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Intranasal delivery of granisetron to the brain via nanostructured cubosomes-based in situ gel for improved management of chemotherapy-induced emesis

Eissa, Essam M., Elkomy, Mohammed H., Eid, Hussein M., Ali, Adel A., Abourehab, Mohammed A. S., Alsubaiyel, Amal M., Naguib, Ibrahim A., Alsalahat, Izzeddin and Hassan, Amira H. 2022. Intranasal delivery of granisetron to the brain via nanostructured cubosomes-based in situ gel for improved management of chemotherapy-induced emesis. Pharmaceutics 14 (7) , 1374. 10.3390/pharmaceutics14071374

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Abstract

This research aimed to boost granisetron (GS) delivery to the brain via the intranasal route to better manage chemotherapy-induced emesis. Glycerol monooleate (GMO), Poloxamer 407 (P 407) and Tween 80 (T 80) were used to formulate GS-loaded cubosomes (GS-CBS) utilizing a melt dispersion-emulsification technique. GS-CBS were characterized by testing particle diameter, surface charge and entrapment efficiency. The formulations were optimized using a Box–Behnken statistical design, and the optimum formula (including GMO with a concentration of 4.9%, P 407 with a concentration of 10%, and T 80 with a concentration of 1%) was investigated for morphology, release behavior, ex vivo permeation through the nasal mucosa, and physical stability. Moreover, the optimal formula was incorporated into a thermosensitive gel and subjected to histopathological and in vivo biodistribution experiments. It demonstrated sustained release characteristics, increased ex vivo permeability and improved physical stability. Moreover, the cubosomal in situ gel was safe and biocompatible when applied to the nasal mucosa. Furthermore, compared to a drug solution, the nose-to-brain pathway enhanced bioavailability and brain distribution. Finally, the cubosomal in situ gel may be a potential nanocarrier for GS delivery to the brain through nose-to-brain pathway.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Schools > Medicine
Publisher: MDPI
ISSN: 1999-4923
Date of First Compliant Deposit: 2 September 2025
Date of Acceptance: 24 June 2022
Last Modified: 02 Sep 2025 11:55
URI: https://orca.cardiff.ac.uk/id/eprint/180816

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