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

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.

Highlights

• Electrospinning was used for the generation of risperidone/cyclodextrin nanofibers.
• Inclusion complexes were formed using hydroxypropyl-β-cyclodextrin (HPβCD).
• Risperidone/HPβCD nanofibers were generated using water only as solvent system.
• Risperidone/HPβCD nanofibers were obtained with ∼100 % of drug preservation.
• Risperidone/HPβCD nanofibers indicated fast release/disintegration profile.

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.

Read more here

Materials

Hydroxypropyl-beta-cyclodextrin (HPβCD, Cavasol W7, DS: ∼0.9) was donated by Wacker Chemie AG (USA). Risperidone (99 %, Fisher Scientific), methanol (≥99.8% (GC), Sigma-Aldrich), phosphate buffered saline tablet (Sigma Aldrich), o-phosphoric acid (85%, HPLC, Fisher Chemical), sodium chloride (NaCl, >99%, Sigma Aldrich), sodium phosphate dibasic heptahydrate (Na2HPO4, 98.0–102.0%, Fisher Chemical), potassium phosphate monobasic (KH2PO4 ≥99.0%, Fisher Chemical),

Tony Tan, Asli Celebioglu, Mahmoud Aboelkheir, Tamer Uyar, Risperidone/cyclodextrin inclusion complex electrospun nanofibers for fast-disintegrating antipsychotic drug delivery, Journal of Drug Delivery Science and Technology, Volume 97, 2024, 105753, ISSN 1773-2247, https://doi.org/10.1016/j.jddst.2024.105753.

Read also our introduction article on Orally Disintegrating Tablets (ODTs) here: