This document summarizes cancer targeting drug delivery systems. It discusses passive targeting using nanoparticles that accumulate in tumors via the enhanced permeability and retention effect. It also discusses active targeting using ligands conjugated to nanoparticles that bind to receptors overexpressed on cancer cells. Examples are given of nanoparticles, monoclonal antibodies, and immunoconjugates used in targeted drug delivery to treat various cancers. The conclusion states that an ideal targeted system would use both passive and active targeting approaches combined with advances in tumor biology and biomaterials.

1. CANCERTARGETTINGDRUGDELIVERY
SYSTEMS
Seminar presentation
Presented by-
OMPRAKASH SAHU
M.Pharm 1St Year
PHARMACEUTICS
I.S.F. COLLEGE OF PHARMACY MOGA
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2. Introduction
Targeted Therapy
Targeted Drug Delivery
Passive Targeting
Active Targeting
Conclusion
FLOWOF PRESENTATION

3. Cancer is a term for large group of different disease in
which cell divide and grow uncontrollably.
Cancer is leading cause of death worldwide. It
accounted for 7.9million death (around 13% of deaths)
in 2008.
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4. Cancer
targeting
Targeted
Therapy
Targeting
Drug
Delivery
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5.  Targeted therapy is a type of medication
that blocks the growth of cancer cells by
interfering with specific targets which are
needed for carcinogenesis and tumor growth.
 Targeted cancer therapies are more effective
than current treatments and less harmful to
normal cells.
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6. Small molecule drugs
Imatinib mesylate
Gefitinib
Erlotinib
Tam oxifen
Monoclonal antibodies
Trastuzum ab
Cetuxim ab
Bevazicum ab
Rituxim ab
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7. TARGETED
DRUG
DELIVERY
PASSIVE
TARGETING
ACTIVE
TARGETING
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8.  Enhance Permeability and Retention effect(EPR effect)
 Angiogenesis & Hyper vasculature (pore size of 100-780 nm)
 Drug delivery system of particle size less than 200 nm have greater
tendency to cross tumor vasculature(Enhance permeability effect).
Failure of Drug Delivery System to drain back into blood from the tumor
interstitial fluid(Retention Effect).
(A)Normal vasculature (B)Tumor vasculature
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9. Nano
carriers
Drug Name Indication
Nanoparticles Albumin
paclitaxel
Abraxane Metastatic
breast cancer
Doxorubicin Transdrug Hepatocarcino
ma
Liposome Doxorubicin Myocel Breast Cancer
Vincristine Onco-TCS Non-
Hodgkin’s
lymphoma
(PEGlyated) Doxorubicin Doxil Ovarian cancer
(PEGylated) Dounorubicin Daunoxomre Kapsol
Sacroma
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10.  Active targeting of the drugs can be achieved by
exploiting the unique features of the tumor cells which
are absent in normal cells.
 Tumor targets(over expressed on tumor cells)
 Tumor associated antigens
 Growth factor receptors
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11. Immunoconjugation
Radioactive
Substances
ADEPT
Drugs(or)
toxin
Genes Liposomes
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12. Radioimmuno therapy:-
 Radionuclide attached to antibody
 Usually β-emitters e.g 131I, 90Y
 Cytotoxic over a distance from its source depending on path
length
Antibody directed enzyme prodrug therapy:-
First
injection
• The monoclonal antibody is given(with the enzyme
attached)
2nd
Injection
(Hours
later)
• A second drug(the pro-drug)is given
Activatio
n
• The pro-drug comes into contact with the enzyme the
drug then able to destroy the cancer cells
Selectivit
y
• Enzyme antibody conjugate doesn’t attach to normal
cells and doesn’t affect them
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13. Drug immunoconjugates:-
Many drug immunoconjugate are prepared and evaluated for
their efficacy and cytotoxicity.
e.g Doxorubicin is coupled to anti-lewis Y(LeY)
antibody(BR96)
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14. Targets for Immunoconjugates
Some of the most exploited targets for antibody targeting are:
• High level of transferrin receptors
on glioma cells
Transferrin
Receptors
• Expressed in and around neoplastic
blood vessels during angiogenesisFibronectin
Epidermal growth
factor receptor2
• Expressed in neoplastic blood vessel
Vascular
endothelial
growth factor
Overexpressed in and around neoplastic
blood vessels during angiogenesis
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15.  Proteins and peptides can be used as potential targeting
moietis or ligands for many receptors
• Arg-Gly-Asp(RGD) tripeptides shows most
efficient bindingIntegrins
• Humanised Epidermal growth factor and Transforming
growth factor-α are use d as ligands
Epidermal Growth
Factor Receptors
• VEGF is used as ligandsVascular Endothelial
Growth Factor
Transferrin
receptors
Transferrin is used as ligand
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16.  The floate receptor is significantly upregulated on
many cancer cells compared to normal
tissue(ovarian,lungs,brain,head and neck tumors).
Conclusion:-
 An ideal tumor targeted systems have to be
developed using the principles of passive & active
targeting combined with the advances in field of tumor
biology and biomaterials.
 And multipurpose systems have to be developed
which can be used for treatment and diagnosis.
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17.  Vyas S.P,Khar R.K,Targeted and controlled
Drug Delivery Novel Carrier Systems;512-556.
 David R.khan,The use of Nano carriers for
Drug Delivery in Cancer therapy;Journal of
Cancer Science and Therapy(2010);058-062.
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