This document provides an overview of targeted drug delivery systems (TDDS). It begins by defining TDDS as systems that selectively target or deliver medication only to its site of action or absorption. It then discusses the need for TDDS to maintain required drug levels at diseased sites while avoiding damage to healthy tissues. The document outlines various types of targeting approaches and drug delivery vehicles used in TDDS, including liposomes, monoclonal antibodies, and nanotechnology-based approaches. It also discusses targeting specific sites like the gastrointestinal tract, respiratory tract, and brain. Finally, it reviews some recent research on using TDDS to deliver therapies for COVID-19 patients more effectively to the damaged lungs.

1. TARGETED DRUG DELIVERY SYSTEM
Presented by : Ms. Tabassum Khaju Shaikh
F.Y M.Pharmacy [ Pharmaceutics ] Sem-1
Guided By : Mr. Devendra Visokar Sir

2. CONTENT’S
▪ Introduction
▪ Need of Targeteddrug delivery system
▪ Type’s of Targeted drug delivery
▪ Drug delivery vehicle
▪ Various Targeting site’s
▪ Research works on TDDS
▪ TDDS vehicles in Covid-19 patient’s
▪ Conclusion
▪ Reference

3. INTRODUCTION
• ‘Targeted drug delivery system is a special form of drug
delivery system where the medicament is selectively
targeted or delivered only to its site of action or
absorption’.
• Targeted drug delivery system is preferredover conventional
drug delivery systems due to three main reason’s.
i. Pharmaceutical properties– TDDShave Higher solubility &
drug stability
ii. Pharmacokinetic properties– TDDSposses high
Absorption, Good half life & Low volume of distribution.
iii. Pharmacodynamic properties – TDDS have High specificity
and High therapeutic index.

4. ❑ Characteristics of Targeted drug delivery system
• Should be biochemically inert.
• Should be non immunogenic.
• Should have therapeutic amount of drug release.
• Carriers used should be biodegradable.
• Should be physically and chemically stable in vivo and in vitro
conditions.
❑ Application of Targeted drug delivery system
• Targeted drug delivery can be used to treat many diseases, such as
cardiovascular diseases and diabetes. Most importantly in cancerous
tumors.
• Liposomes can be used as drug delivery for the treatment of
tuberculosis.

5. ❑ Generation of drug delivery system
• There are five generationsof drug delivery system.
Generationof drug delivery
First
Generation
DDS:
Tablet,
Capsule
Ointment
Suspension
Emulsion
Suppositories.
Second
Generation
DDS:
Repeat action
Tablet,
Prolongaction
Tablet,
Enteric coated
Tablet.
Third
GenerationDDS:
Osmotically
controlled system,
Swelling
controlled system,
Diffusion
controlled system
Fourth
GenerationDDS:
Targeted drug
delivery system
Modulated drug
delivery system
Self regulated
Drugdelivery
system
Fifth
Generation
DDS:
Genetherapy
under various
phase of
development

6. NEED OF TARGETED DRUG DELIVERY SYSTEM
• The need of this systemis to deliver the certain amount of drug
to the targeted diseasedarea withinthe body. This will help to
maintainthe requiredplasma level and tissuedrug level in the
body therefore avoiding any damage to the healthy tissuevia
drug.
Need of Targeted Drug Delivery
System
Pharmacokinetic
Reasons
Pharmacodynamic
Reasons
Pharmaceutical
Reasons
Low
Solubility
Drug
Instability

7. ❑ Advantages of TDDS
• TDDS reduces the side effects and toxicity.
• Dose of the drug reduces.
• It avoids the degradation of drug (first pass metabolism).
• Drug bioavailability increasesand fluctuation in concentration
decreases.
❑ Disadvantages of TDDS
• Advanced techniques and skilled personsare required.
• Sometimes it may causes toxicity and it is very difficult to
maintain stability of dosage forms.

8. TYPES OF TARGETED DRUG DELIVERY SYSTEM
▪ Active targeting - Employs a deliberatelymodified drug carrier
molecule capable of recognizingand interactingwith specific
cell tissue or organ in the body e.g., antigen specific antibody.
▪ Passive targeting - Drug delivery systems which are targeted to
systemic circulation are characterized as Passive delivery
systems.
Level’sof Drugtargeting
First order
targeting
Third order
targeting
Second order
targeting

9. There are different approachesto actively target drugs to the
site of action like ligands,immune reaction, external stimuli
etc.

10. • Ligand mediated targeting – Achievedusingspecific
mechanisms such as receptor dependent uptake of natural LDL
particles and synthetic lipidmicroemulsions of partially re
constitutedLDL particles coated with the apoproteins.
Ligands Target Tumor target
Folate Folate receptor Overexpressionof
folate
receptor
Transferrin Transferrin receptor Overexpressionof
transferrin
receptor
Galactosamine Galactosamine
receptors
on hepatocytes
Hepatoma

11. ▪ Inverse targeting - This approach leads to saturation of RES and
suppression of defense mechanism. This type of targeting is a effective
approach to target drug to non-RES organs.
▪ Dual targeting - In this targeting approach carrier molecule itself have
therapeutic activity and thus increase the therapeutic effect of drug. Ex,
Anti-viral Drug
▪ Double targeting – Targeting drug at specific site & Controlling the
rate of drug delivery to the target site, these both activity combined to
to target a carrier system, then targeting may be called double
targeting.
▪ Combination targeting - These targeting system is equipped with
cariers, polymers and homing devices of molecular specificity that
could provide a direct approach to target site.

12. DRUG DELIVERY VEHICLE
• Most important for successful transportation of the loaded
drug at the specific site.
❑ Characteristics of an ideal drug Vehicle
• Should be able to cross Blood Brain Barrier.
• It must be recognized by target cell’s.
• After recognition, system should releasethe drug inside the
target organs,tissues or cells.
• Non-toxic
• Non-immunogenic
• Biodegradable

13. ❑ Vehicles for targeting drugs :
▪ Liposomes - Liposomes are small artificially designed vesicles
composed of phospholipid bilayers surroundingwith the size
rangingfrom 20 to 10 000 nm. Encapsulation of drug used for
both active & passive targeting. These are extensively
researched for their application in non-viral vector mediated
gene therapy.
▪ Monoclonal antibodies and fragments - MABs are highly
specific and recognize only are antigenic determinantor
receptor site. MABs coupled with an active drug hold great
promisesfor site specific delivery of biological substances,
particularly in cancer chemotherapy.

14. .
▪ Modified plasma proteins – Intelligentdrug vehicle, Bcz of
there solubility & low Molecular weight, Easily get modified
with attachments of differentmolecules( sugar, peptides,
ligands) . Extensive modification are used in liver cell
targeting.
▪ Quantum dots - Quantum dots are miniscule semiconductor
particles that can serve as sign posts of certain types of cells
or molecules in the body. Technique has potential for
targeting cancerous drug.

15. ▪ Microspheresand nanotechnology– Microspheresare,
Microcapsulation in which solid is envoloped in membrane that
may be impermiable or semi-permiable. With particle size
200μm, important approach in delivering drug with sustain &
controlled manner EX, Narcotic, Antagonist, Steroid hormones.
▪ Lipoproteins – LDL & HDL are natural targeted liposomes,it’s
core used to incorporate lipophilicdrugs and it does not require
covalent bondingwith the drug. Used for drug targeting liver.

16. ADVANCED CARRIERS FOR TARGETING DRUGS
▪ NanoTubes - They are hollow cylinder made of carbon,
atoms which can be filled and sealed for potential drug
delivery.
Cellular scale needle for attaching drug molecule to cancer
cells. As an electrode in thermo cells.
▪ Nano wires - the nanowire pinpointdamage from injury and
stroke, localize the cause of seizures,

17. and detect the presence of tumors and other brain
abnormalities.
Techniquehas potential as a treatment for Parkinson's and similar
diseases.
▪ Nanoshells - Nanoshells are hollow silica spheres covered with
gold. Scientists can attach antibodies to their surfaces, enabling
the shells to target certain shells such as cancer cells.

18. Technique has potential for targeting cancerous drug.
 Nano pores - Engineered intoparticles, they are holes that are
so tiny that DNA molecules can pass through them one strand at
a time, allowingfor highly precise and efficient DNA sequencing.
Potential in genetic engineeringand bio technology.

19. ▪ Gold Nano Particle - Scientist uses gold nanoparticle to
develop ultrasensitive detection system for DNA and protein
markersassociated with many forms of cancer, including breast
prostrate cancer.
In cancer Treatment and Genetic engineering.
▪ Dendrimers - Dendrimers precisely defined, synthetic
nanoparticles that are approximately 510 nm in diameter. They are
made up of layers of polymer surroundinga control core. The
dendrimers surface contains many differentsites to which drugs
may be attach.

20. In gene transfection, medical imaging.

21. VARIOUS TARGETING SITES
▪ Targeting GIT :
• Various site-specific oral controlled release systems have
been developed dependingupon the target site which can be
classified as:
I. Systems targeted at stomach / duodenum
II. Systems targeted at small intestine
III. Systems targeted at lymphatic
IV. Systems targeted at colon
▪ Systems targeted at stomach duodenum:
• Prolongsstomach residence time, Active ingredientsreach at
optimum absorption site, Generallyincludes drugs ( insoluble
in GIT fluid, Drugs having site-specific action on
stomachdeodenum,Highly acidic drugs ).

22. ▪ Systems targeted at small intestine:
• Used to permit safe passage of system through acidic
environment of the stomach. Generallyincludes ( drugs
destroyed by gastric acid, drugs irritatingto gastric mucosa &
with site specific action ).
▪ Systems targeted at lymphatic:
• Lymphatic system consists of a network of vessels through
the small and large intestines which are involved in the
potential uptake of particulate administered drugin
micrometer range. Generallyused for ( To avoid first pass
metabolism, mesenteric lymphatic treatment, Inhibition of
cancer cell metastasis, highly hydrophobic drugs )

23. ▪ Systems targeted at colon:
• The delivery of drugs to the colon for local effect is valuable
in a variety of conditions like inflammatory bowel diseases
(e.g., Ulcerative colitis and Crohn’s disease), infectious
diseasesand colon cancer. Have a higher residence time so
increase the absorption of poorly absorbing drug material.
• Mainly this system is used for,
i. Drugs with site-specific action in colon
ii. For macromolecules like proteins& peptides
iii. Poorly absorbing drugs
iv. To avoid first pass metabolism

24. ▪ Targeting the respiratory tract :
• GenerallyBronchodilator & Anti-inflammtory steroidsused
for effective control on asthma.
• Used for local & systemic effect & also for,..
i. Avoiding first pass effect.
ii. Rapid onset of action.
iii. Better patient compliance.
iv. To enhance bioavailability.
v. For protein & peptide
drug moieties.

25. ▪ Targeting the brain :
• The blood brain barrier (BBB) is a unique protective barrier that
providesa very efficient exclusion of variety of blood
components by obstructing free flow of blood between brain &
rest of body. Also restricts the penetration of hydrophilic drugs,
unless these are transported to the brain by an active transport
system.
• Ex, dopamine was delivered using the N1- substituted
dihydropyridine pyridiniumsalt type redox system.

26. RESEARCH WORKS ON TARGETED DRUG DELIVERY SYSTEM
S.N
o
Active
ingredient
Other
ingredient
Method
employed
Effect
1 Meloxicam Ethyl cellulose Tablet
Compre-
ssion
and coating
Retarded the drug
releaseupto 12hrs and
shows
max. of 98.69% drug
release
2 Paracetamol Dextrin,
Polysaccha
ride
Wet
granulation
Tablet containing dextrin
as a carrier and ethyl
celluloseas a binder
found to be suitable for
targeting paracetamolfor
localaction in the
colon Matrix tablets
containing dextrin
released
95-98% paracetamol.

27. .
S.
No
Active
ingredient
Other
ingredient
Method
employed
Effect
3 Doxorubicn
hydrochloride
Chitosan HPLC In-vitro release of
doxorubicinis of zero
order kinetic. This shows
that release is independent
of the concentrationof
drug loaded in the
nanospheres.
4 Diltiazen HCL
and
indomethacin
Polysaccha
ride,
inulin and
shellac
Tablet
compression
and coating
Studies revealedthat the
tablet coated with
inulin and shellachave
limited the drug release
in stomach and small
intestine. And released
maximum amount of drug
in in colonic
environment.

28. TARGETED DELIVERY VEHICLES OF THERAPEUTICS
COVID-19 PATIENT’S
• All treatments rely on systemic delivery but COVID-19 damages
the lungs preferentially.
• So use of a targeted delivery approach is reviewedwhere
engineeredproducts are able to reach damaged lung tissue
directly.
• Only 2 pharmaceuticals have demonstratedsignals toward
efficacy, Remdesivir& Dexamethasone.
• Targeted drug delivery of these promisingpharmaceuticals
might prove to be more effective, enhancingthe local effect.
• SARS-CoV-2 has an affinity for 2 host cell factors, ACE-2 and
TMPRSS2.

29. SOME OF THE NEWER APPROACHES FOR TARGETED DRUG
DELIVERY IN COVID-19 PATIENTS
▪ Microbubbles - Microbubbles specifically have shownto adhere
to sites of damaged vascularendothelium and thus may be a
method of systemically targetingdelivery of therapeutics to
damaged lungs with SARS-CoV-2.
▪ Extracellular Vesicles (EV)- EVs play a criticalrole in cell-to-
cell communications and can be used as uniquedrug carriers to
deliver proteaseinhibitors to treat COVID-19.

30. Covid-19 & Extracellular Vesicles (EV)
(Isolation and drug encapsulationtechniques employed to engineer EVs
could result in the loss of functional properties of the Evs.)

31. ▪ Adenosine Nanoparticles - The efficacy in mitigating
inflammation was demonstrated through the targeted delivery of
adenosineand of multidrug formulations. This nanoparticle
improves the bioavailability ofboth drugs with significant
pharmaceuticalactivity, so several clinicalstudies planned to use
this technology in patients with COVID-19.
▪ Direct Pulmonary Delivery - Directpulmonary delivery (e.g.,
aerosol, inhalers, etc.) is a more selective mode of drug delivery.
Currently, 2 studies are enrolling - the NOSARSCOVID PhaseII
Trial and the Pulsed Inhaled Nitric Oxidefor Treatment of
Patients with Mildor Moderate COVID-19.
▪ Catheter-Based Drug Delivery - Catheter-basedlocal drug
delivery of antivirals (liquid remdesivir)and/or pro-
inflammatory cytokineinhibitors (tocilizumab)can be
performed trans-pulmonary, with a Swan-Ganzcatheter.

32. CONCLUSION
• Delivery of drug molecule to reach its specific siteis itself a
difficulttask. Finally, a targeted drug delivery is coming towards
as an advanced techniqueusedin the treatment of lethal
diseases.
• The advantage of this techniquehas been the reductionin dose
and side effects of the drug.
• Overall it may be concluded as wiser technique.

33. REFERENCE
▪ Aman Kumar1*, Ujjwal Nautiyal1, Charanjeet Kaur, Vaishali
Goel1,Neha Piarchand. Targeted Drug Delivery System: Currentand
Novel Approach, (Review article)
▪ Mrs Jaya Agnihotri*1, Dr.Shubhini Saraf2, Dr.Anubha Khale
.11,3M.E.S. Instititute’s, TARGETING : NEW POTENTIALCARRIERS
FOR TARGETTED DRUG DELIVERYSYSTEM(Review article)
▪ Gupta Manish and Sharma Vimukta. Targeted drug delivery system:
(A Review )
▪ : H. S. Mahajan, S. B. Patil*, S. G. Gattani*, B. S. Kuchekar** Targeted
drug delivery systems
▪ ,Kirti Rani*, Saurabh Paliwal A Review on Targeted Drug Delivery:
its EntireFocus on Advanced Therapeutics andDiagnostics.

34. ▪ Nicholas Kipshidze, PatrickIversen, Thomas R. Porter, Nodar
Kipshidze, Fakiha Siddiqui, George Dangas, and Jawed Fareed,
Targeted, Site-Specific, Delivery Vehicles of Therapeutics for
COVID-19Patients.
• Banker GS, Rhodes CT. In: Modern Pharmaceutics, 3rded.
MarcelDeckerInc: New York;1996.

35. THANK YOU