Background and Purpose: Aiming to achieve light sedation via intranasal administration, this study showed that propofol (PPF) did not permeate across the rabbit nasal mucosa ex vivo from its marketed emulsion for injection. Experimental approach: Dilution of the emulsion with methyl-beta-cyclodextr in in saline solution increased propofol solubility in water and diffusion across the nasal epithelium. Key results and conclusion: Despite these positive effects of the cyclodextrin, the amount of PPF permeated was minimal in 3 h, exceeding the formulation residence time in the nose. These results highlight the key role of formulation and the need for innovation in solubility and transmucosal transport enhancement techniques to optimize drug delivery and therapeutic efficacy.

Ex vivo propofol permeation across nasal mucosa: A proof-of-concept study for outpatient light sedation via nasal route

Spampinato, Michele Domenico
Primo
Data Curation
;
Costanzini, Anna
Secondo
Formal Analysis
;
De Giorgio, Roberto
Funding Acquisition
;
Passaro, Angelina
Resources
;
Realdon, Nicola
Writing – Review & Editing
;
Bortolotti, Fabrizio
Methodology
;
Banella, Sabrina
Penultimo
Investigation
;
Colombo, Gaia
Ultimo
Writing – Original Draft Preparation
2024

Abstract

Background and Purpose: Aiming to achieve light sedation via intranasal administration, this study showed that propofol (PPF) did not permeate across the rabbit nasal mucosa ex vivo from its marketed emulsion for injection. Experimental approach: Dilution of the emulsion with methyl-beta-cyclodextr in in saline solution increased propofol solubility in water and diffusion across the nasal epithelium. Key results and conclusion: Despite these positive effects of the cyclodextrin, the amount of PPF permeated was minimal in 3 h, exceeding the formulation residence time in the nose. These results highlight the key role of formulation and the need for innovation in solubility and transmucosal transport enhancement techniques to optimize drug delivery and therapeutic efficacy.
2024
Spampinato, Michele Domenico; Costanzini, Anna; De Giorgio, Roberto; Passaro, Angelina; Realdon, Nicola; Bortolotti, Fabrizio; Banella, Sabrina; Colom...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/2570933
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