Macromolecular Architecture and Encapsulation of the Anticancer Drug Everolimus Control the Self-Assembly of Amphiphilic Polypeptide-Containing Hybrids

Anastasis Karatzas, Johannes S. Haataja, Dimitrios Skoulas, Panayiotis Bilalis, Spyridon Varlas, Panagiota Apostolidi, Sosanna Sofianopoulou, Efstratios Stratikos, Nikolay Houbenov, Olli Ikkala, Hermis Iatrou*

*Corresponding author for this work

Research output: Contribution to journalArticleScientificpeer-review

Abstract

Macromolecular architecture plays an important role in the self-assembly process of block copolymer amphiphiles. Herein, two series of stimuli-responsive amphiphilic 3-miktoarm star hybrid terpolypeptides and their corresponding linear analogues were synthesized exhibiting the same overall composition and molecular weight but different macromolecular architecture. The macromolecular architecture was found to be a key parameter in defining the morphology of the nanostructures formed in aqueous solutions as well as to alter the self-assembly behavior of the polymers independently of their composition. In addition, it was found that the assemblies prepared from the star-shaped polymers showed superior tolerance against enzymatic degradation due to the increased corona block density on the outer surface of the nanoparticles. Encapsulation of the hydrophobic anticancer drug Everolimus resulted in the formation of intriguing non-spherical and non-symmetric pH-responsive nanostructures, such as "stomatocytes" and "multi-compartmentalized suprapolymersomes", while the pH-triggered release of the drug was also investigated. Owing to the similarities of the developed "stomatocytes" with red blood cells, in combination with their pH-responsiveness and superior stability over enzymatic degradation, they are expected to present advanced drug delivery properties and have the ability to bypass several extra- and intracellular barriers to reach and effectively treat cancer cells.

Original languageEnglish
Pages (from-to)4546-4562
JournalBiomacromolecules
Volume20
Early online date1 Jan 2019
DOIs
Publication statusPublished - 7 Nov 2019
MoE publication typeA1 Journal article-refereed

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