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Poly(2-oxazoline)-Based Amphiphilic Gradient Copolymers as Nanocarriers for Losartan: Insights into Drug–Polymer Interactions

1
Theoretical and Physical Chemistry Institute, National Hellenic Research Foundation, 48 Vassileos Constantinou Avenue, 11635 Athens, Greece
2
Organic Chemistry Laboratory, Department of Chemistry, National and Kapodistrian University of Athens, Panepistimioupolis, 15771 Zografou, Greece
*
Author to whom correspondence should be addressed.
Academic Editor: Ana María Díez-Pascual
Received: 15 June 2021 / Revised: 26 June 2021 / Accepted: 28 June 2021 / Published: 1 July 2021
(This article belongs to the Special Issue Polymers in Nanocarrier Systems)
The current study is focused on the development of highly stable drug nanocarriers by encapsulating losartan potassium (LSR) into an amphiphilic biocompatible poly(2-methyl-2-oxazoline)-grad-poly(2-phenyl-2-oxazoline) (PMeOxz72-grad-PPhOxz28) gradient copolymer (GC). Based on dynamic light scattering (DLS), the PMeOxz72-grad-PPhOxz28 (where the subscripts denote %wt composition of the components) GC formed micelles and aggregates of 13 nm and 96 nm in aqueous milieu. The presence of hydrophobic LSR molecules altered the structural characteristics of the GC, modulating the organization of the polymeric components and revealing the formation of hyper micellar nanostructures in addition to micelles. The 2D-NOESY experiments evidenced intermolecular interactions between the phenyl ring of LSR with the phenyl group of PPhOxz and eminent correlations between the butyl chain of LSR with the phenyl group of PPhOxz and methylene group of PMeOxz, respectively. Additionally, NMR studies as a function of temperature demonstrated that the presence of hydrophilic PMeOxz segments in the gradient core of PMeOxz72-grad-PPhOxz28 nanoassemblies induced an increased fluidity of the core matrix, especially upon heating, thus causing water penetration, resulting in increased proton mobility. Lastly, the ultrasound release profile of LSR signified that a great amount of the encapsulated LSR is tightly bound to the PMeOxz72-grad-PPhOxz28 nanoassemblies. View Full-Text
Keywords: amphiphilic gradient copolymers; polymeric nanocarriers; drug delivery systems; thin film hydration method; drug encapsulation; drug release profile; drug–polymer intermolecular interactions amphiphilic gradient copolymers; polymeric nanocarriers; drug delivery systems; thin film hydration method; drug encapsulation; drug release profile; drug–polymer intermolecular interactions
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MDPI and ACS Style

Chroni, A.; Mavromoustakos, T.; Pispas, S. Poly(2-oxazoline)-Based Amphiphilic Gradient Copolymers as Nanocarriers for Losartan: Insights into Drug–Polymer Interactions. Macromol 2021, 1, 177-200. https://0-doi-org.brum.beds.ac.uk/10.3390/macromol1030014

AMA Style

Chroni A, Mavromoustakos T, Pispas S. Poly(2-oxazoline)-Based Amphiphilic Gradient Copolymers as Nanocarriers for Losartan: Insights into Drug–Polymer Interactions. Macromol. 2021; 1(3):177-200. https://0-doi-org.brum.beds.ac.uk/10.3390/macromol1030014

Chicago/Turabian Style

Chroni, Angeliki, Thomas Mavromoustakos, and Stergios Pispas. 2021. "Poly(2-oxazoline)-Based Amphiphilic Gradient Copolymers as Nanocarriers for Losartan: Insights into Drug–Polymer Interactions" Macromol 1, no. 3: 177-200. https://0-doi-org.brum.beds.ac.uk/10.3390/macromol1030014

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