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Synthesis and pharmacokinetic study of poly(ethylene oxide) triazole dendrimers decorated with aminosteroids as anticancer agent
Author(s) -
Darveau Patrick,
Maltais René,
Roy Jenny,
Poirier Donald,
Morin JeanFrançois
Publication year - 2020
Publication title -
journal of polymer science
Language(s) - English
Resource type - Journals
eISSN - 2642-4169
pISSN - 2642-4150
DOI - 10.1002/pol.20190042
Subject(s) - dendrimer , nanocarriers , ethylene oxide , chemistry , solubility , pharmacokinetics , combinatorial chemistry , materials science , polymer chemistry , organic chemistry , drug delivery , polymer , pharmacology , copolymer , medicine
The use of new aminosteroids has shown increased therapeutic efficiency on multiple cancer cell lines. Those molecules are, however, highly hydrophobic, leading to bad pharmacokinetic properties. Dendrimers are excellent candidates to improve PK, especially for absorption and distribution, since their structure can be designed to be water‐soluble. We have the capacity to tailor the particle's size to allow high‐loading capacity. In this article, we managed to enhance aqueous solubility of the aminosteroid AH‐38 by grafting on three generations of poly(ethylene oxide) triazole dendrimers to reach high drug loading values (w/w %). In vitro and in vivo studies were conducted and showed interesting results, such as increased plasma concentration of the free aminosteroid with G1 and G2 nanocarriers over the AH‐38 administrated as a free drug. © 2020 Wiley Periodicals, Inc. J. Polym. Sci. 2020 , 58 , 654–661