Modifying the physicochemical properties of NSAIDs for nasal and pulmonary administration

Szabó‐Révész, Piroska

doi:10.1016/j.ddtec.2018.03.002

Cited by 28 publications

(22 citation statements)

References 42 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Since the oral administration of NSAIDs results in poor brain penetration, it is favorable to use alternative methods of drug delivery. Nasal delivery provides a promising administration route for the following reasons: the nasal mucosa has a large surface area that is available for drug absorption and the drug can be absorbed directly into the brain and therefore avoids the efflux mechanism of BBB, which offers the possibility of local treatment of the neuroinflammation [5,6]. Furthermore, the easy accessibility of the nasal cavity allows for quick self-administration, thus further improving patient expectations.…”

Section: Introductionmentioning

confidence: 99%

Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach

et al. 2020

View full text Add to dashboard Cite

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.

show abstract

Section: Introductionmentioning

confidence: 99%

Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach

et al. 2020

View full text Add to dashboard Cite

show abstract

“…For pulmonary disorders with increased inflammation, the use of non-steroidal antiinflammatory drugs (NSAIDs), such as ibuprofen, diclofenac, gained the attention of research studies (Szabó-Révész, 2018). Among NSAIDs, meloxicam (MX) is a low water-soluble cyclooxygenase enzyme-2 selective inhibitor, which has anti-inflammatory and antioxidant effects.…”

Section: Introductionmentioning

confidence: 99%

Formulation and comparison of spray dried non-porous and large porous particles containing meloxicam for pulmonary drug delivery

Chvatal

Ambrus

Party

et al. 2019

International Journal of Pharmaceutics

View full text Add to dashboard Cite

Meloxicam is an anti-inflammatory drug that could be interesting to deliver locally to the lungs to treat inflammation occurring in cystic fibrosis or chronic obstructive pulmonary disease (COPD). Spray drying conditions were optimized to prepare inhalable dry powders, from meloxicam aqueous solution with pH adjustment. A comparison study between non-porous and large porous particles (LPPs) was carried out to demonstrate the relevance of the aimed large size (>5 µm) and low density (<0.2 mg/cm 3) formulations. With the appropriate amount of porogen agent, ammonium bicarbonate, LPPs exhibited the same aerodynamic diameter and a higher deposited fraction than smaller but dense particles. The aerodynamic evaluation of LPPs showed that the fine particle fraction (FPF) reached up to 65.8%, while the emitted fraction (EF) reached 85.4%, both higher than for the non-porous particles. Stability tests demonstrated that, after 10 weeks of storage, no significant difference could be detected in the aerodynamic behaviour of the formulations. To the best of our knowledge this is the first time large porous particles, with enhanced aerodynamic properties, from an aqueous solution of meloxicam are reported.

show abstract

“…Formulation and investigation of novel, carrier-based dry powder inhalation system Edit Administration of the drug via the lung has several advantages in the treatment of lung diseases, such as cystic fibrosis and chronic obstructive pulmonary disease. Thus, the development of dry powder systems (DPIs) containing antibiotic [1] and non-steroidal antiinflammatory [2] agents is on every account warranted. In the case of development, it should be borne in mind that the active ingredient particles have a good morphology and low density, between the average particle size of 1-10 µm and the cohesion between the particles is as small as possible.…”

Section: Op-13mentioning

confidence: 99%

Formulation and investigation of novel, carrier-based dry powder inhalation system

Benke

Ambrus

Szabó‐Révész

2019

I. Symposium of Young Researchers on Pharmaceutical Technology, Biotechnology and Regulatory Science

View full text Add to dashboard Cite

Modifying the physicochemical properties of NSAIDs for nasal and pulmonary administration

Cited by 28 publications

References 42 publications

Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach

Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach

Formulation and comparison of spray dried non-porous and large porous particles containing meloxicam for pulmonary drug delivery

Formulation and investigation of novel, carrier-based dry powder inhalation system

Contact Info

Product

Resources

About