Ergul Yilmaz Zeynep, Cordonnier Thomas, Debuigne Antoine, Calvignac Brice, Jerome Christine, Boury Frank
Center for Education and Research on Macromolecules (CERM), University of Liège (ULg),Cesam-RU, Allée du 6 AoÛt, 13, Quartier Agora, Sart Tilman, Building B6a-third floor, B-4000 Liège, Belgium; INSERM U1066, Micro et Nanomedécines Biomimétiques, IBS, University of Angers, 4 rue Larrey, Cedex 9, Angers, 49933, France.
INSERM U1066, Micro et Nanomedécines Biomimétiques, IBS, University of Angers, 4 rue Larrey, Cedex 9, Angers, 49933, France.
Int J Pharm. 2016 Nov 20;513(1-2):130-137. doi: 10.1016/j.ijpharm.2016.09.007. Epub 2016 Sep 4.
Calcium carbonate particles are promising candidates as proteins carriers for their controlled delivery in the body. The present paper aims at investigating the protein encapsulation by in situ precipitation of calcium carbonate particles prepared by a process based on supercritical CO and using a new type of degradable well-defined double hydrophilic block copolymers composed of poly(ethylene oxide) and polyphosphoester blocks acting as templating agent for the calcium carbonate. For this study, lysozyme was chosen as a model for therapeutic protein for its availability and ease of detection. It was found that by this green process, loading into the CaCO microparticles with a diameter about 2μm can be obtained as determined by scanning electron microscopy. A protein loading up to 6.5% active lysozyme was measured by a specific bioassay (Micrococcus lysodeikticus). By encapsulating fluorescent-labelled lysozyme (lysozyme-FITC), the confocal microscopy images confirmed its encapsulation and suggested a core-shell distribution of lysozyme into CaCO, leading to a release profile reaching a steady state at 59% of release after 90min.
碳酸钙颗粒因其在体内的可控递送而有望成为蛋白质载体。本文旨在研究通过基于超临界CO₂的工艺制备碳酸钙颗粒,并使用由聚环氧乙烷和聚磷酸酯嵌段组成的新型可降解明确双亲性嵌段共聚物作为碳酸钙的模板剂,通过原位沉淀法进行蛋白质包封。在本研究中,选择溶菌酶作为治疗性蛋白质的模型,因为其易于获得且易于检测。通过扫描电子显微镜测定发现,通过这种绿色工艺,可以将蛋白质负载到直径约为2μm的CaCO₃微粒中。通过特定的生物测定法(溶壁微球菌)测得活性溶菌酶的蛋白质负载量高达6.5%。通过包封荧光标记的溶菌酶(溶菌酶-FITC),共聚焦显微镜图像证实了其包封,并表明溶菌酶在CaCO₃中呈核壳分布,导致在90分钟后释放曲线达到59%释放的稳定状态。