A new approach to encapsulating nonsteroidal anti-inflammatory drugs. II. Physicochemical properties

1987 ◽  
Vol 4 (2) ◽  
pp. 141-150 ◽  
Author(s):  
M. M. Meshali ◽  
E. Z. El-Dien ◽  
S. A. Omar ◽  
L. A. Luzzi
Keyword(s):  
Physicochemical Properties ◽  
New Approach ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

scholarly journals N,N-Dimethylformamide Prevents LPS-Induced Preterm Birth in a Murine Model by Suppressing the Inflammatory Response

2021 ◽  
Author(s):  
Zeng-Hui Wei ◽  
Oluwabukola Salami ◽  
Jagadish Koya ◽  
Swapna Munnangi ◽  
Ryan Pekson ◽  
...  
Keyword(s):  
Preterm Birth ◽  
Murine Model ◽  
Raw 264.7 Cells ◽  
New Approach ◽  
Affect Cell Viability ◽  
Pregnant Mice ◽  
Inflammatory Drugs ◽  
The Common ◽  
Anti Inflammatory

Abstract Preterm birth accounts for the majority of perinatal mortality worldwide and there remains no FDA-approved drug to prevent it. Recently, we discovered that the common drug excipient, N,N-dimethylacetamide (DMA), prevents inflammation–induced preterm birth in mice by inhibiting NF-κB. Since we reported this finding it has come to light that a group of widely used, structurally related aprotic solvents, including DMA, N-methyl-2-pyrrolidone (NMP) and dimethylformamide (DMF), have anti-inflammatory efficacy. We show here that DMF suppresses LPS-induced TNFα secretion from RAW 264.7 cells and IL-6 and IL-8 secretion from HTR-8 cells at concentrations that do not significantly affect cell viability. In vivo, DMF decreases LPS-induced inflammatory cell infiltration and expression of TNFα and IL-6 in the placental labyrinth, all to near baseline levels. Finally, DMF decreases the rate of preterm birth in LPS-induced pregnant mice (P<.0001) and the rate at which pups are spontaneously aborted (P<.0001). In summary, DMF, a widely used solvent structurally related to DMA and NMP, prevents LPS-induced preterm birth in a murine model without overt toxic or teratogenic effects. Re-purposing the DMA/DMF/NMP family of small molecules as anti-inflammatory drugs is a promising new approach to preventing inflammation–induced preterm birth and potentially other inflammatory disorders as well.

A new approach to anti-inflammatory drugs

1979 ◽  
Vol 28 (12) ◽  
pp. 1959-1961 ◽  
Author(s):  
Gerald A. Higgs ◽  
Roderick J. Flower ◽  
John R. Vane
Keyword(s):  
New Approach ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

scholarly journals Therapeutic Liquid Formulations Based on Low Transition Temperature Mixtures for the Incorporation of Anti-Inflammatory Drugs

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1620
Author(s):  
Ana Roda ◽  
Alexandre Paiva ◽  
Ana Rita C. Duarte
Keyword(s):  
Transition Temperature ◽  
Physicochemical Properties ◽  
Aqueous Solubility ◽  
Therapeutic Efficiency ◽  
Promising Tool ◽  
Solubility Improvement ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
L929 Mouse ◽  
State Of Art

Most nonsteroidal anti-inflammatory drugs (NSAIDs) present poor aqueous solubility, impairing their efficiency in physiological media. In this context, Low Transition Temperature Mixtures (LTTMs) are a promising platform to overcome drugs’ poor solubility, forming therapeutic liquid formulations. In this work, the LTTMs of citric acid:L-arginine:water (C:A:W) and glycerol:sorbitol (G:S) were studied in terms of their features and assessed in terms of their ability to increase the solubility of six NSAIDs in physiological media. The physicochemical properties of LTTMs were characterized by state-of-art techniques commonly used for these systems. The cytotoxicity of G:S was also evaluated in L929 mouse fibroblasts and the viscosity, polarity, and pH properties of the studied mixtures were related to the solubility of NSAIDs. The pH and polarity were the parameters that most influenced the drugs’ solubility. Ibuprofen, naproxen, ketoprofen, indomethacin, and flurbiprofen did not present any solubility improvement in the formulations tested. However, concentrated mixtures of C:A:W or G:S in the physiologic-mimicked media (PBS) rendered a celecoxib solubility 4 and 5 times higher than PBS, respectively. These therapeutic liquid formulations of celecoxib in C:A:W or G:S can be a promising tool to increase celecoxib’s therapeutic efficiency in local applications.

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