type of Device Indication

Scopolamine Transderm scop Reservoir Motion sickness

Nitroglycerine Transderm nitro Reservoir Angina

Nitro dur Monolithic

Nitro disc Monolithic

Estradiol Estraderm Reservoir Hormone

treatment

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1. Prausnitz MR, Mitragotri S, Langer R. Current status
and future potential of transdermal drug delivery.t Rev
Drug Discov. 2004;3:115–124.
2. Bronaugh RL, Maibach HI, editors. Edn. 4th. New York:
Marcel Dekker; 2005. Percutaneous Absorption.
3. Jain N.K. ,Pharmaceutical Product Development, First
edition,CBS publishers
4. Aulton.M.E, Pharmaceutics; The science of dosage form
design, second edition, Marcel Dekker;2002.502-505.

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5. Allen L.V.; Ansel.H.C ;Popovich.N.G ,Pharmaceutical
dosage forms and drug delivery systems, Ninth edition,
Lippincott Williams and Wilkins publication,2011,295.

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