Ciência sem Fronteiras (Science Without Borders)
DIT PhD Project
Supervisor name & contact details:
Name Dr Christine O’Connor
Email Christine.oconnor@dit.ie
Supervisors Profile:
Dr Christine O’Connor, Assistant Head of
School of Food Science and Environmental
Health in DIT. She has been a Chemistry
Lecturer in the School of Chemical and
Pharmaceutical Sciences from 2000 - 2014.
Prior to that she had studied in Dublin City
University with Prof Han Vos where she was
awarded a PhD in the Synthesis and
characterisation of novel Ruthenium (II)
complexes. She has more recently supervised
postgraduate students in the areas of
‘synthesis of novel drug delivery vehicles’ and
‘the design and evaluation of novel metal
complexes for therapeutic applications’.
Christine is a member of the Inorganic, Pharma
and Biomimetic Reseach Centre (IPBRC) and is
based in the Materials Synthesis and
Applications Lab (MSA) in the FOCAS Institute
of DIT. For further information and publications
please see:
http://www.dit.ie/fseh/stafflisting/christineoco
nnor/
http://arrow.dit.ie/do/search/?q=author_lnam
e%3A%22O%27Connor%22%20author_fname
%3A%22Christine%22&start=0&context=49073
8
Research Centre (if applicable):
Inorganic, Pharma and Biomimetic Research
Centre
Research Centre website (if applicable):
http://www.dit.ie/ipbrc/
Supervisors Publication List:
http://www.dit.ie/fseh/stafflisting/christineoco
nnor/
http://arrow.dit.ie/do/search/?q=author_lnam
e%3A%22O%27Connor%22%20author_fname
%3A%22Christine%22&start=0&context=49073
8
Title of the Project: Targeting Therapeutics using Drug Delivery Vehicles.
Project Summary: The use of biocompatible macromolecules such as Cyclodextrin’s (CD) as drug
delivery vehicles has advanced in recent years. The use of drug delivery vehicles broadens the
applications of commonly known drugs. It is known that many commercially viable therapeutics
are not used in the clinic as they do not discriminate from the target diseased site and that of the
healthy cells and cause side effects that outweigh the therapeutic effect of the drug. This is of
particular relevance when dealing with chemotherapeutic drugs when the patients’ immune
system is severely compromised. The use of a drug delivery vehicle that targets the diseased site
and allows the host drug to achieve its function has many advantages such as;
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Lower dosage required of drug
Less side effects to patient
Decrease in cost of therapy
Increase use of commercially available drugs to the clinic
Chemical modification of CDs has shown to extend the physicochemical properties and the host
capacity for a variety of pharmaceutical drugs. In particular β-CD has been widely used in the
early stages of pharmaceutical applications because of its ready availability and its cavity size
suitability for a wide range of drugs. Folate Receptors are over-expressed in several human
cancers including ovarian, breast and renal carcinomas and Tofzikovskyaya (2014) have shown
that folate-cyclodextrin bioconjugates are successful in targeted therapy as opposed to direct
conjugation of folate to the bioactive molecules which leads to loss of targeting or an alteration
of the function of the conjugate and most of the conjugates to date cannot be further modified
to improve targeting or anti-tumour activity. This project entails some chemical synthesis of the
folate-cyclodextrin bioconjugate as described by Clementi (2010) and more recently by
Tofzikovskyaya (2012). All starting materials, intermediates and products will require
spectroscopic characterisation on electronic (UV/Vis), vibrational (IR and Raman), NMR, and Mass
Spectroscopy’s in the FOCAS Institute and in the School of Food Science and Environmental
Health at DIT. The therapeutics required for targeting will be commercially acquired. The chosen
target will be breast cancer initially. This research will be carried out in collaboration with Prof
Mary McNamara.
1. In vitro evaluation of the cytotoxicity of a folate-modified β-cyclodextrin as a new anticancer drug delivery system, Z. Tofzikovskaya, A. Casey, O. Howe, C. O’Connor and M.
McNamara, Journal of Inclusion Phenomena and Macrocyclic Chemistry, July 2014, DOI:
10.1007/s10847-014-0436-0.
2. Synthesis, characterisation and photo-stability of a folate-modified β-cyclodextrin as a
functional food additive, Z. Tofzikovskaya, C. O’Connor and M. McNamara, Journal of
Inclusion Phenomena and Macrocyclic Chemistry, 2012, 74(1-4), 437-445.
3. Synthesis and characterization of a colloidal novel folic acid–β-cyclodextrin conjugate for
targeted drug delivery, A. Clementi, M. C. Aversa, C. Corsaro, J. Spooren, R. Stancanelli, C.
O’Connor, M. McNamara and A. Mazzaglia, Journal of Inclusion Phenomena and
Macrocyclic Chemistry, 2010, DOI: 10.1007/s10847-010-9738-z.
Ciência sem Fronteiras / Science Without Borders Priority Area:
Health and Biomedical Sciences