Transdermal patches Flashcards
Roles of the epidermis(stratum cornuem sits on top ) and dermis layer of skin
Dermis
➢Supplies epidermis with blood, lymphatic vessels and
nerve endings
Epidermis
➢Physiologically active tissues
➢Inactive stratum corneum
Stratum corneum
➢Abt 10-25 mm thick
➢Main barrier to entry of drugs
➢Retains body moisture
2 different drug penetration ways
i. Appendageal route:
- going through the hair, sebaceous and sweat glands
ii. Epidermal route:
- Intracellular
right through to blood vessels
- Intercellular
going through tight junctions in the stratum corneum
Factors affecting percutaneous absorption
- Area of application
- Length of application
- Skin factors:
➢Hydration
➢Thickness of horny layer - Drug factors:
➢Partition coefficient
➢ Molecular weight
➢Concentration
➢Polar/non-polar
Advantages of TDDS
By-pass chemically hostile GI environment and first
pass effect of liver
* Better plasma conc time
profile*
* Predictable and extended
duration of activity
* Increases patient compliance
* Reversibility of drug delivery which allows removal of
drug source
Disadvantages of TDDS
- Cannot cut patches to half the dose
- Paediatric doses
- Only relative potent drugs are suitable for this route
- Issues with skin irritation (1-2%)
- Restricted area of application
Basic components of TDDS.1
Backing, polymer matrix
Backing
➢ Chosen for appearance, flexibility and need for occlusion
➢ Additives don’t leach out into the drug reservoir
➢ Drug reservoir components don’t diffuse through the backing
- Polymer matrix
➢ Stable, non-reactive with the drug, easily manufactured and
inexpensive.
➢ Should not deteriorate excessively when large amounts of active
ingredient are incorporated
➢ Should be biocompatible and chemically compatible with other
components of the system
➢ Should provide consistent and effective delivery of drug throughout
the product’s life
Basic components of TDDS.2
Adhesive layer and release liner
Adhesive layer
➢ Two types: peripheral adhesive or face adhesive
➢ Non-irritating, allow easy peel-off after use, permit unimpeded drug
flux to the skin and be compatible with all other components in the
system.
➢ Related to drug delivery and therapeutic effect
➢ Quality of bond between patch and skin directly reflects consistency of
drug delivered
➢ Poor adhesion results in improper dosing of patients
- Release liner
➢ Protective liner that is removed and discarded before the application
➢ Liner should be chemically inert
Active penetration enhancement techniques
- Iontophoresis (IP)
- Sonophoresis
- Microneedles