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Novel Polyhedral Silsesquioxanes [POSS(OH)32] as Anthracycline Nanocarriers-Potential Anticancer Prodrugs
Kinga Piorecka1, Jan Kurjata1, Wlodzimierz A Stanczyk1
1Centre of Molecular and Macromolecular Studies, Polish Academy of Sciences, Sienkiewicza 112, 90-363 Lodz, Poland.
Abstract:
Anthracyclines belong to the anticancer drugs that are widely used in chemotherapy. However, due to their systemic toxicity they also exert dangerous side effects associated mainly with cardiovascular risks. The pathway that is currently often developed is their chemical and physical modification via formation of conjugated or complexed prodrug systems with a variety of nanocarriers that can selectively release the active species in cancer cells. In this study, six new nanoconjugates were synthesized with the use of polyhedral oligosilsesquioxanes [POSS(OH)32] as nanocarriers of the anticancer drugs anthracyclines-doxorubicin (DOX) and daunorubicin (DAU). These prodrug conjugates are also equipped with poly(ethylene glycol) (PEG) moieties of different structure and molecular weight. Water-soluble POSS, succinic anhydride modified (SAMDOX and SAMDAU) with carboxylic function, and PEGs (PEG1, PEG2 and PEGB3) were used for the synthesis. New nanoconjugates were formed via ester bonds and their structure was confirmed by NMR spectroscopy (1H-NMR, 13C-NMR, 1H-13C HSQC, DOSY and 1H-1H COSY), FTIR and DLS. Drug release rate was evaluated using UV-Vis spectroscopy at pH of 5.5. Release profiles of anthracyclines from conjugates 4-9 point to a range of 10 to 75% (after 42 h). Additionally, model NMR tests as well as diffusion ordered spectroscopy (DOSY) confirmed formation of the relevant prodrugs. The POSS-anthracycline conjugates exhibited prolonged active drug release time that can lead to the possibility of lowering administered doses and thus giving them high potential in chemotherapy. Drug release from conjugate 7 after 42 h was approx. 10%, 33% for conjugate 4, 47% for conjugate 5, 6, 8 and 75% for conjugate 9.
Insights
New nanoconjugates using polyhedral oligosilsesquioxanes [POSS(OH)32] loaded with anticancer drugs doxorubicin (DOX) and daunorubicin (DAU) show prolonged drug release. These POSS-anthracycline conjugates offer potential for reduced chemotherapy doses and improved safety profiles.
Area of Science:
- * Nanotechnology
- * Medicinal Chemistry
- * Pharmacology
Background:
- * Anthracyclines are vital anticancer drugs but cause severe cardiovascular toxicity.
- * Developing targeted drug delivery systems is crucial to mitigate anthracycline side effects.
- * Nanocarriers offer a promising strategy for selective drug release in cancer cells.
Purpose of the Study:
- * To synthesize novel nanoconjugates using polyhedral oligosilsesquioxanes [POSS(OH)32] as carriers for doxorubicin (DOX) and daunorubicin (DAU).
- * To evaluate the drug release profiles and structural characteristics of these new POSS-anthracycline prodrugs.
- * To assess the potential of these nanoconjugates in improving chemotherapy efficacy and safety.
Main Methods:
- * Synthesis of six new nanoconjugates by linking anthracyclines (DOX/DAU) to POSS nanocarriers via ester bonds, incorporating poly(ethylene glycol) (PEG) moieties.
- * Structural characterization using advanced NMR spectroscopy (1H, 13C, HSQC, DOSY, COSY), FTIR, and Dynamic Light Scattering (DLS).
- * In vitro drug release studies conducted using UV-Vis spectroscopy at pH 5.5 to determine release kinetics.
Main Results:
- * Successful synthesis and structural confirmation of novel POSS-anthracycline nanoconjugates (conjugates 4-9).
- * Demonstrated prolonged drug release over 42 hours, with rates varying from approximately 10% to 75% depending on the specific conjugate.
- * NMR and DOSY analyses confirmed the formation of the prodrugs, and DLS indicated their nanocarrier properties.
Conclusions:
- * The synthesized POSS-anthracycline nanoconjugates exhibit controlled and prolonged release of active anticancer drugs.
- * These nanoconjugates hold significant potential for enhancing chemotherapy by allowing dose reduction and minimizing systemic toxicity.
- * Further investigation into the therapeutic efficacy and safety of these novel nanodrugs is warranted.
