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- Title
Development of In Situ Gelling Meloxicam-Human Serum Albumin Nanoparticle Formulation for Nose-to-Brain Application.
- Authors
Katona, Gábor; Sipos, Bence; Budai-Szűcs, Mária; Balogh, György Tibor; Veszelka, Szilvia; Gróf, Ilona; Deli, Mária A.; Volk, Balázs; Szabó-Révész, Piroska; Csóka, Ildikó; Torrado, Juan José
- Abstract
The aim of this study was to develop an intranasal in situ thermo-gelling meloxicam-human serum albumin (MEL-HSA) nanoparticulate formulation applying poloxamer 407 (P407), which can be administered in liquid state into the nostril, and to increase the resistance of the formulation against mucociliary clearance by sol-gel transition on the nasal mucosa, as well as to improve drug absorption. Nanoparticle characterization showed that formulations containing 12–15% w/w P407 met the requirements of intranasal administration. The Z-average (in the range of 180–304 nm), the narrow polydispersity index (PdI, from 0.193 to 0.328), the zeta potential (between −9.4 and −7.0 mV) and the hypotonic osmolality (200–278 mOsmol/L) of MEL-HSA nanoparticles predict enhanced drug absorption through the nasal mucosa. Based on the rheological, muco-adhesion, drug release and permeability studies, the 14% w/w P407 containing formulation (MEL-HSA-P14%) was considered as the optimized formulation, which allows enhanced permeability of MEL through blood–brain barrier-specific lipid fraction. Cell line studies showed no cell damage after 1-h treatment with MEL-HSA-P14% on RPMI 2650 human endothelial cells' moreover, enhanced permeation (four-fold) of MEL from MEL-HSA-P14% was observed in comparison to pure MEL. Overall, MEL-HSA-P14% can be promising for overcoming the challenges of nasal drug delivery.
- Subjects
PAMPAS (Argentina); SERUM albumin; GELATION; NASAL mucosa; INTRANASAL administration; DRUG absorption; PHARMACEUTICAL gels; ORAL mucosa; PHARMACOKINETICS
- Publication
Pharmaceutics, 2021, Vol 13, Issue 5, p646
- ISSN
1999-4923
- Publication type
Article
- DOI
10.3390/pharmaceutics13050646