Transdermal Drug Delivery Sys-tem

Dept. of PharmaceuticsR. C. Patel Institutes of Pharmaceutical Education and Research, Shirpur 425 405

2015-16

By..Mr.Nitin H.Sonar

M. Pharm. (IInd Sem.)

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ContentIntroduction

Advantages And Disadvantages

Structure of Human Skin

Percutaneous absorption

Factors affecting transdemal permeation

Basic componants of transdermal permeation

Classification of TDDS

Evaluation of TDDS

Conclusion

Reference

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IntroductionTransdermal drug delivery systems (TDDSs) facilitate the passage of

therapeutic quantities of drug substances through the skin and into the

general circulation for their systemic effects. In 1965, Stoughton first

conceived of the percutaneous absorption of drug substances.The first

transdermal system, Transdermal Scop , was approved by the Food and

Drug Administration (FDA) in 1979 for prevention of nausea and vomiting

associated with travel.

Definition:- Transdermal drug delivery system can deliver the drugs

through the skin portal to systemic circulation at a predetermined rate

and maintain clinically the effective concentrations over a prolonged

period of time. 3

COMPARISON BETWEEN IV,ORAL AND TDDS

ADVANTAGES IV ORAL TDD

Avoid hepatic first-pass effects YES NO YES

Constant drug levels YES NO YES

Self-administration NO YES YES

Termination of therapy NO YES YES

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Reduces first-pass metabolism effect and GI

incompatibility

Sustains therapeutic drug levels

Permits self-administration

Non-invasive (no needles or injections)

Improves patient compliance

Reduces side effects

Allows removal of drug source

Long acting drug delivery

Advantages of TDDS

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Disadvantages of TDDSPoor diffusion of large molecules

Skin irritation

Only suitable for very potent drugs

More expensive than oral drugs

Heat, cold, sweating (perspiring) and showering

prevent the patch from sticking to the surface of the skin

for more than one day. A new patch has to be applied

daily.6

Structure of human skin

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Surface of sebum

Transder-mal

Transfollicular

Intracellular Pathway Intercellular Pathway

Stratum CorneumPilosebaceous Unit Eccrine Gland

Sebaceous GlandHair Follicles

Der-mis

Microcirculation

Viable Epidermis

Percutaneous absorption

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Factors affecting Transdermal permeation

Physio-chemical

• Partition Coefficient• pH• Molecular Wt. and Size • Concentration of penentrant

Formu-lation

• Vehicle Solubility of drug• pH of Vehicle• Lipophilicity of solvent

Biologi-cal

• Lipidic Film• Skin hydration• Skin Temprature• Pathological injuries

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Release liner

Adhesives

Backing laminate

Penetration enhancers

Polymer matrix

Drug

Basic components of Transdermal drug delivery system

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Drug Selection criteria

Dose is less than 10 mg per day

Molecular weight less than 1000 Daltons

Aqueous solubility >1mg/ml

Oil solubility >1mg/ml

Drug should not be an irritant to skin

Drug should be potent and have short half life

Drug should not stimulate an immune reaction in

the skin 12

DrugShould have compatible with Polymer and excipient

Polymer matrix Should be compatible with drug and excipient

Stable at skin and body temperature

They should not damage skin Ex. Gelatin, Neoprene, Polyethylene

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Penetration enhancersThese are substances which enhances penetration of drug through

skin

Organic solvent

Polar solvent

Surfactant

a) Anionic - Ex. SLS

b) Non-ionic – Ex. Pluronic F-27, F-68

Miscellaneous - Ex. Urea, N-N-Dimethyl

Binary Ex. Propylene glycolic acid

Under Investigation Ex. Soyabean casein

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Adhesives

Compatible with Drug

Should have allergy free

Should have sensation free

Example:PolyacrylatesSilicones

Adhesive are two types

1. Face adhesive

2. Prophylactic adhesive15

Release liner

During storage the patch is covered by a protective liner

that is removed and discharged immediately before the

application of the patch to skin.

Part of primary packaging

Example:

• Polyethylene

• Polyvinylchloride

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Backing laminate

Hold and protect the drug reservoir from exposure

to atmosphere.

Avoid loss of drug

High flexibility

Good oxygen transmission and a high moisture

vapor transmission rate

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1. Polymer membrane permeation-controlled.

2. Polymer matrix diffusion- controlled

3. Drug reservoir gradient-controlled

4. Micro reservoir dissolution-controlled

Classification of TDDS

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Transderm-Scop (scopolamine) for 3 days protection of motion sickness and transderm-nitro (nitroglycerine) for once a day medication of angina pectoris

Membrane permeation controlled TDDS

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Adhesive diffusion controlled TDDS

Deponit (Nitroglycerine) for once a day medication of angina pectoris.

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Nitro- dur (nitroglycerine) used for once a day medication of angina pectoris.

Matrix diffusion controlled TDDS

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Microreservoir dissolution controlled TDDS

Nitrodisc (Searle, USA) :- Nitroglycerin releasing transdermal therapeutic system engineered to provide nitroglycerin at the rate of 0.5 mg/cm2 for once a day therapy of angina pectoris.

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Evaluation Parameters

Physical parameters

Evaluation of adhesive

In-vitro testing

In-vivo assessment

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ConclusionTDDS a realistic practical application as the next generation of drug

delivery system.

Due to the recent advances in technology and the incorporation of the

drug to the site of action without rupturing the skin membrane

transdermal route is becoming the most widely accepted route of drug

administration.

As we know, the basic functions of the skin is protection and hence it

is difficult to target the skin for drug delivery. Because skin having

numerous layers. But using novel techniques in TDDS we have

successfully penetrate the drug into systemic circulation.

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References1) Chien, Y. W. (1992) Novel drug delivery systems, Drugs and the

Pharmaceutical Sciences. Vol. 50, New York: Marcel Dekker, pp.797.

2) Ansel, H. C., Loyd, V. A. and Popovich, N. G. Pharmaceutical dosage

forms and drug delivery systems. 7th ed. New Delhi: Published by

Wolters Kluwer Pvt. Ltd., pp. 294- 311.

3) Lawrence, H. B. Remington (The science and practice of

pharmacy). 21st ed. Published by Wolters Kluwer, Vol. I, pp. 871- 888.

4) Barry, B. W. Aulton’s Pharmaceutics- The science of dosage form

design, 2nd ed. pp. 566- 597.

5) Jain, N.K. (1997) Controlled and novel drug delivery. 1st ed. New

Delhi: CBS publishers and distributors, pp. 100- 127.25

THANK YOU

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Email ID: nitinsonar5@gmail.-com