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

Bartos, Csilla; Ambrus, Rita; Sipos, Péter; Budai-Szűcs, Mária; Csányi, Erzsébet; Gáspár, Róbert; Márki, Árpád; Seres, Adrienn B.; Sztojkov‐Ivanov, Anita; Horváth, Tamás; Szabó‐Révész, Piroska

doi:10.1016/j.ijpharm.2015.06.046

Cited by 39 publications

(43 citation statements)

References 34 publications

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“…According to our pervious results, the pharmacokinetics of nasally applied MX nanoparticles was similar to that after intravenous injection: the C max was reached within 5 min (Kürti et al, 2013). Nasal absorption can be improved through the higher mucoadhesivity of the MX-containing formulation, which increases the residence time in the nasal cavity, and the formation of a well-structured system can ensure the controlled release of MX without C max (Bartos et al, 2015).…”

Section: Discussionmentioning

confidence: 59%

“…In our earlier study, intranasal formulations with a low concentration of HA exhibited a viscoelastic character (Bartos et al, 2015), which was not influenced by micro-and nanoparticles of MX. As a viscosity enhancer, HA aids the homogeneous distribution of suspended drug in the nasal formulation and acts as a mucoadhesive agent, resulting in a longer residence time on the mucosa.…”

Section: Mucoadhesionmentioning

confidence: 75%

“…In the shear rate interval from 0.1 to 100 1/s, viscosity values were plotted. The method was based on earlier studies by Bartos et al (2015). To clarify the roles of MX and MXP in mucoadhesion, samples were prepared with and without mucin; the samples containing mucin were stirred for 3 h before the measurements (the final mucin concentration was 5% w/w).…”

Section: Examination Of Intranasal Spraysmentioning

confidence: 99%

“…The drug contents of blood samples were quantitated with an Agilent 1260 HLPC system (QP, DAD, ALS). The method was published earlier (Bartos et al, 2015). MX, MXP and piroxicam (PIR) as internal standard were separated on a C18 column (Phenomenex Inc., Torrance, CA, USA).…”

Section: Examination Of Intranasal Spraysmentioning

confidence: 99%

“…In our previous work, MX was chosen as NSAID for intranasal administration in order to attain an analgesic effect. MX has poor aqueous solubility (4.4 μg/ml at 25°C) (Ambrus et al, 2009), and we therefore used a "top-down" method with the aim of reducing the particle size into the micro or the nano-range and hence improving its bioavailability, such as dry ball-milling (Kürti et al, 2011), high-pressure homogenization (Pomázi et al, 2013) and combined wet milling technology (Bartos et al, 2015). Nanosuspensions, as potential drug formulations, can be achieved by combined wet milling technology (Liua et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

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Effect of solubility enhancement on nasal absorption of meloxicam

Horváth

Ambrus

Völgyi

et al. 2016

European Journal of Pharmaceutical Sciences

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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.

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Section: Discussionmentioning

confidence: 59%

Section: Mucoadhesionmentioning

confidence: 75%

Section: Examination Of Intranasal Spraysmentioning

confidence: 99%

Section: Examination Of Intranasal Spraysmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Effect of solubility enhancement on nasal absorption of meloxicam

Horváth

Ambrus

Völgyi

et al. 2016

European Journal of Pharmaceutical Sciences

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Nose

Hafner

Szabó‐Révész

2023

Practical Pharmaceutics

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Amorphous nasal powder advanced performance: in vitro/ex vivo studies and correlation with in vivo pharmacokinetics

Henriques,

Bicker,

Carona

et al. 2023

J. Pharm. Investig.

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Purpose Amorphous solid dispersions (ASD) for nasal delivery offer the opportunity to increase drug release performance, while using polymers with mucoadhesive properties. The aim of the present study was to apply this solubility enhancement technique to a poorly soluble drug for nasal delivery, while comparing two particle engineering strategies, namely spray dried microparticles and chimeral agglomerates, with the corresponding physical blends with crystalline drug. Methods Formulations of piroxicam were manufactured using varied polymer and particle engineering strategies and evaluated through in vitro drug release and ex vivo permeation studies, as well as nasal deposition and in vivo pharmacokinetic studies. Results ASD with hydroxypropyl methylcellulose (HPMC) showed enhanced drug release and permeation, compared to polyvinylpyrrolidone/vinyl acetate formulations and blends. Nasal deposition of HPMC chimeral agglomerates suggested off-target deposition. In vivo pharmacokinetic studies revealed that spray-dried HPMC-containing microparticles exhibited the highest maximum plasma concentration (Cmax) and the lowest time to attain it (tmax). In vitro release rate and in vivo absorption rate were correlated as well as tmax and in vitro performance. When excluding the formulation with least nasal targeted deposition, in vitro release and ex vivo permeation performance were also correlated with Cmax and area under the drug concentration-time curve (AUC) from 0 to 1 h, with R2 > 0.89. Conclusion ASD for nasal delivery provide fast drug absorption, which depends on the supersaturation ability of the polymer employed. In vitro-in vivo correlations suggested that in vitro release and ex vivo permeation studies are predictive tools regarding nasal absorption.

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

Cited by 39 publications

References 34 publications

Effect of solubility enhancement on nasal absorption of meloxicam

Effect of solubility enhancement on nasal absorption of meloxicam

Nose

Amorphous nasal powder advanced performance: in vitro/ex vivo studies and correlation with in vivo pharmacokinetics

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