In vitro and in vivo characterization of meloxicam nanoparticles designed for nasal administration

Kürti, Levente; Gáspár, Róbert; Márki, Árpád; Kápolna, Emese; Bocsik, Alexandra; Veszelka, Szilvia; Bartos, Csilla; Ambrus, Rita; Vastag, Mónika; Deli, Mária A.; Szabó‐Révész, Piroska

doi:10.1016/j.ejps.2013.03.012

Cited by 52 publications

(32 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The results indicated that the reduction of the MX particle size into the nanorange led to increased saturation solubility and dissolution rate, and an increased adhesiveness to surfaces as compared with micronized MX particles. In our earlier studies, MX proved not to be toxic in a cell culture model of the nasal epithelium and did not influence the paracellular pathway (Kürti et al, 2013).…”

Section: Introductionmentioning

confidence: 71%

See 1 more Smart Citation

Effect of solubility enhancement on nasal absorption of meloxicam

Horváth

Ambrus

Völgyi

et al. 2016

European Journal of Pharmaceutical Sciences

Self Cite

View full text Add to dashboard Cite

Besides the opioids the standard management of the World Health Organization suggests NSAIDs (non-steroidal anti-inflammatory drugs) alone or in combination to enhance analgesia in malignant and non-malignant pain therapy. The applicability of NSAIDs in a nasal formulation is a new approach in pharmaceutical technology. In order to enhance the nasal absorption of meloxicam (MX) as an NSAID, its salt form, meloxicam potassium monohydrate (MXP), registered by Egis Plc., was investigated in comparison with MX. The physico-chemical properties of the drugs (structural analysis, solubility and dissolution rate) and the mucoadhesivity of nasal formulations were controlled. In vitro and in vivo studies were carried out to determine the nasal applicability of MXP as a drug candidate in pain therapy. It can be concluded that MX and MXP demonstrated the same equilibrium solubility at the pH5.60 of the nasal mucosa (0.017mg/ml); nonetheless, MXP indicated faster dissolution and a higher permeability through the synthetic membrane. The animal studies justified the short T value (15min) and the high AUC of MXP, which is important in acute pain therapy. It can be assumed that the low mucoadhesivity of MXP spray did not increase the residence time in the nasal cavity, and the elimination from the nasal mucosa was therefore faster than in the case of MX. Further experiments are necessary to prove the therapeutic relevance of this MXP-containing innovative intranasal formulation.

show abstract

Section: Introductionmentioning

confidence: 71%

“…MX was the first enolic acid oxicam derivative patented for intranasal administration (Castile et al, 2005). MX has poor water solubility and is relatively well-permeable, and different strategies were therefore used to increase its dissolution rate and solubility (Ambrus et al, 2009, Kürti et al, 2013.…”

Section: Discussionmentioning

confidence: 99%

Effect of solubility enhancement on nasal absorption of meloxicam

Horváth

Ambrus

Völgyi

et al. 2016

European Journal of Pharmaceutical Sciences

Self Cite

View full text Add to dashboard Cite

show abstract

“…A dissolved MEL-containing nasal formulation was patented by Castile et al (2005), but a MEL-containing nanosuspension has not been described to date. MEL proved not to be toxic in a cell culture model of the nasal epithelium and did not influence the paracellular pathway (Kürti et al, 2013). MEL has poor aqueous solubility (4.4 µg/ml) (Ambrus et al, 2009) and high melting point (270 ºC) (Hughey et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Study of sodium hyaluronate-based intranasal formulations containing micro- or nanosized meloxicam particles

Bartos

Ambrus

Sipos

et al. 2015

International Journal of Pharmaceutics

Self Cite

View full text Add to dashboard Cite

“…Currently, glucocorticoids and hyaluronic acid are available for IA administration. 5 Meloxicam-loaded poly (D,L-lactideco-glycolide) (PLGA) nanoparticles were prepared using salting out and emulsion evaporation methods for the treatment of colon adenocarcinoma cells. 6,7 These polymers have many applications in wound healing, cell culture, tissue engineering, drug delivery, and gene delivery.…”

Section: Introductionmentioning

confidence: 99%

Design and optimization of alginate−chitosan−pluronic nanoparticles as a novel meloxicam drug delivery system

Fattahpour

Shamanian

Tavakoli

et al. 2015

J of Applied Polymer Sci

View full text Add to dashboard Cite

The inflammation and pain associated with osteoarthritis are treated with nonsteroidal anti-inflammatory drugs (NSAIDs). This treatment is accompanied by several side effects; therefore local intra articular (IA) NSAID injection can be more efficient and safe than systemic administration or topical use. In this study, alginate2chitosan2pluronic nanoparticles were considered as a new vehicle for IA meloxicam delivery. These novel nanoparticles were prepared using an ionotropic gelation method and were optimized for variables such as alginate to chitosan mass ratio, pluronic concentration, and meloxicam concentration using a 3-factor in 3-level Box-Behnken design. To optimize the formulation, the dependent variables considered were particle size, zeta potential, entrapment efficiency, and mean dissolution time (MDT). The nanoparticles morphology was characterized by FESEM and AFM. The potential interactions of the drug-polymers were investigated by ATR-FTIR and DSC, and the delivery profile of meloxicam from the nanoparticles was obtained. The average particle size of the optimized nanoparticles was 283 nm, the zeta potential was 216.9 mV, the meloxicam entrapment efficiency was 55%, and the MDT was 8.9 hours. The cumulative released meloxicam amount from the composite nanoparticles was 85% at pH 7.4 within 96 h. The release profile showed an initial burst release followed by a sustained release phase. The release mechanism was non-Fickian diffusion.Recently, several studies have been conducted on investigating meloxicam nanoparticles. Shaji and Varkey developed silicacoated solid lipid nanoparticles (SLNs) to evaluate the antioxidant and antiradical effects of meloxicam in the treatment of Additional Supporting Information may be found in the online version of this article.

show abstract

In vitro and in vivo characterization of meloxicam nanoparticles designed for nasal administration

Cited by 52 publications

References 33 publications

Effect of solubility enhancement on nasal absorption of meloxicam

Effect of solubility enhancement on nasal absorption of meloxicam

Study of sodium hyaluronate-based intranasal formulations containing micro- or nanosized meloxicam particles

Design and optimization of alginate−chitosan−pluronic nanoparticles as a novel meloxicam drug delivery system

Contact Info

Product

Resources

About