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Open AccessArticle

Hyaluronan Graft Copolymers Bearing Fatty-Acid Residues as Self-Assembling Nanoparticles for Olanzapine Delivery

1
Dipartimento di Biotecnologie, Chimica e Farmacia (Dipartimento di Eccellenza 2018-2022), Università degli Studi di Siena, Via A. Moro 2, 53100 Siena, Italy
2
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
3
Dipartimento Promozione della Salute, Materno-Infantile, di Medicina Interna e Specialistica di Eccellenza “G. D’Alessandro” (PROMISE), Università degli Studi di Palermo, 90100 Palermo, Italy
4
Leibniz Institute of Polymer Research, Hohe Strasse 6, 01069 Dresden, Germany
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(12), 675; https://doi.org/10.3390/pharmaceutics11120675
Received: 13 November 2019 / Revised: 6 December 2019 / Accepted: 9 December 2019 / Published: 12 December 2019
In order to evaluate the potential of a technology platform based on hyaluronan copolymers grafted with propargylated ferulate fluorophores (HA-FA-Pg) in the development of drug delivery systems, the propargyl groups of HA-FA-Pg derivatives were employed with oleic acid (OA) or stearic acid (SA) residues across a biocompatible hexa(ethylene glycol) (HEG) spacer. The designed materials (i.e., HA-FA-HEG-OA or HA-FA-HEG-SA) showed clear-cut aggregation features in an aqueous environment, as confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM), generating nanoaggregate systems. In fact, HA-FA-HEG-OA and HA-FA-HEG-SA derivatives showed the property to create self-assembled cytocompatible nanostructured aggregates in water, thanks to the simultaneous presence of hydrophilic portions in the polymeric backbone, such as hyaluronic acid, and hydrophobic portions in the side chains. Furthermore, the designed materials interact with living cells showing a high degree of cytocompatibility. The potential ability of nanosystems to load pharmacologically active molecules was assessed by the physical entrapment of olanzapine into both polymeric systems. The drug loading evaluation demonstrated that the nanoparticles are able to incorporate a good quantity of olanzapine, as well as improve drug solubility, release profile, and cytocompatibility. View Full-Text
Keywords: hyaluronic acid; ferulic acid; oleic acid; stearic acid; olanzapine; self-assembling nanocarriers; drug delivery systems hyaluronic acid; ferulic acid; oleic acid; stearic acid; olanzapine; self-assembling nanocarriers; drug delivery systems
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MDPI and ACS Style

Paolino, M.; Licciardi, M.; Savoca, C.; Giammona, G.; Modica De Mohac, L.; Reale, A.; Giuliani, G.; Komber, H.; Donati, A.; Leone, G.; Magnani, A.; Anzini, M.; Cappelli, A. Hyaluronan Graft Copolymers Bearing Fatty-Acid Residues as Self-Assembling Nanoparticles for Olanzapine Delivery. Pharmaceutics 2019, 11, 675.

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