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Lactobionic Acid and Carboxymethyl

Chitosan Functionalized Graphene Oxide


Nanocomposites as Targeted Anticancer
Drug Delivery Systems
Learning Outcome
 To understand the definition of targeted release
 To understand the differences between conventional release
and targeted release
 Knowing and understanding the reason why targeted release
is chosen by the researchers
 Understanding the manufacturing method and the evaluation
process
 Discuss the results and conclusion of the research
 To know one of targeted release product that has been
marketed
What is the advantage
What is targeted drug delivery
of targeted drug
system?
delivery system?
• Increase specific
localization
• Increased
treatment efficacy
• Decreased toxic
side effect
• Reduce dose
• Improved patience
compliance
Rationale of developing targeted
drug delivery
• GO (graphene oxide)
modified to prevent
aggregation and ensure
compatibility with biological
tissue
• CMC, can be used to modify
GO (graphene oxide) to
improve its dispersibility in
water and physiological fluids
through covalent
funtionalization.
• CMC-modified GO to prepare
doxorubicin-loaded
hyaluronic acid-
functionalized system for
targeted delivery to cancer
cells.
BACKGROUND & EXPLANATION
OF RESEARCH
Anti-cancer drug
delivery system
Drug delivery system based on (targeted release)

• Graphene oxide (GO)


• Carboxymethyl chitosan (CMC) GO-CMC-LA would permit their
selective uptake by cancerous
• Lactobionic acid (LA) cells with only minimal uptake by
non cancerous cells

LA
functionalize Rapid release at lower pH
GO-CMC d Loaded typical of cancer cell
materials with DOX microenvironment than at
LA free general physiological pH
Method of Manufacturing

 Materials and
Methods
 Synthesis and
Purification
 GO-CMC
 GO-CMC-FI-LA-Ac
 GO-CMC-FI-Ac
 Characterization
Evaluation & Result

1. Structure Identification
2. Morphological Examination
3. Verify Compositions of the Composites
4. DOX Loading
5. DOX Release
6. Cell Viability
7. Cellular Uptake Assay
8. In Vitro Selectivity Assay
Market Product
• TECENTRIQ provides a new treatment option
for people with previously treated locally
advanced or metastatic non-small cell cancer
(NSCLC)
• Tecentriq is a programmed death-ligand 1
(PD-L1) blocking antibody indicated for the
treatment of patients with locally advanced or
metastatic urothelial carcinoma (also called
transitional cell carcinoma) and metastatic
non-small cell lung cancer.
• Tecentriq is the first PD-L1 inhibitor that works
by blocking the PD-L1 pathway which may
help the body’s own immune system fight off
the cancer cells
Conclusion

 The resultant formulations have high drug loading content and efficiency (>96%) and pH-sensitive release.
Release is both more rapid and reaches a greater extent at the mildly acidic pH typical of the tumor
microenvironment than at pH 7.4. In vitro tests on a liver cancer cell line demonstrated that while the GO
composites are not cytotoxic, the DOX-loaded systems are effective in inducing cell death, being almost
as potent as the free drug. Further, the DOX-loaded lactobionic acid conjugated GO system was able to
selectively induce the death of cancerous cells, but was non-toxic to a non-cancerous cell line. These
promising results show that the GO-based systems generated in this work have great potential for
targeted anticancer therapy in vivo.

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