Journal
PHARMACEUTICS
Volume 12, Issue 2, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics12020097
Keywords
meloxicam; HSA nanoparticles; nose-to-brain delivery; quality by design; physical stability; in vivo animal studies; rapid equilibrium dialysis; PAMPA
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Funding
- Ministry of Human Capacities, Hungary [20391-3/2018/FEKUSTRAT]
- National Research, Development and Innovation Office, Hungary [Richter-GINOP-2.2.1-15-2016-00007]
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The aim of this study was to optimize the formulation of meloxicam (MEL)-containing human serum albumin (HSA) nanoparticles for nose-to-brain via a quality by design (QbD) approach. Liquid and dried formulations of nanoparticles containing Tween 80 and without the surfactant were investigated. Various properties, such as the Z-average, zeta potential, encapsulation efficacy (EE), conjugation of MEL and HSA, physical stability, in vitro dissolution, in vitro permeability, and in vivo plasma and brain distribution of MEL were characterized. From a stability point of view, a solid product (Mel-HSA-Tween) is recommended for further development since it met the desired critical parameters (176 +/- 0.3 nm Z-average, 0.205 +/- 0.01 PdI, -14.1 +/- 0.7 mV zeta potential) after 6 months of storage. In vitro examination showed a significantly increased drug dissolution and permeability of MEL-containing nanoparticles, especially in the case of applying Tween 80. The in vivo studies confirmed both the trans-epithelial and axonal transport of nanoparticles, and a significantly higher cerebral concentration of MEL was detected with nose-to-brain delivery, in comparison with intravenous or per os administration. These results indicate intranasal the administration of optimized MEL-containing HSA formulations as a potentially applicable value-added product for the treatment of neuroinflammation.
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