Enhanced Anti-Inflammatory Effects of Nanoencapsulated Diclofenac

Goh, Jun Zheng; Tang, S.N.; Zuraini, A.; Zakaria, Zuhaina; Kadir, Arifah Abdul; Chiong, Hoe Siong; Fauzee, M.S.O.; Hakim, Muhammad Nazrul

doi:10.1177/1721727x1301100328

Cited by 4 publications

(4 citation statements)

References 19 publications

(19 reference statements)

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“…Indeed, encapsulation with liposomes 29 or other materials [30][31][32] will significantly improve a drug's efficacy, and thus reduce its side effects by using lower doses. 33 Similarly to other NSAIDs, the usage of diclofenac is often associated with gastric mucosal erosion, ulceration, hemorrhage, epigastric pain, and platelet dysfunction owing to the inhibition of prostaglandin synthesis by cyclooxygenase enzyme (COX). 33 Conventionally prescribed diclofenac formulation has also been reported to be more commonly associated with hepatotoxicity, gastrointestinal toxicity, and renal toxicity, especially during prolonged administration.…”

Section: Discussionmentioning

confidence: 99%

“…33 Similarly to other NSAIDs, the usage of diclofenac is often associated with gastric mucosal erosion, ulceration, hemorrhage, epigastric pain, and platelet dysfunction owing to the inhibition of prostaglandin synthesis by cyclooxygenase enzyme (COX). 33 Conventionally prescribed diclofenac formulation has also been reported to be more commonly associated with hepatotoxicity, gastrointestinal toxicity, and renal toxicity, especially during prolonged administration. [34][35][36] Inflammatory pain involved complex mechanisms that, in general, are defined as a combination of spontaneous pain and hyperalgesia.…”

Section: Discussionmentioning

confidence: 99%

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

Goh

Tang

Chiong

et al. 2014

IJN

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Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, antinociceptive, and antipyretic activities. Liposomes have been shown to improve the therapeutic efficacy of encapsulated drugs. The present study was conducted to compare the antinociceptive properties between liposome-encapsulated and free-form diclofenac in vivo via different nociceptive assay models. Liposome-encapsulated diclofenac was prepared using the commercialized proliposome method. Antinociceptive effects of liposome-encapsulated and free-form diclofenac were evaluated using formalin test, acetic acid-induced abdominal writhing test, Randall–Selitto paw pressure test, and plantar test. The results of the writhing test showed a significant reduction of abdominal constriction in all treatment groups in a dose-dependent manner. The 20 mg/kg liposome-encapsulated diclofenac demonstrated the highest antinociceptive effect at 78.97% compared with 55.89% in the free-form group at equivalent dosage. Both liposome-encapsulated and free-form diclofenac produced significant results in the late phase of formalin assay at a dose of 20 mg/kg, with antinociception percentages of 78.84% and 60.71%, respectively. Significant results of antinociception were also observed in both hyperalgesia assays. For Randall–Sellito assay, the highest antinociception effect of 71.38% was achieved with 20 mg/kg liposome-encapsulated diclofenac, while the lowest antinociceptive effect of 17.32% was recorded with 0 mg/kg liposome formulation, whereas in the plantar test, the highest antinociceptive effect was achieved at 56.7% with 20 mg/kg liposome-encapsulated diclofenac, and the lowest effect was shown with 0 mg/kg liposome formulation of 8.89%. The present study suggests that liposome-encapsulated diclofenac exhibits higher antinociceptive efficacy in a dose-dependent manner in comparison with free-form diclofenac.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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

Goh

Tang

Chiong

et al. 2014

IJN

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“…In fact, some studies showed that NSAID-loaded vesicles have better performance in terms of prolonged drug release [ 38 ] and improved therapeutic effects [ 39 ] compared with the free form of the same compound. Considering that niosomes are a very promising system to administer compounds of different features topically or orally [ 40 , 41 , 42 ], we evaluated the capability of niosomes to increase antinociceptive effects of Ibuprofen also in terms of lasting effects after s.c injection. Writhing and capsaicin tests are screening assays commonly used to study peripheral and central antinociceptive activity.…”

Section: Discussionmentioning

confidence: 99%

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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“…*p < 0.0001 when compared with Dic-Gel implying non-inflammatory pain. In contrast, the late phase reflects inflammatory pain [50]. Terpenes are lipophilic compounds that can influence intercellular lipids and the non-polar penetration pathway [51].…”

Section: Formalin Testmentioning

confidence: 99%

Development of a novel nanoemulgel formulation containing cumin essential oil as skin permeation enhancer

Morteza‐Semnani

Saeedi

Âkbari

et al. 2021

Drug Deliv. and Transl. Res.

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Essential oils have been proposed as promising non-toxic transdermal permeation enhancers. Their use is limited because of their low water solubility. The use of nanotechnology-based strategies is one of the ways to overcome this limitation. This study aimed to explore the transdermal permeation enhancing capability of cumin essential oil in nanoemulgel systems containing diclofenac sodium. Cumin essential oil nanoemulsion was produced by high-pressure homogenization technique. The formulation was optimized by changing HLB values in a range of 9.65–16.7 using different surfactant mixtures, namely, Tween 20, Tween 80, and Span 80. Preparations were characterized by polydispersity index, droplet size, and zeta potential. Nanoemulsion with concentrations of 2 and 4% essential oil was incorporated into 0.75% Carbopol gel matrix to make nanoemulgel formulation, and its permeation enhancing effect was performed through Franz diffusion cells. Antinociceptive activities of the formulations were measured in thermal (tail-flick) and chemical (formalin) models of nociception in mice. Characterization exhibited that at HLB value of 9.65, the smallest particle size (82.20 ± 5.82 nm) was formed. By increasing the essential oil percentage in the nanoemulgel from 1 to 2%, the permeation of diclofenac increased from 28.39 ± 1.23 to 34.75 ± 1.07 µg/cm2 at 24 h. The value of permeation from the simple gel (21.18 ± 2.51 µg/cm2) and the marketed product (22.97 ± 1.92 µg/cm2) was lower than the formulations containing essential oil. Nanoemulgel of diclofenac containing essential oil showed stronger antinociceptive effects in formalin and tail-flick tests than simple diclofenac gel and marketed formulation. In conclusion, the study proved that nanoemulgel formulation containing cumin essential oil could be considered as a promising skin enhancer to enhance the therapeutic effect of drugs. Graphical abstract

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Enhanced Anti-Inflammatory Effects of Nanoencapsulated Diclofenac

Cited by 4 publications

References 19 publications

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

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

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

Development of a novel nanoemulgel formulation containing cumin essential oil as skin permeation enhancer

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