Risperidone/cyclodextrin inclusion complex electrospun nanofibers for fast-disintegrating antipsychotic drug delivery

Abstract

In this paper, the inclusion complexes (ICs) of hydroxypropyl-beta-cyclodextrin (HPβCD) and risperidone were electrospun into nanofibrous film for potential fast-disintegrating drug delivery system. Risperidone is used to treat bipolar disorder, schizophrenia, and mood swings from autism. However, it is practically insoluble in aqueous medium. On the other hand, the encapsulation of risperidone into HPβCD cavity by inclusion complexation can enhance water solubility of this drug molecule. Here, the IC systems were prepared with 4/1 and 2/1 M ratio (HPβCD/risperidone). The highly concentrated HPβCD aqueous solutions (200 %, w/v) were used for the fiber formation. Finally, the system having 4/1 M ratio resulted in a clear and homogeneous solution showing that the HPβCD and risperidone completely formed IC. However, HPβCD/risperidone-IC having 2/1 M ratio was turbid and contained some small clumps of un-complexed risperidone. Even so, free-standing and thin nanofibrous films were obtained for both systems with an average fiber diameter of ∼315 nm and ∼280 nm for 2/1 and 4/1 systems, respectively. Both HPβCD/risperidone-IC nanofibers were produced with approximately 100 % preservation of risperidone within the nanofiber matrix without the loss of risperidone during electrospinning process, that is, HPβCD/risperidone-IC nanofibers retained the initial M ratio of 2/1 and 4/1 as in electrospinning solution. Both HPβCD/risperidone-IC nanofibrous films showed fast-disintegration and fast-release characteristics in artificial saliva and aqueous medium verifying their potential as a fast-disintegrating oral drug delivery system for risperidone.