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TRANSDERMAL DRUG
DELIVERY SYSTEM
Definition
• Self contained discrete dosage forms which when applied to the intact skin
deliver the drug through the skin at a controlled rate to the systemic circulation.
• It improves patient compliance
• It is easy to apply as a patch
ADVANTAGES
• Hepatic first pass metabolism, salivary metabolism and intestinal metabolism are avoided.
• The ease of usage makes it possible for patients to self-administer these systems.
• In case of an emergency, removing the patch at any point of time during therapy can instantly
stop drug input.
• Since the composition of skin structurally and biologically is the same in almost all the humans,
there is minimal inter and intra patient variation.
• Drugs showing gastrointestinal irritation and absorption can be suitably administered through the
skin.
• Continuous, non-invasive infusion can be achieved for drugs with short biological half-lives, which
would otherwise require frequent dosing.
• Due to reduced frequency of dosing there is better patient compliance.
• Therapeutic failures associated with irregularities in the dosing with conventional therapies can
be avoided.
• The adverse effects are minimized due to a steady and optimum blood concentration time profile.
DISADVANTAGES
• There is possibility of skin irritation due to the one or many of the
formulation components.
• Binding of drug to skin may result in dose dumping.
• It can be used only for chronic conditions where drug therapy is desired for
a long period of time e.g., hypertension, angina and diabetes etc.
• Lag time is variable and can vary from several hours to days for different
drug candidates.
• Cutaneous metabolism will affect therapeutic performance of the system.
• Transdermal therapy is feasible for certain potent drugs only.
• Transdermal therapy is not feasible for ionic drugs.
• It cannot deliver drug in pulsatile fashion.
Drug Trade name Company
Estradiol
Estraderm Ciba Geigy
Climara Berlexpharma
Fempatuch Parke Davies
Alora Proctor & Gamble
Fentanyl Duragesic Alza corp, N.J.
Testosterone
Testoderm Alza corp, N.J
Androderm Alza corp, N.J
Nitroglycerin
Deponit Schwarz Pharma
Nitrodur Ciba Geigy
Nitrodisc Robests Pharma
Minitran 3 M
Transderm nitro Ciba Geigy
Clonidine Catapress Boehringer Ingelheim
Scopolamine Transderm scope Ciba Geigy
Nicotine
Nicoderm Smithkline Beecham
Nicotrol Mc neol consumer products
Prostep Ledisle Pharma
Habitrol Ciba Geigy
MARKETED TRANSDERMAL DRUG DELIVERY SYSTEMS
• Skin as route of Transdermal Drug Delivery:
• The transdermal permeation of a chemical involves partitioning into and transport
through the cutaneous layers, namely the stratum corneum, the viable epidermis
(stratum basale) and the upper dermis.
• The skin is a barrier to topically administered drugs.
• Thus, the permeability of drugs depends on the degree of hydration.
• Cosolvents may later the barrier properties of the skin.
brief review of skin structure: The skin can be considered to have four distinct
layers of tissue.
•Non-viable epidermis (stratum corneum)
•Viable epidermis
•Viable dermis
•Subcutaneous connective tissue (hypodermis)
er the circulatory system before reaching the hypodermis, where the fatty tissue serve
as a depot of the drug
Epidermis: The epidermis is the relatively thin, tough, outer layer of the skin. The
epidermis is keratinocytes. They originate from cells in the deepest layer of the
epidermis called the basal layer. New keratinocytes slowly migrate up toward the
surface of the epidermis.
Non-viable epidermis (stratum corneum): The outermost portion of the epidermis,
known as the stratum corneum, is relatively waterproof and, when undamaged,
prevents most bacteria, viruses, and other foreign substances from entering the body.
The epidermis also protects the internal organs, muscles, nerves, and blood vessels
against trauma. The outer keratin layer of the epidermis (stratum corneum) is much
thicker.
Viable Epidermis: This layer of the skin resides between the stratum corneum and the
dermis and has a thickness ranging from 50-100 µm. The structure of the cells in the
viable epidermis is physiochemically similar to other living tissues. Cells are held
together by tonofibrils. The water content is about 90%.
Dermis: The dermis, the skin's next layer, is a thick layer of fibrous and elastic tissue
(made mostly of collagen, elastin and fibrillin) that gives the skin its flexibility and
strength. The dermis contains nerve endings, sweat glands and oil glands, hair
follicles, and blood vessels.
Subcutaneous Connective Tissue: The subcutaneous tissue also known as
hypodermis is not actually accepted a true part of the structured connective tissue is
composed of loose textured, white, fibrous connective tissue containing blood and
lymph vessels, Most investigators consider drug permeating through the skin ent
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TRANSDERMAL DRUG DELIVERY SYSTEM.pptx

  • 2. Definition • Self contained discrete dosage forms which when applied to the intact skin deliver the drug through the skin at a controlled rate to the systemic circulation. • It improves patient compliance • It is easy to apply as a patch
  • 3. ADVANTAGES • Hepatic first pass metabolism, salivary metabolism and intestinal metabolism are avoided. • The ease of usage makes it possible for patients to self-administer these systems. • In case of an emergency, removing the patch at any point of time during therapy can instantly stop drug input. • Since the composition of skin structurally and biologically is the same in almost all the humans, there is minimal inter and intra patient variation. • Drugs showing gastrointestinal irritation and absorption can be suitably administered through the skin. • Continuous, non-invasive infusion can be achieved for drugs with short biological half-lives, which would otherwise require frequent dosing. • Due to reduced frequency of dosing there is better patient compliance. • Therapeutic failures associated with irregularities in the dosing with conventional therapies can be avoided. • The adverse effects are minimized due to a steady and optimum blood concentration time profile.
  • 4. DISADVANTAGES • There is possibility of skin irritation due to the one or many of the formulation components. • Binding of drug to skin may result in dose dumping. • It can be used only for chronic conditions where drug therapy is desired for a long period of time e.g., hypertension, angina and diabetes etc. • Lag time is variable and can vary from several hours to days for different drug candidates. • Cutaneous metabolism will affect therapeutic performance of the system. • Transdermal therapy is feasible for certain potent drugs only. • Transdermal therapy is not feasible for ionic drugs. • It cannot deliver drug in pulsatile fashion.
  • 5. Drug Trade name Company Estradiol Estraderm Ciba Geigy Climara Berlexpharma Fempatuch Parke Davies Alora Proctor & Gamble Fentanyl Duragesic Alza corp, N.J. Testosterone Testoderm Alza corp, N.J Androderm Alza corp, N.J Nitroglycerin Deponit Schwarz Pharma Nitrodur Ciba Geigy Nitrodisc Robests Pharma Minitran 3 M Transderm nitro Ciba Geigy Clonidine Catapress Boehringer Ingelheim Scopolamine Transderm scope Ciba Geigy Nicotine Nicoderm Smithkline Beecham Nicotrol Mc neol consumer products Prostep Ledisle Pharma Habitrol Ciba Geigy MARKETED TRANSDERMAL DRUG DELIVERY SYSTEMS
  • 6. • Skin as route of Transdermal Drug Delivery: • The transdermal permeation of a chemical involves partitioning into and transport through the cutaneous layers, namely the stratum corneum, the viable epidermis (stratum basale) and the upper dermis. • The skin is a barrier to topically administered drugs. • Thus, the permeability of drugs depends on the degree of hydration. • Cosolvents may later the barrier properties of the skin.
  • 7. brief review of skin structure: The skin can be considered to have four distinct layers of tissue. •Non-viable epidermis (stratum corneum) •Viable epidermis •Viable dermis •Subcutaneous connective tissue (hypodermis) er the circulatory system before reaching the hypodermis, where the fatty tissue serve as a depot of the drug Epidermis: The epidermis is the relatively thin, tough, outer layer of the skin. The epidermis is keratinocytes. They originate from cells in the deepest layer of the epidermis called the basal layer. New keratinocytes slowly migrate up toward the surface of the epidermis. Non-viable epidermis (stratum corneum): The outermost portion of the epidermis, known as the stratum corneum, is relatively waterproof and, when undamaged, prevents most bacteria, viruses, and other foreign substances from entering the body. The epidermis also protects the internal organs, muscles, nerves, and blood vessels against trauma. The outer keratin layer of the epidermis (stratum corneum) is much thicker.
  • 8. Viable Epidermis: This layer of the skin resides between the stratum corneum and the dermis and has a thickness ranging from 50-100 µm. The structure of the cells in the viable epidermis is physiochemically similar to other living tissues. Cells are held together by tonofibrils. The water content is about 90%. Dermis: The dermis, the skin's next layer, is a thick layer of fibrous and elastic tissue (made mostly of collagen, elastin and fibrillin) that gives the skin its flexibility and strength. The dermis contains nerve endings, sweat glands and oil glands, hair follicles, and blood vessels. Subcutaneous Connective Tissue: The subcutaneous tissue also known as hypodermis is not actually accepted a true part of the structured connective tissue is composed of loose textured, white, fibrous connective tissue containing blood and lymph vessels, Most investigators consider drug permeating through the skin ent