Unit:
Department of ChemistryLibrary of the School of Science
Author:
Panagiotaki Aikaterini
Dissertation committee:
Μαρίνος Πιτσικάλης, Καθηγητής, Τμήμα Χημείας, ΕΚΠΑ
Ερμόλαος Ιατρού, Καθηγητής, Τμήμα Χημείας, ΕΚΠΑ
Ωραιοζήλη Σιδεράτου, Ερευνήτρια Α, ΙΝΝ, ΕΚΕΦΕ "Δημόκρητος"
Γεώργιος Σακελαρίου, Αναπληρωτής Καθηγητής, Τμήμα Χημείας, ΕΚΠΑ
Γεώργιος Βουγιουκαλάκης, Επίκουρους Καθηγητής, Τμήμα Χημείας, ΕΚΠΑ
Δημήτριος Τσιούρβας, Ερευνητής Α, ΙΝΝ, ΕΚΕΦΕ "Δημόκρητος"
Μαρία Παραβατού, Ερευνήτρια Β, ΙΝΝ, ΕΚΕΦΕ "Δημόκρητος"
Original Title:
Καινοτόμα νανο-υλικά με βάση λειτουργικά δενδριτικά πολυμερή για βιολογικές εφαρμογές
Translated title:
Innovative functionalized dendritic polymers based nano materials for biological applications
Summary:
It is well established in the literature that drug delivery systems incorporating triphenylphosphonium groups are very effective in targeting the mitochondria of cells, particularly tumor cell mitochondria. In this research, drug delivery systems based on functionalized dendritic polymers were developed bearing on their surface triphenylphosphonium groups (TPP) through an alkyl chain having either 3 or 10 carbon atoms. The dendritic polymers that were synthesized are derivatives of hyperbranched poly(ethylenimine) of two different molecular weights (1300 and 5000 Da). In these systems the bioactive molecules of doxorubicin and chloroquine were encapsulated. Bioactive molecules were entrapped in the nanocavities of dendritic systems and their biological activity and intracellular localization was studied against a variety of cancer cell lines. Also, the effect of the nanoparticles with the encapsulated drugs was investigated in the cell cycle of cancer cells. Based on the obtained results, it was found that most effective system was the derivative of poly(ethylenimine) of molecular weight 1300 with the TPP groups attached through a spacer of decyl chain, that was found to improve considerably the anticancer effect of both drugs due to their successful accumulation in cell mitochondria.
It is known from the literature that systems carrying triphenyphosphonium groups also exhibit enhanced antibacterial properties. Thus, all above derivatives were also studied for their antibacterial activity towards two bacterial strains, one gram (-), i.e. Escherichia coli, and one gram (+), i.e. Staphylococcus Aureus. The rate of bacteria growth, toxicity, oxidative stress and morphological changes in the presence of the TPP-functionalized hyperbranched derivatives was studied. It was found that the derivatives of hyperbranched poly(ethylenimine) of both molecular weights functionalized with decyl-triphenylphosphonium groups are more toxic, while in all cases the tested derivatives showed higher potency against gram (+) Staphylococcus Aureus bacteria.
Main subject category:
Science
Keywords:
dendritic polymers, hyperbranched poly(ethylenimine), nanoparticles, drug nanocarriers, doxorubicin, antibacterial materials, antibacterial properties, bacteria.
