Tran Le Tuyet Chau, Gueutin Claire, Frebourg Ghislaine, Burucoa Christophe, Faivre Vincent
Institut Galien Paris-Sud, CNRS, Université Paris-Saclay, Univ. Paris-Sud, 5, rue Jean-Baptiste Clément, Châtenay-Malabry 92296, France.
Institut de Biologie Paris-Seine (IBPS), Université Pierre et Marie CURIE, SME-9 Quai St Bernard, 75252 Paris Cedex 05, France.
Biochem Biophys Res Commun. 2017 Nov 4;493(1):146-151. doi: 10.1016/j.bbrc.2017.09.060. Epub 2017 Sep 14.
Poorly water-soluble and unstable compounds are difficult to develop as drug products using conventional formulation techniques. The aim of the present study was to develop and evaluate a nanoformulation prepared by a hot high-pressure homogenization method, which was a scalable and solvent-free process. We successfully prepared stable nanodispersions to protect a labile antibiotic, erythromycin. The mean diameter of the dispersed droplets was approximately 150 nm, and size distribution was unimodal. Dispersion was physically stable at room temperature for over six months. Using erythromycin as a model compound, we studied its antimicrobial activity in vitro on Helicobacter pylori. Results showed that drug encapsulation improves API stability in an acidic environment and is conducive to a synergistic effect between the drug and the formulation.
水溶性差且不稳定的化合物难以使用传统制剂技术开发成药品。本研究的目的是开发并评估一种通过热高压均质法制备的纳米制剂,该方法是一种可扩展且无溶剂的工艺。我们成功制备了稳定的纳米分散体以保护一种不稳定的抗生素——红霉素。分散液滴的平均直径约为150纳米,且粒径分布呈单峰。该分散体在室温下物理稳定超过六个月。以红霉素作为模型化合物,我们研究了其对幽门螺杆菌的体外抗菌活性。结果表明,药物包封提高了活性药物成分在酸性环境中的稳定性,并有利于药物与制剂之间的协同作用。