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

J Funct Biomater. 2023 Sep 20;14(9):482. doi: 10.3390/jfb14090482.

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.

Keywords: amphiphilic; cholesterol; emulsifier; polyacrylate; solid-state NMR; topical formulations.