Posted by A recent review [1] used risperidone as a pharmacological model to examine the impact of solubility enhancement at the primary administration site for drugs under BCS Class II often having a low bioavailability. For tackling drug-related pertains like disease diagnostics, therapy, and prophylactic measures at the cellular or molecular levels, implementing nanocarriers in therapeutics has significant potential. The comprehensive pharmaceutical compositions of risperidone nano-microparticles that have been developed to alleviate psychosis are highlighted in the study which does not mention the CD-related formulations although these are in the focus of the research.
The aqueous solubility of risperidone was enhanced by 4.75-fold and 2-fold using HP-β-CD and HP-γ-CD, respectively. [2] RIS-HP-β-CD complex (CX) and physical mixture (PM) directly compressed tablets were prepared and combined with hydrogel-forming microneedle array patches (HFMAPs). HFMAPs) are microneedles that create microconduits upon insertion and swelling in the skin, potentially allowing prolonged drug delivery without generating sharps waste. Among the tested formulations, RIS-HP-β-CD PM reservoirs with 11 x 11 PVA/PVP HFMAPs exhibited the best performance in ex vivo studies and were further evaluated in in vivo experiments using female Sprague Dawley rats. The extended wear time of the MAPs resulted in the sustained release of RIS and its active metabolite 9-hydroxyrisperidone (9-OH-RIS) in plasma samples, lasting from 3 to 5 days with a 1-day application and up to 10 days with a 5-day application. For a 1-day application, HFMAPs showed greater systemic exposure to RIS compared to intramuscular control (AUC0-t: 13330.05 ± 2759.95 ng/mL/hour versus 2706 ± 1472 ng/mL/hour). Moreover, RIS exposure was extended to 5 days (AUC0-t: 12292.37 ± 1801.94 ng/mL/hour).
HPBCD complexes prepared with 4/1 and 2/1 M ratio (HPβCD/risperidone) were used for electrospinning [3]. 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.
References:
[1] Rathi R, Mehetre NM, Goyal S, Singh I, Huanbutta K, Sangnim T. (2024) Advanced Drug Delivery Technologies for Enhancing Bioavailability and Efficacy of Risperidone. Int J Nanomedicine. 19:, 2871-12887. https://doi.org/10.2147/IJN.S492684
[2] Rand Ghanma, Qonita Kurnia Anjani, Yara A. Naser, Akmal Hidayat Bin Sabri, Aaron R.J. Hutton, Lalitkumar K. Vora, Achmad Himawan, Brett Greer, Helen O. McCarthy, Ryan F. Donnelly (2024) Risperidone-cyclodextrin complex reservoir combined with hydrogel-forming microneedle array patches for enhanced transdermal delivery. European Journal of Pharmaceutics and Biopharmaceutics 202, 114415.
https://doi.org/10.1016/j.ejpb.2024.114415
[3] Tony Tan, Asli Celebioglu, Mahmoud Aboelkheir, Tamer Uyar (2024) Risperidone/cyclodextrin inclusion complex electrospun nanofibers for fast-disintegrating antipsychotic drug delivery. Journal of Drug Delivery Science and Technology 97, 105753. https://doi.org/10.1016/j.jddst.2024.105753