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Article

Structure-to-Efficacy Relationship of HPMA-Based Nanomedicines: The Tumor Spheroid Penetration Study

1
Institute of Macromolecular Chemistry, Czech Academy of Sciences, Heyrovskeho nam. 2, 162 06 Prague 6, Czech Republic
2
Faculty of Pharmaceutical Science, Sojo University, Ikeda 4-22-1, Nishi-ku, Kumamoto 860-0082, Japan
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(12), 1242; https://doi.org/10.3390/pharmaceutics12121242
Received: 1 December 2020 / Revised: 17 December 2020 / Accepted: 17 December 2020 / Published: 20 December 2020
(This article belongs to the Special Issue Design of Novel Polymeric Systems for Controlled Drug Delivery)
Nanomedicines are a novel class of therapeutics that benefit from the nano dimensions of the drug carrier. These nanosystems are highly advantageous mainly within cancer treatment due to their enhanced tumor accumulation. Monolayer tumor cells frequently used in routine preclinical assessment of nanotherapeutics do not have a spatial structural architecture that allows the investigation of the penetration of nanomedicines to predict their behavior in real tumor tissue. Therefore, tumor spheroids from colon carcinoma C26 cells and glioblastoma U87-MG cells were used as 3D in vitro models to analyze the effect of the inner structure, hydrodynamic size, dispersity, and biodegradability of N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-based nanomedicines carrying anticancer drug pirarubicin (THP) on the penetration within spheroids. While almost identical penetration through spheroids of linear and star-like copolymers and also their conjugates with THP was observed, THP penetration after nanomedicines application was considerably deeper than for the free THP, thus proving the benefit of polymer carriers. The cytotoxicity of THP-polymer nanomedicines against tumor cell spheroids was almost identical as for the free THP, whereas the 2D cell cytotoxicity of these nanomedicines is usually lower. The nanomedicines thus proved the enhanced efficacy within the more realistic 3D tumor cell spheroid system. View Full-Text
Keywords: HPMA polymers; pirarubicin; tumor spheroids; penetration; cytotoxicity HPMA polymers; pirarubicin; tumor spheroids; penetration; cytotoxicity
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MDPI and ACS Style

Kudláčová, J.; Kotrchová, L.; Kostka, L.; Randárová, E.; Filipová, M.; Janoušková, O.; Fang, J.; Etrych, T. Structure-to-Efficacy Relationship of HPMA-Based Nanomedicines: The Tumor Spheroid Penetration Study. Pharmaceutics 2020, 12, 1242. https://doi.org/10.3390/pharmaceutics12121242

AMA Style

Kudláčová J, Kotrchová L, Kostka L, Randárová E, Filipová M, Janoušková O, Fang J, Etrych T. Structure-to-Efficacy Relationship of HPMA-Based Nanomedicines: The Tumor Spheroid Penetration Study. Pharmaceutics. 2020; 12(12):1242. https://doi.org/10.3390/pharmaceutics12121242

Chicago/Turabian Style

Kudláčová, Júlia; Kotrchová, Lenka; Kostka, Libor; Randárová, Eva; Filipová, Marcela; Janoušková, Olga; Fang, Jun; Etrych, Tomáš. 2020. "Structure-to-Efficacy Relationship of HPMA-Based Nanomedicines: The Tumor Spheroid Penetration Study" Pharmaceutics 12, no. 12: 1242. https://doi.org/10.3390/pharmaceutics12121242

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