Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems

被引:19
作者
Bartos, Csilla [1 ]
Ambrus, Rita [1 ]
Kovacs, Anita [1 ]
Gaspar, Robert [2 ]
Sztojkov-Ivanov, Anita [2 ]
Marki, Arpad [2 ]
Janaky, Tamas [3 ]
Tomosi, Ferenc [3 ]
Kecskemeti, Gabor [3 ]
Szabo-Revesz, Piroska [1 ]
机构
[1] Univ Szeged, Inst Pharmaceut Technol & Regulatory Affairs, Eotvos U 6, H-6720 Szeged, Hungary
[2] Univ Szeged, Dept Pharmacodynam & Biopharm, Eotvos U 6, H-6720 Szeged, Hungary
[3] Univ Szeged, Dept Med Chem, Dom ter 8, H-6720 Szeged, Hungary
关键词
nanosized meloxicam; meloxicam potassium monohydrate; intranasal formulation; dissolution rate; in vitro diffusion; plasma drug-content; absolute bioavailability for brain; IN-VITRO; DRUG-DELIVERY; BRAIN DELIVERY; SODIUM HYALURONATE; ALZHEIMERS-DISEASE; NANOPARTICLES; NOSE; THERAPY; RELEASE;
D O I
10.3390/molecules23040784
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The aim of this article was to study the trans-epithelial absorption to reach the blood and to target the brain by axonal transport using nasal formulations with nanonized meloxicam (nano MEL spray) and its salt form known as meloxicam potassium monohydrate (MELP spray). The physicochemical properties and the mucoadhesivity of nasal formulations were controlled. In vitro and in vivo studies were carried out. These forms were first investigated in "nose-to-brain" relation. It was found that the in vitro study and in vivo study did not show any significant correlation. In vitro experiments demonstrated faster dissolution rate and higher diffusion of MELP from the spray compared with the nano MEL spray. The administration of the nano MEL spray resulted in faster absorption and constant plasma concentration of the drug after five minutes of administration as compared to MELP. The axonal transport of the drug was justified. MEL appeared in the brain tissues after the first five minutes of administration in the case of both spray forms, but its amount was too small in comparison with the total plasma concentration. The application of the nano MEL spray resulted in the same AUC in the brain as the intravenous injection. The "nose-to-blood" results predicted the nasal applicability of MEL and MELP in pain management. The "nose-to-brain" pathway requires further study.
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页数:13
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