Nanocarrier systems assembled from PEGylated hyperbranched poly(arylene oxindole)

• Published in: European polymer journal 2019-10, Vol.119, p.247-259
• Main Authors: Soultan, Al Halifa, Lambrechts, Dennis, Verheyen, Thomas, Van Gorp, Hans, Roeffaers, Maarten B.J., Smet, Mario, De Borggraeve, Wim M., Patterson, Jennifer
• Format: Article
• Language: English
• Subjects: Alkynes; Biocompatibility; Cellular uptake; Cisplatin; Cycloaddition; Derivatives; Diagnostic software; Diagnostic systems; Drug release; Fluorescein; Hyperbranched polymers; Medicine; Nanomaterials; Nanoparticles; PEGylation; Polymers; Self-assembly; Zeta potential
• ISSN: 0014-3057; 1873-1945
• DOI: 10.1016/j.eurpolymj.2019.07.029

[Display omitted] •New amphiphilic hyperbranched poly(arylene oxindole)s by PEGylation using CuAAC.•Spherical nanoparticles with tunable size and zeta potential from PEGylation degree.•Efficient loading and release of compounds interacting with poly(arylene oxindole).•Nanoparticles demonstrate fast cellular uptake with low intercellular variability.•Intracellular accumulation of fluorescent nanoparticles correlates with dose. Nanoparticles (NPs) formed from hyperbranched polymers are highly attractive organized structures in nanomedicine. Herein, we utilize copper-catalyzed azide-alkyne cycloaddition of hyperbranched poly(arylene oxindole) derivatives to prepare amphiphilic conjugates with different degrees of PEGylation that form spherical NPs in water with tunable particle diameters (25 ± 5 nm for PEG0.3-NPs and 120 ± 10 nm for PEG0.1-NPs) and zeta potential (−7 ± 2 mV for PEG0.3-NPs and −23 ± 3 mV for PEG0.1-NPs). Cisplatin and BODIPY derivatives can be loaded into the PEG0.1-NPs, and their release over 5 d depends on the physicochemical properties of the payload. Moreover, changing the time and conditions for self-assembly leads to the formation of polymer vesicles that can encapsulate and release hydrophilic cargo, as shown with fluorescein. In vitro cellular uptake experiments demonstrate that at concentrations ≤10 μg/mL the BODIPY-loaded NPs do not induce morphological differences or cause a reduction in metabolic activity of the cells, confirming their cytocompatibility. They are rapidly taken up by ATDC5 cells and remain stable for 7 d thus highlighting their potential as carrier systems for diagnostic or therapeutic applications.