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Immobilization of Levocetirizine on Mesoporous Silica for Antiallergenic Gel Formulation

Authors :
Klára Szentmihályi
Szilvia Klébert
Krisztina Móricz
Antal Balázs Szenes-Nagy
Zoltán May
Eszter Bódis
Miklós Mohai
László Trif
Mirella Mirankó
Tivadar Feczkó
Zoltán Károly
Source :
Applied Sciences, Vol 14, Iss 20, p 9605 (2024)
Publication Year :
2024
Publisher :
MDPI AG, 2024.

Abstract

Levocetirizine dihydrochloride is an effective antiallergenic drug applied mostly orally; however, developing a topical formulation for localized treatment could be beneficial. To achieve this, a modified formulation technique is necessary to enhance bioavailability efficiency and minimize possible side effects. Therefore, levocetirizine particles were prepared by immobilization on mesoporous silica material. Both the dihydrochloride form and its free base of levocetirizine were fixed on a silica-type Syloid support. Immobilization of the active ingredient levocetirizine in a free base form on a Syloid support by mixing in a dichloromethane solution provides better surface coverage (65.5%) than immobilization in the dihydrochloride form in water or methanol (24.5% for both). The successful binding of levocetirizine was confirmed by X-ray photoelectron spectroscopy and infrared measurements. The active ingredient in the form of hydrochloride is more likely to be in the pores, while the free base is bound to the surface in larger quantities. The time-dependent levocetirizine release showed that the liberation of the active ingredient from the Syloid is slower than the dissolution of the starting active ingredient itself, so it may be suitable for exerting a more reliable and prolonged local effect. A gel containing a Syloid-fixed levocetirizine free base was tested in vivo in a croton oil-induced ear edema mouse model. When compared to a reference gel, the half-dose formulation containing levocetirizine free base demonstrated a similar efficacy to Fenistil gel, indicating that the new formulation may offer superior effectiveness at lower doses.

Details

Language :
English
ISSN :
20763417
Volume :
14
Issue :
20
Database :
Directory of Open Access Journals
Journal :
Applied Sciences
Publication Type :
Academic Journal
Accession number :
edsdoj.8b4a9558459434c8cc8439afa2a2674
Document Type :
article
Full Text :
https://doi.org/10.3390/app14209605