School of Medical And Allied Sciences

Course Code : MPHT1002 Course Name: Drug delivery system

Module 4
Lecture 6
Transdermal drug delivery systems

Name of the Faculty: Prof. P.K Sharma Program Name: M.Pharm

 Disclaimer

• All the content material provided here is only for

teaching purpose.
 Objective

To study the factors affecting trans dermal drug delivery

system?
To study the penetration mechanism of trans dermal drug
delivery system ?
Chemical Penetration Enhancement:-
✓Ideal characteristics of chemical penetration enhancers
✓Non-toxic, non-irritating and non-allergenic
✓The activity and duration of effect should be both
predictable and reproducible.
✓No pharmacological activity within the body.
✓Unidirectional
✓Barrier properties should return to normal.
✓Cosmetically acceptable with an appropriate skin feel.
Mechanism of chemical penetration enhancement:-

✓Disruption of the highly ordered structure of stratum

corneum lipid.
✓Interaction with intercellular protein.
✓Improved partition of the drug, co enhancer or solvent
into the stratum corneum
1. Sulphoxides and similar chemicals:-
Aprotic solvent, colourless, odourless and hydroscopic
It is known as ‘Universal Solvent’ for TDDs.
The effect is concentration-dependant (›60% )
Cause erythema, denaturing of skin, burning sensation.
Ex- showing a 12-fold increase in the flux of caffeine permeating
across a DMF-treated human skin, but it also shows irreversible
damage to skin.
2. Azone:-
Azone (1-dodecylazacycloheptan-2-one or laurocapran)
Colourless, odourless liquid with a melting point of -7 ºC
Smooth, oily but yet non-greasy feel.
Soluble in most of organic solvent.
Effect showing in 0.1-5% (more often between 1-3%)

3. Pyrrolidones:-
Used as permeation enhancers for numerous molecules including
hydrophilic (e.g. mannitol and 5-flurouracil) and lipophilic
(progesterone and hydrocortisone) permeants.
Ex-N-methyl-2 pyrolidone was employed with limited success as
a penetration enhancer for captopril when formulated in a
matrix-type transdermal patch.
4. Fatty acids:-
Percutaneous absorption can be increased by long-chain
fatty acids such as oleic acid.
Ex- Oleic acid increase the flux 28 fold of salicylic acid and
56 of 5-flourouracil.

5. Essential oils, terpenes and terpenoids:- It is used as

medicinal use as well as flavoring agent and fragrance
agent.
Ex- Chenopodium found to be effective penetration
enhancers for 5-flouorouracil transversing human skin.
6. Oxazolidinones:-
Potential for use in many cosmetic and personal care product
formulations.
It having ability to localize co-administered drug in skin layers,
resulting in low systemic
permeation.
Ex- 4-decyloxazolidin-2-one -localize the delivery of retinoic acid
and diclofenac sodium
in skin layers.

7. Urea
Cyclic urea permeation enhancers are biodegradable and non-
toxic molecules.
Enhancement mechanism by lipid disruption mechanism
 Conclusion

Students understudied the factors affecting trans dermal

drug delivery system.
Students understudied penetration mechanism of trans
dermal drug delivery system.
 References:-
1. Chein, Y W, 1992, Novel Drug Delivery System, 2nd edition, vol-
14, Marcel Dekker Inc, New York, pp- 301-314.
2. Banker, G S, & Rhodes, C T, 2002, Modern Pharmaceutics, 4th
edition, vol-121, Marcel Dekker Inc, New York, pp. 187-192.
3. Hsieh, D S, 1994, Drug Permeation Enhancement, theory and
application, vol-62, Marcel Dekker Inc, New York, pp. 3-23.
4. Roberts, M S, & Walters, K A, 1998, Dermal Absorption and
Toxicity Assessment, vol-91, Marcel Dekker Inc, New York, pp
297-309 371-375.
5. Walters, K A, 2002, Dermatological and Transdermal
Formulation,vol-119, Marcel Dekker Inc, New York, pp 1-14 337-
339.
6. Brahmankar, D M & Jaiswal, S B, 2005, Biopharmaceutics and
Pharmacokinetics A Treatise, Vallabh prakashan, Delhi, pp-365-
369.