Soluplus® promotes efficient transport of meloxicam to the central nervous system via nasal administration

In our present series of experiments, we investigated the nasal applicability of the previously developed Soluplus® – Meloxicam polymeric micelle formulation. Utilizing the nasal drug investigations, moderately high mucoadhesion was experienced in nasal conditions which alongside the appropriate physicochemical properties in liquid state, contributed to rapid drug absorption through human RPMI 2650 cell line. Ex vivo studies also confirmed that higher nasal mucosal permeation could be expected with the polymeric micelle nanoformulation compared to a regular MEL suspension. Also, the nanoformulation met the requirements to provide rapid drug permeation in less 1 hour of our measurement.

Highlights

• Meloxicam-loaded micelles provided efficient cellular permeability.

• The micelle formulation is applicable for the nasal administration.

• Meloxicam-loaded nasal micelles achieved efficient concentration in the brain.

The non-toxic, non-cell barrier damaging formulation also proved to provide a successful passive transport across excides human nasal mucosa. Based on our in vivo investigations, it can be concluded that the polymeric micelle formulation provides higher meloxicam transport to the central nervous system followed by a slow and long-lasting elimination process compared to prior results where physical particle size reduction methods were applied. With these results, a promising solution and nanocarrier is proposed for the successful transport of non-steroidal anti-inflammatory drugs with acidic character to the brain.

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Bence Sipos, Zsolt Bella, Ilona Gróf, Szilvia Veszelka, Mária A. Deli, Kálmán F. Szűcs, Anita Sztojkov-Ivanov, Eszter Ducza, Róbert Gáspár, Gábor Kecskeméti, Tamás Janáky, Balázs Volk, Mária Budai-Szűcs, Rita Ambrus, Piroska Szabó-Révész, Ildikó Csóka, Gábor Katona, Soluplus® promotes efficient transport of meloxicam to the central nervous system via nasal administration, International Journal of Pharmaceutics, 2023, 122594, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2023.122594.

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