Complexation and organization of doxorubicin on polystyrene sulfonate chains: impacts on doxorubicin dimerization and quenching

Gjerde, Natalie; Nardi, Alessandro Nicola; Chen, Cheng Giuseppe; Gianvincenzo, Paolo Di; D’Abramo, Marco; Scipioni, Anita; Galantini, Luciano; Moya, Sergio; Giustini, Mauro

doi:10.1039/d2cp02714c

Cited by 7 publications

(2 citation statements)

References 21 publications

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“…Doxorubicin occurs in the complexes as monomers because, as a dimer, it is characterized by a practically complete lack of fluorescence (Φ DIM = 10 −5 ). DOX monomers have a very high fluorescence yield, Φ MON = 3.9 × 10 −2 [ 42 , 43 ]. The phenomenon of fluorescence in G4.0 PAMAM-DOX systems not only confirms the presence of the drug in the carrier structure but also proves that it exists in a monomeric form.…”

Section: Resultsmentioning

confidence: 99%

Effect of Alkaline Conditions on Forming an Effective G4.0 PAMAM Complex with Doxorubicin

Szota

Jachimska

2023

Pharmaceutics

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In this study, special attention was paid to the correlation between the degree of ionization of the components and the effective formation of the complex under alkaline conditions. Using UV-Vis, 1H NMR, and CD, structural changes of the drug depending on the pH were monitored. In the pH range of 9.0 to 10.0, the G4.0 PAMAM dendrimer can bind 1 to 10 DOX molecules, while the efficiency increases with the concentration of the drug relative to the carrier. The binding efficiency was described by the parameters of loading content (LC = 4.80–39.20%) and encapsulation efficiency (EE = 17.21–40.16%), whose values increased twofold or even fourfold depending on the conditions. The highest efficiency was obtained for G4.0PAMAM-DOX at a molar ratio of 1:24. Nevertheless, regardless of the conditions, the DLS study indicates system aggregation. Changes in the zeta potential confirm the immobilization of an average of two drug molecules on the dendrimer’s surface. Circular dichroism spectra analysis shows a stable dendrimer-drug complex for all the systems obtained. Since the doxorubicin molecule can simultaneously act as a therapeutic and an imaging agent, the theranostic properties of the PAMAM-DOX system have been demonstrated by the high fluorescence intensity observable on fluorescence microscopy.

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Section: Resultsmentioning

confidence: 99%

Effect of Alkaline Conditions on Forming an Effective G4.0 PAMAM Complex with Doxorubicin

Szota

Jachimska

2023

Pharmaceutics

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“…The fluorescence properties of DOX can help study carrier-drug interactions and imaging in biological systems [42,43]. In the present study, fluorescent properties of doxorubicin were used to determine G4.0-DOX binding constants (Ka) by fluorescence quenching through the presence of a dendrimer (Figure 4).…”

Section: Binding Constants and Thermodynamic Parameters Of G40-doxmentioning

confidence: 99%

Dendrimer Platforms for Targeted Doxorubicin Delivery – Physicochemical Properties in Context to Biological Responses

Szota,

Szwedowicz,

Rembiałkowska

et al. 2024

Preprint

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The unique structure of G4.0 PAMAM dendrimers allows the drug to be enclosed in internal spaces or immobilized on the surface. In the conducted research, the conditions for the formation of the active G4.0 PAMAM complex with doxorubicin (DOX) were optimized. The physicochemical properties of the system were monitored using DLS, CD, and fluorescence spectroscopy. The QCM-D method was chosen to determine the preferential conditions for the complex formation. The highest binding efficiency of the drug to the cationic dendrimer was observed under basic conditions when the DOX molecule was deprotonated. The decrease in the zeta potential of the complex confirms that DOX immobilizes through electrostatic interaction with the carrier's surface amine groups. The binding constants were determined from the fluorescence quenching of the DOX molecule in the presence of G4.0 PAMAM. The two-fold way of binding doxorubicin in the structure of dendrimers was visible in the ITC isotherm. Fluorescence spectra and release curves identified reversible binding of DOX to the nanocarrier. Among the selected cancer cells, the most promising anticancer activity of G4.0-DOX was observed in A375 malignant melanoma cells. Moreover, the preferred intracellular location of the complexes concerning the free drug was found, which is important from a therapeutic point of view.

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Fluorescence Label‐Free Doxorubicin Sensor Using Polystyrene Sulfonate as a Synthetic Receptor in Whispering Gallery Mode Microresonators

Maurina,

Domac,

Olszyna

et al. 2024

Advanced Sensor Research

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The conventional quantification of Doxorubicin (DXR), a crucial anticancer drug, typically relies on complex and expensive techniques, limiting measurements beyond hospital settings and at different time intervals. Here, a label‐free fluorescence sensor is presented for DXR utilizing Whispering Gallery Mode (WGM) resonators. The resonators are based on fluorescent microparticles coated with a nanometer‐thick polystyrene sulfonate (PSS) layer serving as a synthetic receptor. The sensor demonstrates linear response for both position and width of the resonance peaks within the concentration range of 1–10 µg mL−1 of DXR of clinical interest. It also exhibits good selectivity against other chemotherapy drugs and can operate in complex biological fluids. The findings underscore the potential of WGM resonators as versatile multiparameter sensors for the sensitive and selective detection of small molecules, also in complex biological media.

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Complexation and organization of doxorubicin on polystyrene sulfonate chains: impacts on doxorubicin dimerization and quenching

Abstract: The anthracycline doxorubicin hydrochloride (DX) is a positively charged fluorescent drug, which associates into non fluorescent antiparallel dimers with increasing concentration and/or ionic strength. The positive charge of DX allows...

Cited by 7 publications

References 21 publications

Effect of Alkaline Conditions on Forming an Effective G4.0 PAMAM Complex with Doxorubicin

Effect of Alkaline Conditions on Forming an Effective G4.0 PAMAM Complex with Doxorubicin

Dendrimer Platforms for Targeted Doxorubicin Delivery – Physicochemical Properties in Context to Biological Responses

Fluorescence Label‐Free Doxorubicin Sensor Using Polystyrene Sulfonate as a Synthetic Receptor in Whispering Gallery Mode Microresonators

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