TRANSDERMAL DRUG DELIVERY SYSTEMS TYPES OF TDDS

Chapter 9 MONOLITHIC SYSTEM

Percutaneous Absorption  A TDDS that incorporates a drug matrix between backing and
 It refers to the direct penetration of the drug through the frontal layers
stratum corneum Examples
 The stratum corneum is a 10-15 mm thick layer of flat,  Salonpas
partially dessicated nonliving tissue.  Band-aid
 It is composed of approximately 40% protein [keratin], 40% MEMBRANE-CONTROLLED SYSTEM
water, with the balance being lipid [principally as  A TTDS designed to contain a drug reservoir [or a pouch
triglycerides, free fatty acids, cholesterol and phospholipids]. usually in liquid or gel form], a rate-controlling membrane
FACTORS AFFECTING PERCUTANEOUS ABSORPTION and backing, adhesive and protective layer
 Hydration of the skin generally favors percutaneous COMPONENTS OF TDDS
absorption. BACKING LAYER
 Generally, the longer the TDDS is permitted to remain in  An occlusive backing membrane to protect the system from
contact with the skin, the greater is the total drug absorption. environmental entry and from loss of drug from the system
 More of the drug is absorbed when the TDDS is applied to a or moisture from the skin
large surface area. DRUG RESERVOIR/MATRIX SYSTEM
PERCUTANEOUS ABSORPTION ENHANCERS  A system to store and release the drug at the skin site
CHEMICAL ENHANCERS RELEASE LINER/PROTECTIVE LINER
 A chemical skin penetration enhancer increases skin  It is removed from the system prior to application and
permeability by reversibly damaging or altering the enables drug release
physicochemical nature of the stratum corneum to reduce ADHESIVE LAYER
its diffusional resistance.  A layer used to maintain contact with the skin after
IONTOPHORESIS application
 Is a delivery of a charged chemical compound across the skin Types
membrane using an electric field  Peripheral adhesive
Examples - Contains adhesive around the outer edges of the TDDS
 Lidocaine  Face adhesive
- Covers the entire face of the TDDS
 Dexamethasone
 Polybutyl acrylate is the commonly used adhesive in TDDS
 Amino acids, peptides and insulin
ADVANTAGES OF TDDS
 Verapamil
 Can avoid gastrointestinal absorption difficulties
 Propranolol  Can substitute for oral administration of medication when
 Percutaneous Absorption that route is unsuitable
 Enhancers  Avoid first pass effect
SONOPHORESIS  Non-invasive
 Involves the use of high-frequency ultrasound to enhance  Provide extended therapy with a single application
DISADVANTAGES OF TDDS
transdermal drug delivery
o Only relatively potent drugs are suitable candidates for
Examples
transdermal delivery
 Hydrocortisone
o Some patients may develop contact dermatitis at the site of
 Lidocaine
application
 Salicylic acid
EXAMPLES OF TDDS
TRANSDERMAL DRUG DELIVERY SYSTEMS
TDDS OR TRANSDERMAL PATCHES Transdermal Scopolamine
 Are dosage forms designed to support the passage of drug  The first TDDS to receive FDA approval
substances from the surface of the skin through its various  A belladonna alkaloid used to prevent travel-related motion
layers and into the systemic circulation sickness and the nausea and vomiting that result from the
use of certain anesthetics and analgesics in surgery
 It is worn in a hairless area behind the ear
Transdermal Nitroglycerin
 Used widely in the prophylactic treatment of angina
 Placed in the chest, back, upper arms or shoulders
 The site should be free of hair, clean and dry
Transdermal Clonidine
 The first TDDS for hypertension
 It is applied to a hairless area of intact skin on the upper
outer arm or chest
Transdermal Nicotine
 Are used as adjuncts in smoking cessation programs
 It is applied to the arm or upper front torso
Transdermal Estradiol
 It is indicated for the treatment of moderate to severe
vasomotor symptoms associated with menopause, female
hypogonadism, female castration, primary ovarian failure and
atrophic conditions caused by deficient estrogen production
 It is applied to a clean, dry area of the skin on the body trunk,
either the abdomen or upper quadrant of the buttocks
Transdermal Testosterone
 Used as hormone replacement therapy in men who have an
absence or deficiency of testosterone
 It is applied to a clean, dry scrotal skin that has been dry-
shaved
 It is also applied to a clean, dry, unbraided area of the skin of
the back, abdomen, upper arms or thighs
Transdermal Contraceptive System
 It contains norelgestromin and ethinyl estradiol indicated for
family planning
Other TransdermalTherapeutic Systems
 Diltiazem, ISDN, propranolol, nifedipine, mepindololand
verapamil for cardiovascular problems
 Levenorgestrel with estradiol for hormonal contraception
 Physostigmine and xanomeline for Alzheimer’s disease
 Naltrexone and methadone for substance addiction
 Buspirone for anxiety
 Bupropion for smoking cessation
 Papaverine for male impotence
GENERAL CONSIDERATIONS IN THE USE OF TDDS
 There is a preferred site of application for every TDDS
product
 They are applied to clean, dry skin areas, relatively
free from hair, oil, irritation, inflammation, abrasion or
callous
 Use of skin lotions should be avoided at the application site
 TDDS should not be physically altered by cutting
 A TDDS should be removed from its protective package, being
careful not to tear or cut-off the unit
 It should be placed at a site that is not subject to being
rubbed off by clothing or movement
 It should be worn for the full period of time stated in the
product’s instructions
 The user’s should clean their hands thoroughly before and
after applying a TDDS
 If the patient exhibits sensitivity or intolerance to the TDDS,
he should seek reevaluation
 Upon removal, a used TDDS should be folded in half with the
adhesive layer together so that it cannot be re-used