Comprehensive evaluation of xylometazoline hydrochloride formulations: Ex-vivo and in-vitro studies

[Display omitted] Xylometazoline is a well-established nasal decongestant that has been used alone and in combination with dexpanthenol as an over the counter (OTC) medicine. Considering the possibility of further improvement of xylometazoline nasal formulations, hyaluronic acid (HA) was evaluated a...

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Published in:European journal of pharmaceutics and biopharmaceutics 2024-10, Vol.203, p.114466, Article 114466
Main Authors: Tuncay Tanriverdi, Sakine, Gokce, Evren Homan, Sušanj, Ivan, Simić, Laura, Vukelić, Karina, Knežević, Zdravka, Ilhan, Pelin, Sendemir, Aylin, Ozer, Ozgen
Format: Article
Language:English
Subjects:
Administration, Intranasal
Animals
Chemistry, Pharmaceutical - methods
Drug Compounding - methods
Humans
Hyaluronic acid
Hyaluronic Acid - chemistry
Imidazoles - administration & dosage
Imidazoles - chemistry
Imidazoles - pharmacokinetics
Imidazoles - pharmacology
Nasal
Nasal Decongestants - administration & dosage
Nasal Mucosa - drug effects
Nasal Mucosa - metabolism
Permeability
Scratch test
Sheep
TEER
Xylometazoline
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Summary:[Display omitted] Xylometazoline is a well-established nasal decongestant that has been used alone and in combination with dexpanthenol as an over the counter (OTC) medicine. Considering the possibility of further improvement of xylometazoline nasal formulations, hyaluronic acid (HA) was evaluated as an additional ingredient. The aim of this study was to investigate the permeation, mucosal retention, and mucoadhesion properties of a new xylometazoline-HA [Xylo-HA] formulation ex vivo and to explore the potential benefits of incorporating HA in the formulation in vitro. Sheep nasal mucosa was used in the ex vivo study, where Xylo-HA was compared with xylometazoline alone [Xylo-Mono], and in combination with dexpanthenol [Xylo-Dex] to understand the impact of formulation changes. The permeation of xylometazoline was generally low (Xylo-Mono 11.14 ± 4.75 %, Xylo-HA 14.57 ± 5.72 % and Xylo-Dex 11.00 ± 3.05 % of the applied dose). The steady state fluxes of xylometazoline were determined as 12.64 ± 3.52 μg/cm2h, 14.94 ± 3.38 μg/cm2h and 12.19 ± 2.05 μg/cm2h for Xylo-Mono, Xylo-HA and Xylo-Dex, respectively. No significant differences were observed between the formulations in the permeation nor mucosal retention studies (p > 0.05 for all), while Xylo-HA exhibited superior mucoadhesive proprieties (p 
ISSN:0939-6411
1873-3441
1873-3441
DOI:10.1016/j.ejpb.2024.114466