Viola Marco, Migliorini Claudia, Ziarelli Fabio, Viel Stéphane, Cencetti Claudia, Di Risola Daniel, Mosca Luciana, Masuelli Laura, Matricardi Pietro, Di Meo Chiara
Department of Drug Chemistry and Technologies, Sapienza University of Rome, 00185 Rome, Italy.
Aix-Marseille Université, CNRS, Centrale Méditerranée, Fédération Sciences Chimiques Marseille, 13013 Marseille, France.
J Funct Biomater. 2023 Sep 20;14(9):482. doi: 10.3390/jfb14090482.
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.
先前合成的接枝有胆固醇部分的新型两亲性聚丙烯酸酯PAAbCH，已在实验室和工业化前规模上进行了深入表征和研究。固态核磁共振分析证实了聚合物结构，并开发了几种水性医药和化妆品产品。特别是，制备了含有植物油、角鲨烯和神经酰胺的稳定油/水乳液，以及负载双氯芬酸的亲水性药用薄膜，实现了药物的长效释放。PAAbCH在宏观和纳米尺度上还与壳聚糖形成了聚电解质水凝胶复合物。结果表明，这种聚合物作为一种创新辅料具有广阔的潜力，可作为增溶剂、增稠剂和乳化剂，且易于放大生产。
