Evaluation of antinociceptive activity of nanoliposome-encapsulated and free-form diclofenac in rats and mice

Goh, Jun Zheng; Tang, S.N.; Chiong, Hoe Siong; Yong, Yoke Keong; Ahmad, Zubair; Hakim, Muhammad Nazrul

doi:10.2147/ijn.s75545

Cited by 9 publications

(4 citation statements)

References 30 publications

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“…The capsaicin test confirmed the long-lasting effects of Ibuprofen-loaded niosomes. Similar results were obtained with diclofenac-loaded liposomes administered orally, as reported by Goh et al [43]. Consistently, in a formalin test, Ibuprofen-loaded niosomes displayed a peripheral antinociceptive activity and were more effective than free Ibuprofen in suppressing inflammatory pain.…”

Section: Discussionsupporting

confidence: 89%

Long-Lasting, Antinociceptive Effects of pH-Sensitive Niosomes Loaded with Ibuprofen in Acute and Chronic Models of Pain

et al. 2019

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Ibuprofen is one of the non-steroidal anti-inflammatory drugs (NSAIDs) widely used to treat pain conditions. NSAIDs encounter several obstacles to passing across biological membranes. To overcome these constraints, we decided to study the effects of a new pH-sensitive formulation of niosomes containing Polysorbate 20 derivatized by Glycine and loaded with ibuprofen (NioIbu) in several animal models of pain in mice. We performed two tests commonly used to study acute antinociceptive activity, namely the writhing test and the capsaicin test. Our results demonstrated that NioIbu, administered 2 h before testing, reduced nociception, whereas the free form of ibuprofen was ineffective. In a model of inflammatory pain, hyperalgesia induced by zymosan, NioIbu induced a long-lasting reduction in hyperalgesia in treated mice. In a model of neuropathic pain induced by sciatic nerve chronic constriction, NioIbu reduced both neuropathy-induced allodynia and hyperalgesia. The results obtained in our experiments suggest that pH-sensitive niosomes containing Polysorbate 20 derivatized by Glycine is an effective model for NSAIDs delivery, providing durable antinociceptive effects and reducing the incidence of side effects.

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Section: Discussionsupporting

confidence: 89%

Long-Lasting, Antinociceptive Effects of pH-Sensitive Niosomes Loaded with Ibuprofen in Acute and Chronic Models of Pain

et al. 2019

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“…ambrosioides HCE had anti-inflammatory and antinociceptive effects, which means that it is similar to drugs already used therapeutically. One example is diclofenac, a non-steroidal anti-inflammatory that reduced the intensity of mechanical hyperalgesia [ 32 ].…”

Section: Discussionmentioning

confidence: 99%

Chenopodium ambrosioides L. Reduces Synovial Inflammation and Pain in Experimental Osteoarthritis

et al. 2015

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The chronicity of osteoarthritis (OA), characterized by pain and inflammation in the joints, is linked to a glutamate receptor, N-methyl-D-aspartate (NMDA). The use of plant species such as Chenopodium ambrosioides L. (Amaranthaceae) as NMDA antagonists offers a promising perspective. This work aims to analyze the antinociceptive and anti-inflammatory responses of the crude hydroalcoholic extract (HCE) of C. ambrosioides leaves in an experimental OA model. Wistar rats were separated into six groups (n = 24): clean (C), negative control (CTL-), positive control (CTL+), HCE0.5, HCE5 and HCE50. The first group received no intervention. The other groups received an intra-articular injection of sodium monoiodoacetate (MIA) (8 mg/kg) on day 0. After six hours, they were orally treated with saline, Maxicam plus (meloxicam + chondroitin sulfate) and HCE at doses of 0.5 mg/kg, 5 mg/kg and 50 mg/kg, respectively. After three, seven and ten days, clinical evaluations were performed (knee diameter, mechanical allodynia, mechanical hyperalgesia and motor activity). On the tenth day, after euthanasia, synovial fluid and draining lymph node were collected for cellular quantification, and cartilage was collected for histopathological analysis. Finally, molecular docking was performed to evaluate the compatibility of ascaridole, a monoterpene found in HCE, with the NMDA receptor. After the third day, HCE reduced knee edema. HCE5 showed less cellular infiltrate in the cartilage and synovium and lower intensities of allodynia from the third day and of hyperalgesia from the seventh day up to the last treatment day. The HCE5 and HCE50 groups improved in forced walking. In relation to molecular docking, ascaridole showed NMDA receptor binding affinity. C. ambrosioides HCE was effective in the treatment of OA because it reduced synovial inflammation and behavioral changes due to pain. This effect may be related to the antagonistic effect of ascaridole on the NMDA receptor.

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“…To ensure DREADDs did not transfect thermal nociceptors, animals were subjected to the Hargreaves test (Ugo Basile, catalog number: 37370) with methods described by Goh et al [40]. In brief, rats were placed individually in clear plastic chambers for 5 min each day for three days to acclimate.…”

Section: Hargreaves Test (Thermal Hyperalgesia)mentioning

confidence: 99%

Addition of angled rungs to the horizontal ladder walking task for more sensitive probing of sensorimotor changes

et al. 2021

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One method for the evaluation of sensorimotor therapeutic interventions, the horizontal ladder walking task, analyzes locomotor changes that may occur after disease, injury, or by external manipulation. Although this task is well suited for detection of large effects, it may overlook smaller changes. The inability to detect small effect sizes may be due to a neural compensatory mechanism known as “cross limb transfer”, or the contribution of the contralateral limb to estimate an injured or perturbed limb’s position. The robust transfer of compensation from the contralateral limb may obscure subtle locomotor outcomes that are evoked by clinically relevant therapies, in the early onset of disease, or between higher levels of recovery. Here, we propose angled rungs as a novel modification to the horizontal ladder walking task. Easily-adjustable angled rungs force rats to locomote across a different locomotion path for each hindlimb and may therefore make information from the contralateral limb less useful. Using hM3Dq (excitatory) Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) expressed in large diameter peripheral afferents of the hindlimb in the intact animal, we characterized the sensitivity of our design to detect stepping differences by comparing locomotor changes observed on angled rungs to those observed on a standard horizontal ladder. On our novel asymmetrical ladder, activation of DREADDs resulted in significant differences in rung misses (p = 0.000011) and weight-supporting events (p = 0.049). By comparison, on a standard ladder, we did not observe differences in these parameters (p = 0.86 and p = 0.98, respectively). Additionally, no locomotor differences were detected in baseline and inactivated DREADDs trials when we compared ladder types, suggesting that the angled rungs do not change animal gait behavior unless intervention or injury is introduced. Significant changes observed with angled rungs may demonstrate more sensitive probing of locomotor changes due to the decoupling of cross limb transfer.

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Evaluation of antinociceptive activity of nanoliposome-encapsulated and free-form diclofenac in rats and mice

Cited by 9 publications

References 30 publications

Long-Lasting, Antinociceptive Effects of pH-Sensitive Niosomes Loaded with Ibuprofen in Acute and Chronic Models of Pain

Long-Lasting, Antinociceptive Effects of pH-Sensitive Niosomes Loaded with Ibuprofen in Acute and Chronic Models of Pain

Chenopodium ambrosioides L. Reduces Synovial Inflammation and Pain in Experimental Osteoarthritis

Addition of angled rungs to the horizontal ladder walking task for more sensitive probing of sensorimotor changes

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