Dexketoprofen Trometamol

Çelik C. Heliyon, 2024, 10(18), e37695.

Dexketoprofen trometamol (DT), a selective cyclooxygenase-1 (COX-1) inhibitor, has been investigated for its effects on immune modulation in insects, specifically in the endoparasitoid Pimpla turionellae. This study explores DT's role in modulating eicosanoid biosynthesis, particularly prostaglandins (PGs), which influence the immune response to viral infections.
In this experiment, P. turionellae adults were exposed to bovine herpes simplex virus-1 (BHSV-1) after treatment with DT via intrahaemocoelic injection and dietary administration. Results demonstrated a significant reduction in nodulation, the first immune defense mechanism involving melanization in response to microbial threats, when insects were co-injected with DT and BHSV-1. At higher dietary concentrations of DT (0.1 g/100 ml diet), the number of nodules formed was reduced by approximately 12-fold, while phenoloxidase (PO) activity, a marker for immune activation, increased nearly threefold.
Specifically, low concentrations of DT (0.001%) enhanced PO enzyme activity, while reducing nodules in virus-infected P. turionellae adults. This indicates that DT can modulate the immune response, skewing it towards heightened enzyme activity while suppressing nodulation. These findings suggest that COX-1 derived PGs play a pivotal role in the regulation of immune responses to viral pathogens in parasitic insects.

Turgut K, et al. Wilderness & Environmental Medicine, 2022, 33(4,) 379-385.

Dexketoprofen trometamol, a nonsteroidal anti-inflammatory drug (NSAID), is commonly utilized for pain relief due to its potent analgesic properties. In a recent randomized, placebo-controlled study, the efficacy of intravenous (IV) dexketoprofen trometamol was compared to IV paracetamol, topical lidocaine, and placebo in patients experiencing pain from scorpion stings. The study aimed to assess the analgesic effects within the first 60 minutes of administration in a tertiary hospital emergency department setting.
A total of 106 patients were included, with 26 assigned to the dexketoprofen trometamol group. The study found that, within the first 30 minutes, there was no significant difference in pain reduction between the treatment groups (P=0.185). However, after 60 minutes, both IV dexketoprofen trometamol and IV paracetamol provided significantly better pain relief compared to placebo (P<0.05). Interestingly, the analgesic effects of dexketoprofen trometamol and topical lidocaine were not significantly different (P>0.05), indicating that dexketoprofen trometamol could be a viable alternative to topical treatments in acute pain management.
This evidence supports the use of IV dexketoprofen trometamol as an effective analgesic for managing moderate to severe pain, particularly in emergency settings where rapid onset of action is critical. Furthermore, its comparable efficacy to paracetamol underscores its potential as an important therapeutic option in the management of acute pain resulting from injuries such as scorpion stings.

Soliman SM, et al. International Journal of Pharmaceutics, 2023, 631, 122525.

Dexketoprofen trometamol (DKT), a water-soluble nonselective NSAID, is widely used for its anti-inflammatory and analgesic properties. However, its clinical efficacy is limited due to rapid renal elimination following oral administration. To overcome these limitations, transdermal drug delivery systems, particularly invasomes, have been explored to enhance DKT's permeation through the skin, providing sustained therapeutic effects.
This study developed and characterized DKT-loaded invasomes, optimized with Citral, to improve transdermal flux and skin deposition. The formulation (C1) demonstrated optimal encapsulation efficiency (86.51 ± 1.05%) and nanosized vesicles (211.9 ± 0.57 nm), with a PDI of 0.353 and a ZP of -19.15 ± 2.45 mV, indicating stable formulations. The invasomes significantly increased DKT flux by 2.6 folds and deposition in skin layers by 3.51 folds compared to conventional gel formulations.
In an in vivo model of xylene-induced ear edema in rats, DKT transdermal invasomes (C1-G) exhibited substantial anti-inflammatory activity. The formulation reduced the upregulation of pro-inflammatory markers such as COX-2, MPO, NF-κB, TNF-α, IL-1β, and MDA levels, while restoring oxidative stress markers like GSH and TAC. Histopathological analysis supported these findings, confirming the formulation's efficacy in mitigating inflammation and oxidative damage.

Öztürk AA, et al. Microvascular Research, 2020, 128, 103961.

This case study focuses on the formulation of a novel oral controlled-release dosage form of dexketoprofen trometamol (DT), designed to achieve lower dosages and minimize side effects. The primary objective is to enhance the therapeutic profile of DT while improving patient compliance.
In this study, chitosan (CS) nanoparticles (CS-NPs) were employed as a delivery system for DT. Chitosan, a biocompatible polysaccharide, was utilized for its ability to encapsulate the drug effectively and provide controlled release. The CS-NPs were prepared using an optimized spray-drying method, ensuring high encapsulation efficiency and desirable physicochemical properties.
To prepare the CS-NPs, chitosan was dissolved in a 2% acetic acid solution and stirred for 4 hours to obtain a clear solution. Methanol was subsequently added to reduce the viscosity, and DT was incorporated into the solution under continuous stirring. The formulation was processed in a spray-drying apparatus under controlled conditions, with an inlet temperature of 120°C and an outlet temperature of 60°C. The resulting nanoparticles were collected and characterized for their size, morphology, and drug-release profile.
The findings indicate that the spray-dried chitosan nanoparticles provide a promising approach for the controlled release of DT, ensuring a prolonged analgesic effect with reduced side effects. This formulation is a significant advancement in the oral delivery of NSAIDs, offering a viable alternative to traditional dosage forms.