Polyacrylate–Cholesterol Amphiphilic Derivative: Formulation Development and Scale-up for Health Care Applications

Author:

Viola Marco1,Migliorini Claudia1,Ziarelli Fabio2ORCID,Viel Stéphane34,Cencetti Claudia5,Di Risola Daniel6ORCID,Mosca Luciana6ORCID,Masuelli Laura7,Matricardi Pietro1ORCID,Di Meo Chiara1ORCID

Affiliation:

1. Department of Drug Chemistry and Technologies, Sapienza University of Rome, 00185 Rome, Italy

2. Aix-Marseille Université, CNRS, Centrale Méditerranée, Fédération Sciences Chimiques Marseille, 13013 Marseille, France

3. Aix-Marseille Université, CNRS, Institut de Chimie Radicalaire, 13013 Marseille, France

4. Institut Universitaire de France, 75005 Paris, France

5. QI SRL, Pomezia, 00071 Rome, Italy

6. Department of Biochemical Sciences “A. Rossi Fanelli”, Sapienza University of Rome, 00185 Rome, Italy

7. Department of Experimental Medicine, Sapienza University of Rome, 00161 Rome, Italy

Abstract

The novel amphiphilic polyacrylate grafted with cholesterol moieties, PAAbCH, previously synthesized, was deeply characterized and investigated in the lab and on a pre-industrial scale. Solid-state NMR analysis confirmed the polymer structure, and several water-based pharmaceutical and cosmetic products were developed. In particular, stable oil/water emulsions with vegetable oils, squalene, and ceramides were prepared, as well as hydrophilic medicated films loaded with diclofenac, providing a prolonged drug release. PAAbCH also formed polyelectrolyte hydrogel complexes with chitosan, both at the macro- and nano-scale. The results demonstrate that this polymer has promising potential as an innovative excipient, acting as a solubility enhancer, viscosity enhancer, and emulsifying agent with an easy scale-up transfer process.

Funder

Sapienza University of Rome

Publisher

MDPI AG

Subject

Biomedical Engineering,Biomaterials

Reference63 articles.

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