This document discusses the history and generations of transdermal drug delivery systems (TDDS). It describes 1st generation TDDS which use liquid reservoirs or adhesive matrices to deliver small, lipophilic drugs. 2nd generation systems use techniques like chemical enhancers, heat, or iontophoresis to increase skin permeability for small molecules. Recent 3rd generation techniques disrupt the skin barrier more extensively through iontophoresis, thermal ablation, ultrasound, or microneedle arrays to deliver larger or hydrophilic drugs like peptides. Transdermal delivery offers benefits over oral or injection routes but continuing innovation is needed to expand the types of drugs that can be delivered through the skin.
Transdermal Drug Delivery System (TDDS) is the one of the novel technology to deliver the molecules through the skin for long period of time.
Transdermal Drug Delivery System (TDDS) are defined as self contained, discrete dosage forms which are also known as “patches” 2, 3 when patches are applied to the intact skin, deliver the drug through the skin at a controlled rate to the systemic circulation
Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
Transdermal Drug Delivery System (TDDS) is the one of the novel technology to deliver the molecules through the skin for long period of time.
Transdermal Drug Delivery System (TDDS) are defined as self contained, discrete dosage forms which are also known as “patches” 2, 3 when patches are applied to the intact skin, deliver the drug through the skin at a controlled rate to the systemic circulation
Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
Formulation and evaluation of transdermal drug delivery system (TDDS)SanketPawar47
This is slide about formulation and evaluations of transdermal drugs delivery system . Introduction , general structure of TDDS , basic components of TDDS , approch for formulation of TDDS , manufacturing processes for TDDS ,and evaluations of TDDS
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Application Of Polymer In Controlled Release FormulationAnindya Jana
Polymers are becoming increasingly important in the field of drug delivery. The pharmaceutical applications of polymers range from their use as binders in tablets to viscosity and flow controlling agents in liquids, suspensions and emulsions. Polymers can be used as film coatings to disguise the unpleasant taste of a drug, to enhance drug stability and to modify drug release characteristics.
As a consequence, increasing attention has been focused on methods of giving drugs continually for a prolonged time periods and in a controlled fashion.
This technology now spans many fields and includes pharmaceutical, food and agricultural applications, pesticides, cosmetics, and household products.
Formulation and evaluation of transdermal drug delivery system (TDDS)SanketPawar47
This is slide about formulation and evaluations of transdermal drugs delivery system . Introduction , general structure of TDDS , basic components of TDDS , approch for formulation of TDDS , manufacturing processes for TDDS ,and evaluations of TDDS
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Application Of Polymer In Controlled Release FormulationAnindya Jana
Polymers are becoming increasingly important in the field of drug delivery. The pharmaceutical applications of polymers range from their use as binders in tablets to viscosity and flow controlling agents in liquids, suspensions and emulsions. Polymers can be used as film coatings to disguise the unpleasant taste of a drug, to enhance drug stability and to modify drug release characteristics.
As a consequence, increasing attention has been focused on methods of giving drugs continually for a prolonged time periods and in a controlled fashion.
This technology now spans many fields and includes pharmaceutical, food and agricultural applications, pesticides, cosmetics, and household products.
Overview of Transdermal Drug Delivery Systemijtsrd
Transdermal drug delivery systems are topically administered medicaments. Transdermal drug transport structures TDDS are the dosage shape of adhesive patch this is positioned on the skin to deliver specific dose of medication through the skin and in to the blood stream. The main objective of transdermal drug delivery system is to deliver drug into systemic circulation through skin at predetermined rate with minimal inter and intrapatients variation. This article gives a brief overview over principles behind transdermal drug delivery, as well as the advantages and disadvantages of transdermal therapeutic system and the recent innovations in the field of transdermal drug delivery and also describe the methods of preparation of different types of transdermal patches, evaluation parameters and some available marketed products. Sayali Dhepe | Manisha Sukre | Vikram Veer "Overview of Transdermal Drug Delivery System" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-6 | Issue-4 , June 2022, URL: https://www.ijtsrd.com/papers/ijtsrd50107.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50107/overview-of-transdermal-drug-delivery-system/sayali-dhepe
Transdermal delivery systems are topically administered medicaments in
the form of patches that deliver drugs for systemic effects at a
predetermined and controlled rate.
• Transdermal Drug Delivery System (TDDS) are defined as self-contained,
discrete dosage forms which are also known as “patches”, when patches
are applied to the intact skin, deliver the drug through the skin at a
controlled rate to the systemic circulation.
• TDDS are dosage forms designed to deliver a therapeutically effective
amount of drug across a patient’s skin.
• Currently transdermal delivery is one of the most promising methods for
drug application. It reduces the load that the oral route commonly places
on the digestive tract and liver.
• Transdermal delivery not only provides controlled, constant
administration of drugs, but also allows continuous input of drugs with
short biological half-lives and eliminates pulsed entry into systemic
circulation, which often causes undesirable side effects.
• A transdermal drug delivery device, which may be of an active or a
passive design, is a device which provides an alternative route for
administering medication. These devices allow for pharmaceuticals to be
delivered across the skin barrier.
• A drug is applied in a relatively high dosage to the inside of a patch,
which is worn on the skin for an extended period of time. Through a
diffusion process, the drug enters the bloodstream directly through the
skin.
Although transdermal drug administration has made a significant contribution to medical practise, it has yet to realise its full potential as an alternative to oral drug delivery and hypodermic injections. The patch can essentially provide a controlled release of the medication into the patient, usually through either a porous membrane covering a reservoir of medication or through body heat melting thin layers of medication embedded in the adhesive, which is an advantage of transdermal drug delivery over other types of delivery systems such as oral, topical, intravenous, intramuscular, and so on. The clinical usage of first generation transdermal delivery systems for the delivery of tiny, lipophilic, low dose medicines has increased steadily. Chemical enhancers, non cavitational ultrasound, and iontophoresis have all been used in second generation delivery methods. Akshay Kaware | Prof. Santosh Waghmare | Dr. Hemant Kamble "Transdermal Drug Delivery System: A Review" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-6 | Issue-3 , April 2022, URL: https://www.ijtsrd.com/papers/ijtsrd49639.pdf Paper URL: https://www.ijtsrd.com/pharmacy/other/49639/transdermal-drug-delivery-system-a-review/akshay-kaware
2. Introduction, advantages & disadvantages .
Skin : site of drug delivery.
Skin Anatomy , transport mechanisms.
Components of transdermal patches.
Generations of TDDS.
Recent Methods for enhancing permeation of TDDS
3. Transdermal drug delivery offers an attractive
alternative to the oral administration and injection.
Today about 74% of drugs are taken orally and
are found not to be as effective as desired.
Drug delivery through the skin
(for systemic effect ) is commonly
known as TDD and differs from
traditional topical drug delivery.
4. also known popularly as ‘patches’.
Transdermal patches: are dosage forms designed
to deliver a therapeutically effective amount of
drug from the outside of the skin through its
layers into the blood stream.
5. 1. avoids the stomach environment;
2. no GI distress or other physiological
contraindications of the oral route exist;
3. easy to use, patches can compliance &
medical costs;
4. avoids the first-pass effect;
5. If a transdermal delivery system is used in
place of a needle, then medical waste can
also be , again, healthcare costs.
6. 6. allows for the effective use of drugs with short
biological half-lives;
7. allows for the administration of drugs with
narrow therapeutic windows;
8. provides steady plasma levels of highly potent
drugs;
9. TDDS, especially simple patches, are easy
to use and noninvasive and patients like
noninvasive therapies.
7.
8. 1. drugs that require high blood levels cannot be
administered;
2. The adhesive used may not adhere well to all
types of skin;
3. drug or drug formulation may cause skin
irritation or sensitization;
4. the patches can be uncomfortable to wear;
5. and this system may not be economical for
some patients.
9. FDA (2005) announced that fentanyl td patches cause
narcotic overdose and deaths
Cause: manufacturing defect that allowed the gel
containing the medication to leak out of its pouch too
quickly, which could result in overdose and death.
Improvement : use a matrix/adhesive
suspension (where the medication is
blended with the adhesive instead of
held in a separate pouch with a porous
membrane)
10.
11. oThe human skin is a readily accessible surface for
drug delivery.
oSkin of an average adult body
covers a surface of ~ 2 m² and
receives about 1/3 of the
blood circulating through
the body.
oHuman skin comprises of three
distinct but mutually dependent
layers :
12. Microscopically skin is a multilayered organ broadly composed of
three tissue layers :
The Epidermis
The Dermis
Subcutaneous fatty tissue.
13.
14. Hairy skin develops hair
follicles and sebaceous glands
The most important layer is the
stratum corneum, or horny layer,
which usually provides the rate-
limiting or slowest step in the
penetration process.
15. Principle mechanism is passive diffusion of drug
through the skin. macro-routes may comprise:
a.Transepidermal pathway b. Transfollicular pathway
Hair follicle
Sebaceous
gland Sweat gland
18. 1. Liquid reservoir system where the patch consists of a backing material
that is both protective and adhesive,a liquid drug reservoir, a release
membrane.
2. Adhesive matrix system where the adhesive and the drug are
combined in the same layer leaving only three layers to the patch;
the backing layer, the drug and adhesive layer, and the protective layer.
1st Generation
20. delivery of organic molecules by disrupting st.
cor. barrier function by providing a driving force for
the movement of molecules through the epidermis.
This disruption should be reversible and avoid
injury to the skin.
Enhancement techniques are limited to
small, lipophilic molecules and still have little effect
on larger or hydrophilic molecules.
2nd Generation
23. 2. Heat as a penetration enhancer
The use of heat to increase the permeability of the
skin.
One safe use of heat as a penetration enhancer is the
Controlled Heat-Assisted Drug Delivery(CHADD)
system.
The lidocaine/tetracaine patch system.
25. The use of tiny electric current to promote flow
of the drug (usually charged) through the skin.
3. Iontophoresis as a 2nd G.penetration enhancer
Iontophoresis is a powered drug
delivery system that is indicated for
the local administration of ionic
drug solutions into the body for
medical purposes and can be used
as an alternative to injections.
27. Self-contained, ultra-thin battery technology.
Prepared by the clinician and applied to the patient in the
clinic.
With no external batteries or wires, patients are
able to return to their daily activities while
receiving time-released iontophoresis.
A charged
drug delivery
electrode
(negative)
repels the
drug ions
into the
underlying
tissue.
31. 2. Thermal ablation as a 3rd G.penetration enhancer
Thermal ablation technique seeks to severely disrupt the
stratum corneum.
100s of degrees for very short periods of time (micro- to
milliseconds) and forms painless, reversible microchannels in
the stratum corneum without damaging the underlying tissue
(2008).
33. 3. Ultrasound as a penetration enhancer
Ultrasound to Enhance Skin Permeability
34. Microneedle array consists of chips.
Used for adminstration of therapeutic proteins and
vaccines.
4. Microneedle as a penetration enhancer
200-750 microns in length
150-650 microneedles/cm2
37. Intanza® is a seasonal flu
vaccine that has been
approved in Europe since
2009.
4. Microneedle as a penetration enhancer
38. Transdermal drug delivery technologies are
becoming one of the fastest growing sectors within
the pharmaceutical industry.
Despite some disadvantages, transdermal
drug delivery offers many advantages capable
of improving patient health and quality of life.
1st and 2nd generation TDDS
offer these advantages but are
limited in the scope of molecules
delivered through the skin.