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Article

Synthesis, Self-Assembly and In Vitro Cellular Uptake Kinetics of Nanosized Drug Carriers Based on Aggregates of Amphiphilic Oligomers of N-Vinyl-2-pyrrolidone

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Department of Biomaterials, D. Mendeleev University of Chemical Technology of Russia, 125047 Moscow, Russia
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Centre for Strategic Planning of FMBA of Russia, 119121 Moscow, Russia
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Department of Materials and Production, Aalborg University, Skjernvej 4A, 9220 Aalborg, Denmark
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Department of Health Science and Technology, Aalborg University, Fredrik Bajers Vej 3B, 9220 Aalborg, Denmark
*
Authors to whom correspondence should be addressed.
Academic Editor: Katarzyna Winnicka
Materials 2021, 14(20), 5977; https://doi.org/10.3390/ma14205977
Received: 13 August 2021 / Revised: 7 October 2021 / Accepted: 8 October 2021 / Published: 11 October 2021
(This article belongs to the Special Issue Nanomaterials for Drug Delivery Application)
Development of nanocarrier-based drug delivery systems is a major breakthrough in pharmacology, promising targeted delivery and reduction in drug toxicity. On the cellular level, encapsulation of a drug substantially affects the endocytic processes due to nanocarrier–membrane interaction. In this study we synthesized and characterized nanocarriers assembled from amphiphilic oligomers of N-vinyl-2-pyrrolidone with a terminal thiooctadecyl group (PVP-OD). It was found that the dissolution free energy of PVP-OD depends linearly on the molecular mass of its hydrophilic part up to M¯n = 2 × 104, leading to an exponential dependence of critical aggregation concentration (CAC) on the molar mass. A model hydrophobic compound (DiI dye) was loaded into the nanocarriers and exhibited slow release into the aqueous phase on a scale of 18 h. Cellular uptake of the loaded nanocarriers and that of free DiI were compared in vitro using glioblastoma (U87) and fibroblast (CRL2429) cells. While the uptake of both DiI/PVP-OD nanocarriers and free DiI was inhibited by dynasore, indicating a dynamin-dependent endocytic pathway as a major mechanism, a decrease in the uptake rate of free DiI was observed in the presence of wortmannin. This suggests that while macropinocytosis plays a role in the uptake of low-molecular components, this pathway might be circumvented by incorporation of DiI into nanocarriers. View Full-Text
Keywords: drug delivery; nanocarriers; endocytosis drug delivery; nanocarriers; endocytosis
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MDPI and ACS Style

Kulikov, P.P.; Luss, A.L.; Nelemans, L.C.; Shtilman, M.I.; Mezhuev, Y.O.; Kuznetsov, I.A.; Sizova, O.Y.; Christiansen, G.; Pennisi, C.P.; Gurevich, L. Synthesis, Self-Assembly and In Vitro Cellular Uptake Kinetics of Nanosized Drug Carriers Based on Aggregates of Amphiphilic Oligomers of N-Vinyl-2-pyrrolidone. Materials 2021, 14, 5977. https://doi.org/10.3390/ma14205977

AMA Style

Kulikov PP, Luss AL, Nelemans LC, Shtilman MI, Mezhuev YO, Kuznetsov IA, Sizova OY, Christiansen G, Pennisi CP, Gurevich L. Synthesis, Self-Assembly and In Vitro Cellular Uptake Kinetics of Nanosized Drug Carriers Based on Aggregates of Amphiphilic Oligomers of N-Vinyl-2-pyrrolidone. Materials. 2021; 14(20):5977. https://doi.org/10.3390/ma14205977

Chicago/Turabian Style

Kulikov, Pavel P., Anna L. Luss, Levi C. Nelemans, Mikhail I. Shtilman, Yaroslav O. Mezhuev, Igor A. Kuznetsov, Oksana Y. Sizova, Gunna Christiansen, Cristian P. Pennisi, and Leonid Gurevich. 2021. "Synthesis, Self-Assembly and In Vitro Cellular Uptake Kinetics of Nanosized Drug Carriers Based on Aggregates of Amphiphilic Oligomers of N-Vinyl-2-pyrrolidone" Materials 14, no. 20: 5977. https://doi.org/10.3390/ma14205977

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