Posted by Nasal drug delivery is increasingly recognized as an alternative to oral and parenteral administration, offering advantages such as rapid absorption and avoidance of first-pass metabolism. However, effective nasal formulations require excipients that can enhance mucosal permeability and prolong drug residence time.
This study explored the development of meloxicam potassium monohydrate (MXP)-containing nasal powders using a nano spray dryer, incorporating various β-cyclodextrins (neutral BCD, anionic SBECD and cationic QABCD) and polyvinyl alcohol (PVA) as excipients. The particle size and morphology, physicochemical properties, mucoadhesivity, in vitro drug release, and in vitro permeability through an artificial membrane and RPMI 2650 cell model were investigated.
The resulting particles, with sizes ranging from 1.89 to 2.21 µm exhibited an amorphous state of MXP, which combined with the high water solubility of the excipients facilitated rapid and complete drug release. Examining the adhesivity of the samples by a texture analyser, ionic cyclodextrins demonstrated higher adhesive force values regardless of charge type compared to the neutral variant, although PVA did not have significant enhancing effect. In vitro permeability studies revealed that the presence of PVA improved MXP diffusion across the artificial membrane, therefore PVA-containing samples were further investigated involving RPMI 2650 cells. After determining the non-cytotoxic concentrations of the samples (MTS assay and LDH release), diffusion studies revealed the permeation enhancing effect of only the anionic β-cyclodextrin (SBECD) under the applied test conditions.
Despite these promising results, further investigation into the aerodynamic properties and the specific conditions under which SBECD enhances permeation is necessary.
Patrícia Varga, Anett Németh, Scarlett Zeiringer, Eva Roblegg, Mária Budai-Szűcs, Csilla Balla-Bartos, Rita Ambrus (2024) Formulation and investigation of differently charged β-cyclodextrin-based meloxicam potassium containing nasal powders,. European Journal of Pharmaceutical Sciences 202, 106879,
https://doi.org/10.1016/j.ejps.2024.106879