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

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. Dilution of the emulsion with methyl-β-cyclodextrin in saline solution increased propofol solubility...

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Veröffentlicht in:ADMET & DMPK 2024-01, Vol.12 (5), p.759-768
Hauptverfasser: Spampinato, Michele D, Costanzini, Anna, De Giorgio, Roberto, Passaro, Angelina, Realdon, Nicola, Bortolotti, Fabrizio, Banella, Sabrina, Colombo, Gaia
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Sprache:eng
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Zusammenfassung: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. Dilution of the emulsion with methyl-β-cyclodextrin in saline solution increased propofol solubility in water and diffusion across the nasal epithelium. 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.
ISSN:1848-7718
1848-7718
DOI:10.5599/admet.2403