Its Transdermal Drug Delivery system

1. Transdermal Drug Delivery System
Dept. of Pharmaceutics
R. 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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2. Content
Introduction
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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3. Introduction
Transdermal 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.
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4. 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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5. 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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6. Disadvantages of TDDS
Poor 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.
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7. 7

8. 8

9. Surface of sebum
Transdermal Transfollicular
Intracellular Pathway Intercellular Pathway
Stratum Corneum
Pilosebaceous Unit Eccrine Gland
Sebaceous GlandHair Follicles
Dermis
Microcirculation
Viable Epidermis
Percutaneous absorption
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10. Factors affecting Transdermal permeation
• Partition Coefficient
• pH
• Molecular Wt. and Size
• Concentration of penentrant
Physiochemical
• Vehicle Solubility of drug
• pH of Vehicle
• Lipophilicity of solvent
Formulation
• Lipidic Film
• Skin hydration
• Skin Temprature
• Pathological injuries
Biological
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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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12. 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

13. Drug
Should 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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14. Penetration enhancers
These 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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15. Adhesives
Compatible with Drug
Should have allergy free
Should have sensation free
Example:
Polyacrylates
Silicones
Adhesive are two types
1. Face adhesive
2. Prophylactic adhesive
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16. 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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17. 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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18. 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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19. 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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20. Adhesive diffusion controlled
TDDS
Deponit (Nitroglycerine) for once a day medication
of angina pectoris.
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21. Nitro- dur (nitroglycerine) used for once a day
medication of angina pectoris.
Matrix diffusion controlled TDDS
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22. 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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23. Evaluation Parameters
Physical parameters
Evaluation of adhesive
In-vitro testing
In-vivo assessment
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24. Conclusion
TDDS 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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25. References
1) 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.
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26. THANK YOU
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Email ID: nitinsonar5@gmail.com