The presentation overviews on Introduction to transdermal drug delivery system, Various TDDS technologies that includes active and passive methods . Active delivery methods containing iontophoresis, sonophoresis,electroporation,micro needles,Thermal ablation ,whereas passive delivery method consisting of vesicles and nanoparticles .It also explain various challenges and opportunities for transdermal drug delivery system.
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Emerging trends in transdermal drug delivery technology.pptx version 1-1.pdf
1. Shri Balasaheb Mane Shikshan Prasarak Mandal Ambap’s
ASHOKRAO MANE COLLEGE OF PHARMACY,PETH VADGAON
DEPARTMENT OF PHARMACEUTICS
TITLE OF SEMINAR: “EMERGING TRENDS IN TRANSDERMAL
DRUG DELIVERY TECHNOLOGIES”
SEMESTER -1
Academic Year 2023-24
Presented by Guided by
Miss Prajakta R. Patil Dr. Sachin S. Mali
M.pharm I year Professor and Head,
Roll No-11 Department of Pharmaceutics
2. CONTENT
Introduction
Introduction to Transdermal Drug Delivery System.
Advantages and Disadvantages of TDDS.
Basic components of TDDS
Transdermal Drug Delivery Technologies
Equipment assisted Transdermal Delivery (Active Delivery)
Chemical Enhancer Assisted Transdermal Delivery (Passive Delivery)
Literature Review
Challenges and Opportunities
Conclusion
References
3. INTRODUCTION
Transdermal drug delivery System are defined as self contained, discrete dosage forms
which are applied to intact skin, deliver the drug through skin at predetermined rate.
Transdermal Drug Delivery system (TDDS) is one of the systems lying under the
category of controlled drug delivery, in which the aim is to deliver the drug through skin at
predetermined and controlled rate.
TDDS has emerged as one of the most extensively researched non-invasive drug
delivery methods via the skin.
4. Advantages and Disadvantages of TDDS
Advantages of Transdermal Drug
Delivery System
Disadvantages of Transdermal Drug
Delivery System
1. Enables the avoidance of GI absorption
2. Avoidance of First pass metabolism
3. It also achieves consistent plasma
levels.
4. Used as an alternative delivery system
for patient who cannot tolerate oral
dosage form.
5. Provide utilization of drug with narrow
therapeutic window and short half lives.
6. Cost effective.
1. Drugs with hydrophilic structures permeates
the skin too slowly may not achieve
therapeutic level.
2. It cannot develop for drugs of high
molecular size.
3. It cannot develop if drug or formulation
causes irritation to skin.
4. Possibility of local irritation at site of
application.
5. The barrier function of skin changes from
one person to person and also with age.
5. BASIC COMPONENT OF TDDS
1. Polymer Matrix
2. Membrane
3. Drug
4. Penetration Enhancer
5. Pressure Sensitive Adhesives
6. Backing laminate
7. Release Liner
8. Other Excipients
7. ACTIVE DELIVERY
1. Iontophoresis:
Iontophoresis is a method of electrodynamic transdermal drug delivery.
Drug must ionize and have net charge (+ or -)
Negative drugs are placed on cathode(-) and they migrate transdermally to
anode (+)
Positive drugs are placed on anode (+) and they migrate transdermally to
cathode (-)
9. Drug delivery
Iontophoresis
Negative drug(-) Positive drug (+)
On cathode On anode
Max current Density(0.5mA/cm2)
Max current Intensity(MCA x SA)
Dose= Intensity(mA) x Time(min)
Dose=(40-80mA min)
Duration ≤ 30 min
1.Determine chemical charge
of Dexamethasone
Negative
2. Determine where to put
Dexamethasone
Cathode
3.Determine Maximum safe
current density and
intensity
MCD= 0.5mA/cm2
MCI =0.5mA/cm2 x 6 cm2
=3.0mA
4.Determine treatment
duration
Duration=Dose/Intensity
Dur1=60mA min /3mA=20 min
Dur2=60mA min/2mA=30 min
Dur3=60mA min/1mA=60min NO
Cont….
Max current Density(0.1mA/cm2)
Max current Intensity(MCA x
SA)
Dose= Intensity(mA) xTime(min)
Dose=(40-80mA min)
Duration ≤ 30 min
10. 2. Sonophoresis:
Sonophoresis (Phonophoresis) is the method that utilizes ultrasound ,which is
used to drive medication transdermally through skin.
Similar to that of iontophoresis, where instead of electric current, ultrasound is
used to deliver drugs through skin.
Slide 11-https://www.youtube.com/watch?v=Vonw27Swm5Q
11. Inflammation
Reduce inflammation
Drive drug transdermally
Non-thermal duty cycle
3 MHz Frequency
0.5-1.0W/cm2 Intensity
5-10 min/ x ERA Duration
Thermal
Prevents drug
transport
100%
duty
20% duty
20kHz
125 mW/cm2
5-10 min/2 x ERA
Low frequency US
Allows larger MW
drug to diffuse
Cont….
12. 3. Electroporation:
This method uses the application of high voltage electric pulses ranging from
50 to 500 V for short exposure times (~ms) to the skin, which leads to the
formation of small pores in the SC that improve permeability and aid drug
diffusion.
For safe and painless drug administration, electric pulses are introduced using
closely positioned electrodes.
The main advantages offered by electroporation are quick onset of action,
delivery of macromolecules.
13. v
v
v
Electric field
50-500 v
Pulse duration
10-100ms
Power supply
Pore formation +
electric repulsion
Drug
solution
Basic Design of Electroporation delivery devices
Cont….
14. 4.Microneedle:
The micro needle drug delivery system is a novel drug delivery system, in
which drugs are delivered to the circulatory system through a needle. This
represents one of the most popular methods for Transdermal drug delivery
and is an active area of current research.
The micro needle patches range in size from the size of phone sim card to the
size of mobile phone i.e. can be fabricated to different size and ranges.
15. Schematic representation of comparison of topical, parenteral, and Transdermal
drug delivery systems utilized in the management of pain.
Cont….
16. 5.Thermal Ablation:
Thermal ablation, also known as thermophoresis, is a promising technique for
selectively disrupting the stratum corneum structure by localized heat which
provides enhanced drug delivery through micro channels created in the skin.
To ablate the stratum corneum by thermal ablation, a high temperature above
100 °C is required and this leads to heating and vaporization of keratin.
Thermal ablation is induced by laser or radiofrequency method.
17. Passive Delivery
1. Vesicles:
Vesicles are colloidal particles filled with water and consist of amphiphilic
molecules in a bilayer arrangement. Under conditions of excess water, these
amphiphilic molecules form concentric bilayers with one or more shells
(multilayer vesicles).
Vesicles can carry water-soluble and fat-soluble drugs to achieve
transdermal absorption. When utilized for topical applications, vesicles can
be used to achieve sustained release of stored drugs.
Types of vesicles includes: a) Liposomes, b) Transferosomes c) Ethosomes
18. a) Liposome's:
Liposome's are circular soft vesicles formed by one or more bilayer
membranes that separate an aqueous medium from another. Their main
components are usually phospholipids, with or without cholesterol.
Phospholipids molecules are mainly composed of different polar head groups
and two hydrophobic hydrocarbon chains.
19. b) Transferosomes:
Transferosomes are also called deformable liposome's, or elastic or highly
flexible liposome's. The most important feature of these vesicles is the
elasticity that results from the addition of single-chain surfactants.
TDDS using Transferosomes allows the administration of macromolecular
drugs such as peptides or proteins
20. c) Ethosomes:
Ethosomes are composed of phospholipids, alcohols, and water.
Compared with liposome's, Ethosomes have higher alcohol concentrations.
Ethosomes promote the percutaneous penetration of drugs, with
phospholipids also contributing to the process.
21. 2. Polymeric Nanoparticles:
Nanoparticles (NPs) are nanocarriers with sizes ranging between 1 and 1000 nm
and can be classified into several types according to their composition. Drug
administration in the form of NPs leads to targeted and controlled release
behaviour.
In the field of TDDS, polymeric NPs are gaining increased attention because they
can overcome the limitations of other lipid-based systems, such as by conferring
protection to unstable drugs against degradation and denaturation and achieving
continuous drug release to reduce side effects.
22. Applications:
1. Precision in Drug Release: Active systems, such as iontophoresis or electroporation, allow for
controlled and targeted drug delivery, enhancing precision in dosage and timing.
2. Macromolecule Delivery: They are effective for delivering larger molecules that might struggle
to pass through the skin barrier passively.
3. Therapeutic Monitoring: Active systems can be integrated with sensors to monitor drug levels,
enabling real-time adjustments for optimal therapeutic outcomes.
4. Rapid Onset: Active methods often result in faster onset of action, making them suitable for
conditions requiring quick relief.
5. Patient Compliance: Since passive systems are usually non-invasive and require less
maintenance, they enhance patient compliance.
6. Reduced Side Effects: They may lead to fewer side effects compared to active methods, as
they typically involve lower drug concentrations
23. Literature Review
1. Woo Yeup Jeong et.al (2021) reviewed on recent advances in transdermal drug
delivery system that consist of Active and Passive methods for drug delivery along
with their advantages, disadvantages and characterization methods.
2. Y. Wang et.al (2021) discussed about various influencing factors and drug
application using iontophoresis in TDDS.
3. Brenden Cheong Qi Seah et.al (2018) discussed about recent advances in
ultrasound based transdermal drug delivery.
4. NA Charoo et.al (2010) overviewed in vitro and in vivo studies demonstrating
therapeutic benefits offered by electroporation assisted permeation.
5. Tejashree Waghule et.al (2019) discussed about micro needles as a smart
approach and its increasing potential for TDDS.
24. Challenges and Opportunities
Challenges
Developing TDD technologies faces challenges such as achieving sufficient
drug permeation through the skin barrier.
Passive methods such as chemical enhancers have had limited success in
increasing transdermal transport of large molecules.
Opportunities
Advances in these TDDS could provide the driving force for controlling
prevalence of diseases of CVS and CNS, diabetes, neuromuscular diseases,
genetic diseases, and infectious and localized infectious diseases.
Spearheading advances in vaccination and supporting patient preference for
self-administration of drugs for long-term treatment.
They also have the potential to enable controlled and sustained release,
allowing for more precise therapeutic outcomes.
25. Conclusion
TDDS is non-invasive, non allergenic, and has a set duration and dose
delivery method.
TDDS allows uniform distribution of drugs at prescribed and controlled rates.
TDDS technology is growing rapidly in the pharmaceutical field and has
succeeded in capturing key value in the market for biomedical applications
as a formulation system that can improve drug delivery through topical
routes.
27. References:
1. Wang Y, Zeng L, Song W, Liu J. Influencing factors and drug application of iontophoresis in transdermal drug
delivery: an overview of recent progress. Drug Delivery and Translational Research. 2021 Jan 23:1-2.
2. Seah BC, Teo BM. Recent advances in ultrasound-based transdermal drug delivery. International journal of
nanomedicine. 2018 Nov 20:7749-63.
3. Nguyen HX, Banga AK. Electrically and ultrasonically enhanced transdermal delivery of methotrexate.
Pharmaceutics. 2018 Aug 5;10(3):117.
4. A Charoo N, Rahman Z, A Repka M, N Murthy S. Electroporation: an avenue for transdermal drug delivery. Current
Drug Delivery. 2010 Apr 1;7(2):125-36.
5. Agrawal S, Gandhi SN, Gurjar P, Saraswathy N. Microneedles: An advancement to transdermal drug delivery system
approach. Journal of Applied Pharmaceutical Science. 2020 Mar 5;10(3):149-59.
6. Hajare AA, Salunkhe SS, Mali SS, Gorde SS, Nadaf SJ, Pishawikar SA. Review on: High-throughput screening is an
approach to drug discovery. Am. J. Pharm. Tech. Res. 2013;4:112-29.
7. Zaid Alkilani A, McCrudden MT, Donnelly RF. Transdermal drug delivery: Innovative pharmaceutical developments
based on disruption of the barrier properties of the stratum corneum. Pharmaceutics. 2015 Oct 22;7(4):438-70.
8. Babaie S, Del Bakhshayesh AR, Ha JW, Hamishehkar H, Kim KH. Invasome: A novel nanocarrier for transdermal
drug delivery. Nanomaterials. 2020 Feb 17;10(2):341