Use of mesoporous cellular foam (MCF) in preparation of polymeric microspheres for long acting injectable release formulations of paliperidone antipsychotic drug

作者：Nanaki Stavroula; Tseklima Maria; Terzopoulou Zoe; Nerantzaki Maria; Giliopoulos Dimitrios J; Triantafyllidis Konstantinos; Kostoglou Margaritis; Bikiaris Dimitrios N^*

来源：European Journal of Pharmaceutics and Biopharmaceutics, 2017, 117: 77-90.

DOI：10.1016/j.ejpb.2017.03.016

• PLA
• PLGA
• Mesoporous cellular foam (MCF)
• Microspheres
• Paliparidone
• Long acting injectable
• Antipsychotic drug

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 75/25 w/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 15,days.

• 出版日期2017-8