Nanaki Stavroula, Tseklima Maria, Terzopoulou Zoe, Nerantzaki Maria, Giliopoulos Dimitrios J, Triantafyllidis Konstantinos, Kostoglou Margaritis, Bikiaris Dimitrios N
Laboratory of Polymer Chemistry and Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
Laboratory of General and Inorganic Chemical Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
Eur J Pharm Biopharm. 2017 Aug;117:77-90. doi: 10.1016/j.ejpb.2017.03.016. Epub 2017 Apr 4.
In this study, high surface area mesoporous silica foam with cellular pore morphology (MCF) was used for injectable delivery of paliperidone, an antipsychotic drug used in patients suffering from bipolar disorder. The aim was to enhance paliperidone solubility and simultaneously to prepare long active intractable microspheres. For this reason paliperidone was first loaded in MCF silica, and the whole system was further encapsulated into PLA and PLGA 75/25w/w copolymer in the form of microspheres. It was found that paliperidone, after its adsorption into MCF, was transformed in its amorphous state, thus leading to enhanced in vitro dissolution profile. Furthermore, incorporation of the drug-loaded MCF to polymeric microparticles (PLA and PLGA) prolonged the release time of paliperidone from 10 to 15days.
在本研究中，具有蜂窝状孔形态的高比表面积介孔二氧化硅泡沫（MCF）被用于注射递送帕利哌酮，这是一种用于双相情感障碍患者的抗精神病药物。目的是提高帕利哌酮的溶解度，同时制备长效活性难溶性微球。因此，首先将帕利哌酮负载于MCF二氧化硅中，然后将整个体系进一步以微球形式包封于聚乳酸（PLA）和聚乳酸-羟基乙酸共聚物（PLGA 75/25 w/w）中。结果发现，帕利哌酮吸附到MCF中后转变为无定形状态，从而导致体外溶出曲线得到改善。此外，将载药的MCF掺入聚合物微粒（PLA和PLGA）中，使帕利哌酮的释放时间从10天延长至15天。
