Topical Application of a Novel Oxycodone Gel Formulation (Tocopheryl Phosphate Mixture) in a Rat Model of Peripheral Inflammatory Pain Produces Localized Pain Relief Without Significant Systemic Exposure

2015 ◽  
Vol 104 (7) ◽  
pp. 2388-2396 ◽  
Author(s):  
Maree T. Smith ◽  
Bruce D. Wyse ◽  
Stephen R. Edwards ◽  
Mahmoud El-Tamimy ◽  
Giacinto Gaetano ◽  
...  
2021 ◽  
Vol 899 ◽  
pp. 174029
Author(s):  
Sang Wan Ryu ◽  
Yeo Ok Kim ◽  
Han-Byul Kim ◽  
Seog Bae Oh ◽  
Jeong Il Choi ◽  
...  

2021 ◽  
Vol 11 (1) ◽  
pp. 11
Author(s):  
Ira Widjiastuti ◽  
Widya Saraswati ◽  
Annisa Rahma

Background: Inflammation of the pulp can lead to elicit pain. Pain in inflammation is induced by the cyclooxygenase-2 enzyme (COX-2) which induces prostaglandin E2 (PGE2) resulting in pain. Pain in the pulp can be relieved by eugenol. In its application, eugenol is toxic to pulp fibroblasts. Due to the side effect, it is worth considering other biocompatible materials with minimal side effects, such as propolis. Flavonoids and phenolic acids that contained in propolis can inhibit COX-2. Therefore, an analysis outlined in the literature review is needed to examine the results of research related to the role of propolis as pulp pain relief by inhibiting COX-2 expression. Purpose: To analyze the role of propolis in pulp pain by inhibiting COX-2 expression. Reviews: Propolis extract that extracted by ethanol, water, and hydroalcohol has pain relief properties in the pulp by inhibiting COX-2 by directly binding to the COX-2 receptors and by reducing the production of proinflammatory cytokines which are COX-2 inducers, proven through in vivo, in vitro, and in silico studies in various target cell organs. Conclusion: Propolis extract has high prospect as inflammatory pain inhibitor in the pulp by inhibit COX-2 expression.


Pain ◽  
2013 ◽  
Vol 154 (2) ◽  
pp. 294-305 ◽  
Author(s):  
Xianze Meng ◽  
Yu Zhang ◽  
Lixing Lao ◽  
Rikka Saito ◽  
Aihui Li ◽  
...  

2018 ◽  
Vol 96 (8) ◽  
pp. 855-858
Author(s):  
Chelsa Killey ◽  
Shane Cleary ◽  
Julie Orr ◽  
Jefferson C. Frisbee ◽  
Dwayne Jackson ◽  
...  

This study used an anaesthetized rat model to directly observe changes in diameter of the vessels supplying the sciatic nerve in response to acetylcholine (10−4 M), a muscarinic receptor agonist, and atropine (10−5 M), a muscarinic receptor antagonist. Topical application of acetylcholine resulted in increases in vessel diameter (baseline: 22.0 ± 2.5 μm, acetylcholine: 28.8 ± 3.3 μm), while topical application of atropine resulted in a decrease in diameter (baseline: 26.6 ± 3.2 μm, atropine: 15.5 ± 3.6 μm) of the epineurial vessels. Mean arterial pressure was not affected by either acetylcholine (baseline: 103.8 ± 1.8 mm Hg, acetylcholine: 102.8 ± 3.2 mm Hg) or atropine (baseline: 104.0 ± 1.9 mm Hg, atropine: 105.2 ± 2.2 mm Hg). These data suggest that muscarinic-receptor-mediated responses can affect the diameter of the epineurial vessels at the sciatic nerve. In addition, muscarinic-receptor-mediated responses appear to contribute to baseline diameter of epineurial vessels at the sciatic nerve.


2020 ◽  
Vol 17 (1) ◽  
Author(s):  
Na Meng ◽  
Ning-Ning Ji ◽  
Ziming Zhou ◽  
Yicheng Qian ◽  
Yu Tang ◽  
...  

2015 ◽  
Vol 3 (5) ◽  
pp. 703-706 ◽  
Author(s):  
BOPAIAH P. CHEPPUDIRA ◽  
THOMAS H. GARZA ◽  
LAWRENCE N. PETZ ◽  
JOHN L. CLIFFORD ◽  
MARCIE FOWLER

2019 ◽  
Vol 37 (2) ◽  
Author(s):  
Cristine Steen-Louws ◽  
Peter Boross ◽  
Judith Prado ◽  
Jan Meeldijk ◽  
Jurgen B. Langenhorst ◽  
...  

Abstract Purpose Modulating sialylation of therapeutic glycoproteins may be used to influence their clearance and systemic exposure. We studied the effect of low and high sialylated IL4–10 fusion protein (IL4–10 FP) on in vitro and in vivo bioactivity and evaluated the effect of differential sialylation on pharmacokinetic parameters. Methods CHO cell lines producing low (IL4–10 FP lowSA) and high sialylated (IL4–10 FP highSA) fusion protein were generated. Bioactivity of the proteins was evaluated in an LPS-stimulated whole blood assay. Pharmacokinetics were studied in rats, analyzing plasma levels of IL4–10 FP upon intravenous injection. In vivo activity was assessed in an inflammatory pain mice model upon intrathecal injection. Results IL4–10 FP lowSA and IL4–10 FP highSA had similar potency in vitro. The pharmacokinetics study showed a 4-fold higher initial systemic clearance of IL4–10 FP lowSA, whereas the calculated half-life of both IL4–10 FP lowSA and IL4–10 FP highSA was 20.7 min. Finally, both IL4–10 FP glycoforms inhibited persistent inflammatory pain in mice to the same extent. Conclusions Differential sialylation of IL4–10 fusion protein does not affect the in vitro and in vivo activity, but clearly results in a difference in systemic exposure. The rapid systemic clearance of low sialylated IL4–10 FP could be a favorable characteristic to minimize systemic exposure after administration in a local compartment.


2019 ◽  
Vol 2019 ◽  
pp. 1-7 ◽  
Author(s):  
Chuan-Yi Zuo ◽  
Peng Lv ◽  
Cheng-Shun Zhang ◽  
Ru-Xue Lei ◽  
Wei Zhou ◽  
...  

The aim of this study was to investigate whether contralateral moxibustion would generate a similar analgesic effect with ipsilateral moxibustion. Contra- and ipsilateral moxibustion were separately applied to Zusanli (ST36) acupoints of inflammatory pain mice. The analgesic effect was evaluated, respectively, by licking/biting time (LBT) of formalin-induced inflammatory pain and thermal withdrawal latency (TWL) of complete Freund’s adjuvant- (CFA-) induced inflammatory pain. For formalin-induced pain, compared with formalin group, the total LBT of ipsi- and contralateral moxibustion reduced in both phase I and phase II, but there was no significant difference between ipsi- and contralateral moxibustion. For CFA-induced inflammatory pain, compared with CFA group, TWL of ipsi- and contra-Moxi groups increased immediately after moxibustion intervention; however there was no obvious difference between ipsi- and contralateral moxibustion at any timepoint. It indicated that contralateral moxibustion had a similar analgesic effect with ipsilateral moxibustion in both formalin- and CFA-induced pain. These results suggest that both ipsi- and contralateral moxibustion could be applied for pain relief.


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