Drug-drug eutectic mixtures of celecoxib with tapentadol and milnacipran which could improve analgesic and antidepressant efficacy

Yang, Zhengge; Ma, Ru; Yin, Chenghong; Yi-fang, Zhang; Liu, Xin; Liu, Bi-Feng; Zhang, Guisen; Hao, Chao

doi:10.1016/j.jddst.2021.102995

Cited by 6 publications

(8 citation statements)

References 50 publications

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“…However, in general, the intensities of the diffraction peaks decreased. These results prove that the co‐crystallization of fenofibric acid and syringic acid produced a eutectic mixture rather than a new cocrystal phase [21] . The PXRD data support the thermal behavior analysis of the binary mixture mentioned earlier.…”

Section: Resultssupporting

confidence: 82%

Eutectic Mixture of Fenofibric Acid and Syringic Acid: Improvement of Dissolution Rate and Its Antihyperlipidemic Activity

et al. 2023

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Fenofibric acid is a poorly water‐soluble drug with high permeability; thus, it is classified as a Biopharmaceutical Classification System (BCS) class II. This study aimed to prepare a eutectic mixture of fenofibric acid with syringic acid as a coformer to improve its solubility, dissolution rate, and antihyperlipidemic activity. The solvent co‐evaporation method was used to form a eutectic mixture. Solid‐state properties were characterized, solubility and in vitro dissolution profiles were studied, and in vivo antihyperlipidemic effectiveness was investigated in male Wistar rats. The results showed that the eutectic mixture of fenofibric acid‐syringic acid enhanced the solubility (3.4‐fold) and in vitro dissolution rate (3.62‐fold) and significantly improved the antihyperlipidemic activity compared with intact fenofibric acid.

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Section: Resultssupporting

confidence: 82%

Eutectic Mixture of Fenofibric Acid and Syringic Acid: Improvement of Dissolution Rate and Its Antihyperlipidemic Activity

et al. 2023

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Section: Determination Of Mixtures Composition At the Eutectic Pointmentioning

confidence: 99%

“…Eutectic mixtures are easily produced [24] and may offer a potentially fruitful alternative for combination therapy [16]. Furthermore, the eutectic mixtures are cost-effective, easily scaled-up, and do not require clinical trials [16,28]. Hence, the aim of this study was to obtain a eutectic mixture from SQV using PIP as a coformer to improve the dissolution of this Class II drug.…”

Section: Determination Of Mixtures Composition At the Eutectic Pointmentioning

confidence: 99%

“…Over 50 years ago, crystal engineering was applied to a wide range of crystalline powders in order to modulate the performance of Class II and IV raw materials [2][3][4]. Since then, the process of reducing particle size to increase the surface area [5][6][7], as well as obtaining salts [4,8,9], nanocrystals [10,11], cocrystals [12,13], and eutectic mixtures [14][15][16] were some of the approaches that have been explored. Saquinavir base (SQV) (Figure 1) is an anti-HIV drug which belongs to Class II in the BCS.…”

Section: Introductionmentioning

confidence: 99%

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Saquinavir-Piperine Eutectic Mixture: Preparation, Characterization, and Dissolution Profile

Fandaruff,

Quirós-Fallas,

Vega-Baudrit

et al. 2023

Pharmaceutics

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The dissolution rate of the anti-HIV drug saquinavir base (SQV), a poorly water-soluble and extremely low absolute bioavailability drug, was improved through a eutectic mixture formation approach. A screening based on a liquid-assisted grinding technique was performed using a 1:1 molar ratio of the drug and the coformers sodium saccharinate, theobromine, nicotinic acid, nicotinamide, vanillin, vanillic acid, and piperine (PIP), followed by differential scanning calorimetry (DSC). Given that SQV-PIP was the only resulting eutectic system from the screening, both the binary phase and the Tammann diagrams were adapted to this system using DSC data of mixtures prepared from 0.1 to 1.0 molar ratios in order to determine the exact eutectic composition. The SQV-PIP system formed a eutectic at a composition of 0.6 and 0.40, respectively. Then, a solid-state characterization through DSC, powder X-ray diffraction (PXRD), including small-angle X-ray scattering (SAXS) measurements to explore the small-angle region in detail, Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), and a powder dissolution test were performed. The conventional PXRD analyses suggested that the eutectic mixture did not exhibit structural changes; however, the small-angle region explored through the SAXS instrument revealed a change in the crystal structure of one of their components. FT-IR spectra showed no molecular interaction in the solid state. Finally, the dissolution profile of SQV in the eutectic mixture was different from the dissolution of pure SQV. After 45 min, approximately 55% of the drug in the eutectic mixture was dissolved, while, for pure SQV, 42% dissolved within this time. Hence, this study concludes that the dissolution rate of SQV can be effectively improved through the approach of using PIP as a coformer.

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“…Celecoxib undergoes substantial human metabolism and is eliminated predominantly through metabolites [ 11 ]. Celecoxib’s bioavailability has been improved through the use of a variety of formulation strategies, including a self-micro-emulsifying delivery system [ 13 ], solid lipid nanoparticles (NPs) [ 14 ], the formation of a complex with β-cyclodextrins [ 15 , 16 ], the formation of eutectic mixtures [ 17 ], and the utilization of silica–lipid hybrid microcapsules [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

Celecoxib-Loaded Cubosomal Nanoparticles as a Therapeutic Approach for Staphylococcus aureus In Vivo Infection

Alshawwa,

El-Masry,

Nasr

et al. 2023

Microorganisms

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There is a great need for novel approaches to treating bacterial infections, due to the vast dissemination of resistance among pathogenic bacteria. Staphylococcus aureus are ubiquitous Gram-positive pathogenic bacteria and are rapidly acquiring antibiotic resistance. Here, celecoxib was encapsulated into cubosomal nanoparticles, and the particle morphology, size distribution, zeta potential, entrapment efficiency, and celecoxib release were evaluated in vitro. Also, a systemic infection model in mice elucidated the in vivo antibacterial action of the celecoxib cubosomes. Cubosomes are a nanotechnology-based delivery system which can adhere to the external peptidoglycan layers of Gram-positive bacteria and penetrate them. The size distribution investigation revealed that the prepared celecoxib-loaded cubosomes had a mean particle size of 128.15 ± 3.04 nm with a low polydispersity index of 0.235 ± 0.023. The zeta potential measurement showed that the prepared cubosomes had a negative surface charge of −17.50 ± 0.45, indicating a highly stable nanodispersion formation with little susceptibility to particle aggregation. The cubosomal dispersion exhibited an entrapment efficiency of 88.57 ± 2.36%. The transmission electron micrograph for the prepared celecoxib-loaded cubosomes showed a narrow size distribution for the cubosomal nanoparticles, which had a spherical shape and were non-aggregated. The tested cubosomes diminished the inflammation in the treated mice’s liver and spleen tissues, as revealed by hematoxylin and eosin stain and Masson’s trichrome stain. The immunostained tissues with nuclear factor kappa B and caspase-3 monoclonal antibodies revealed a marked decrease in these markers in the celecoxib-treated group, as it resulted in negative or weak immunostaining in liver and spleen that ranged from 4.54% to 17.43%. This indicates their inhibitory effect on the inflammatory pathway and apoptosis, respectively. Furthermore, they reduced the bacterial burden in the studied tissues. This is alongside a decrease in the inflammatory markers (interleukin-1 beta, interleukin-6, cyclooxygenase-2, and tumor necrosis factor-alpha) determined by ELISA and qRT-PCR. The IL-1β levels were 16.66 ± 0.5 pg/mg and 17 ± 0.9 pg/mg in liver and spleen, respectively. Also, IL-6 levels were 85 ± 3.2 pg/mg and 84 ± 2.4 pg/mg in liver and spleen, respectively. In conclusion, the current study introduced cubosomes as an approach for the formulation of celecoxib to enhance its in vivo antibacterial action by improving its oral bioavailability.

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Drug-drug eutectic mixtures of celecoxib with tapentadol and milnacipran which could improve analgesic and antidepressant efficacy

Cited by 6 publications

References 50 publications

Eutectic Mixture of Fenofibric Acid and Syringic Acid: Improvement of Dissolution Rate and Its Antihyperlipidemic Activity

Eutectic Mixture of Fenofibric Acid and Syringic Acid: Improvement of Dissolution Rate and Its Antihyperlipidemic Activity

Saquinavir-Piperine Eutectic Mixture: Preparation, Characterization, and Dissolution Profile

Celecoxib-Loaded Cubosomal Nanoparticles as a Therapeutic Approach for Staphylococcus aureus In Vivo Infection

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