Analgesic effect of flurbiprofen ester and its effect on serum inflammatory factors and Β-endorphin expression in rats with incision pain

Here, we evaluate the feasibility of co-loading plain ranitidine hydrochloride (RHCl) and microencapsulated flurbiprofen (FBP) in a Lycoat® RS780-based oral fast disintegrating film (ODF). These films were developed by the solvent casting method to minimize the adverse effects of FBP and reduce the dosage form burden on patients. Optimized FBP microparticles (M3) with an average size of 21.2 ± 9.2 µm were loaded alone (F1) and in combination with plain RHCl (F2) in the composite ODF. All films were evaluated physicomechanically and physicochemically. These films were resilient, flexible, and disintegrated within thirty seconds. SEM images showed intact FBP microparticles in both formulations and, moreover, did not observe an interaction between the drug and film components. Microencapsulated FBP was released in a controlled manner over 48 h from the proposed formulations, while RHCl was released within 5 min from F2. After in vitro evaluation, formulations were also tested for in vivo anti-inflammatory activity, cytokine (TNF-α and IL-6) levels, and gastroprotective effects in rats. The anti-inflammatory activity and gastroprotective effect of F2 were markedly higher than pure FBP and other synthesized formulations (M3 and F1). The average score of gastric lesions was in the order of pure FBP (15.5 ± 1.32) > M3 (8 ± 2) > F1 (1 ± 0.5) > F2 (0.5 ± 0) > control (0). Additionally, F2 showed a sustained anti-inflammatory effect up to 10 h in the rat paw edema model. Furthermore, F2 also markedly reduced TNF-α and IL-6 levels. Conclusively, the Lycoat® RS780-based composite film could be a promising carrier for the co-loading of microencapsulated FBP with RHCl. In the future, an optimized formulation (F2) could be capable of countering the issues related to multiple drug administration in geriatric patients and evading the gastric irritation associated with FBP.

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“…F1 and F2 were administered to animals and were equivalent to 5 mg/kg of FBP. Pure FBP was also administered at 5 mg/kg for comparison [ 34 ].…”

Section: Methodsmentioning

confidence: 99%

In Vitro and In Vivo Evaluation of Composite Oral Fast Disintegrating Film: An Innovative Strategy for the Codelivery of Ranitidine HCl and Flurbiprofen

et al. 2023

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“…Flurbiprofen is a nonsteroidal anti-inflammatory drug with analgesic and antipyretic properties. However, its analgesic activity was for mild to moderate pain, similar to other NSAIDs, and it has recently been clinically used to treat various neoplastic nociception (1). Flurbiprofen is a non-selective cyclooxygenase inhibitor, both centrally and peripherally, which results in the cutoff of the sequence of inducible and housekeeping prostaglandins from arachidonic acid (2).…”

Section: Introductionmentioning

confidence: 99%

Flurbiprofen: Determination of safety profile, analgesic effect, and interaction with lipoic acid in murine

Alberifki¹,

Naser²

2023

IJVS

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our study aimed study aimed to detect and investigate the safety profile of flurbiprofen and evaluate the analgesic effects of the tail immersion and writhing tests, as well as its interaction with lipoic acid as an analgesic for visceral pain in mice. The up-and-down manner described by Dixon was utilized to determine the median lethal dose (LD50) and the median analgesic dose (ED50), the safety criteria were calculated, mathematical equations were applied, and the interaction between flurbiprofen and alpha-lipoic acid was evaluated using the writhing test. The LD50 of oral flurbiprofen was 1147.4 mg/kg, and the ED50 of oral flurbiprofen was 8.6 mg/kg using the tail immersion test. The therapeutic index was 133, and the standard safety margin was 35%. The highest analgesia time was one h after dosing, which faded after 24 h. Administration of flurbiprofen 10, 20, and 40 mg/kg had an analgesic effect in a dose-dependent manner. Flurbiprofen relieved visceral pain when dosed at 20, 40, and 80 mg/kg, with analgesic efficacies of 53, 56, and 65%, respectively. The simultaneous administration of flurbiprofen and alpha-lipoic acid had a synergistic analgesic effect on visceral pain. From our results, we conclude that flurbiprofen has a wide range of safety and is an effective analgesic for peripheral and visceral pain. The synergistic effect between flurbiprofen and alpha-lipoic acid may have clinical benefits, including reducing the dose of flurbiprofen when used together.

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Analgesic effect of flurbiprofen ester and its effect on serum inflammatory factors and Β-endorphin expression in rats with incision pain

Cited by 2 publications

References 9 publications

In Vitro and In Vivo Evaluation of Composite Oral Fast Disintegrating Film: An Innovative Strategy for the Codelivery of Ranitidine HCl and Flurbiprofen

In Vitro and In Vivo Evaluation of Composite Oral Fast Disintegrating Film: An Innovative Strategy for the Codelivery of Ranitidine HCl and Flurbiprofen

Flurbiprofen: Determination of safety profile, analgesic effect, and interaction with lipoic acid in murine

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