Topical pregabalin and diclofenac for the treatment of neuropathic orofacial pain in rats

Plaza-Villegas, Francisco; Heir, Gary M.; Markman, Stanley; Khan, Junad; Noma, Noboru; Benoliel, Rafael; Patel, J. M.; Eliav, Eli

doi:10.1016/j.oooo.2012.05.002

Cited by 23 publications

(16 citation statements)

References 23 publications

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“…Pregabalin has also been shown to attenuate mechanical allodynia in the tibial neuroma transposition (TNT) model [14]. The topical application of pregabalin (10 %) for 4 consecutive days after 7 days of surgical nerve injury is reported to reduce neuropathic orofacial pain intensity in an infraorbital nerve injury model in rats [15]. Administration of pregabalin (2 mg/kg, i.v.)…”

Section: Evidences For Its Pain Attenuating Effects From Preclinical mentioning

confidence: 99%

Pregabalin in Neuropathic Pain: Evidences and Possible Mechanisms

Verma¹,

Singh²,

Jaggi

2014

161

119

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Pregabalin is an antagonist of voltage gated Ca2+ channels and specifically binds to alpha-2-delta subunit to produce antiepileptic and analgesic actions. It successfully alleviates the symptoms of various types of neuropathic pain and presents itself as a first line therapeutic agent with remarkable safety and efficacy. Preclinical studies in various animal models of neuropathic pain have shown its effectiveness in treating the symptoms like allodynia and hyperalgesia. Clinical studies in different age groups and in different types of neuropathic pain (peripheral diabetic neuropathy, fibromyalgia, post-herpetic neuralgia, cancer chemotherapy-induced neuropathic pain) have projected it as the most effective agent either as monotherapy or in combined regimens in terms of cost effectiveness, tolerability and overall improvement in neuropathic pain states. Preclinical studies employing pregabalin in different neuropathic pain models have explored various molecular targets and the signaling systems including Ca2+ channel-mediated neurotransmitter release, activation of excitatory amino acid transporters (EAATs), potassium channels and inhibition of pathways involving inflammatory mediators. The present review summarizes the important aspects of pregabalin as analgesic in preclinical and clinical studies as well as focuses on the possible mechanisms.

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Section: Evidences For Its Pain Attenuating Effects From Preclinical mentioning

confidence: 99%

Pregabalin in Neuropathic Pain: Evidences and Possible Mechanisms

Verma¹,

Singh²,

Jaggi

2014

161

119

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“…In the present work; inclusion of PG in niosomal hydrogel preparation is of great importance as many reported PG formulations including PG conventional topical gel 15 , PG patch 16 and PG solution 17 were not enhanced with such innovative nano-vesicles, resulting in the lacking of their ability to deliver PG in controlled pattern with good skin permeation profiles to achieve the bioavailability augmentation.…”

mentioning

confidence: 99%

DOE Optimization of Nano-based Carrier of Pregabalin as Hydrogel: New Therapeutic & Chemometric Approaches for Controlled Drug Delivery Systems

Arafa

Ayoub

2017

Sci Rep

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Niosomes entrapping pregabalin (PG) were prepared using span 60 and cholesterol in different molar ratios by hydration method, the remaining PG from the hydrating solution was separated from vesicles by freeze centrifugation. Optimization of nano-based carrier of pregabalin (PG) was achieved. Quality by Design strategy was successfully employed to obtain PG-loaded niosomes with the desired properties. The optimal particle size, drug release and entrapment efficiency were attained by Minitab® program using design of experiment (DOE) that predicted the best parameters by investigating the combined effect of different factors simultaneously. Pareto chart was used in the screening step to exclude the insignificant variables while response surface methodology (RSM) was used in the optimization step to study the significant factors. Best formula was selected to prepare topical hydrogels loaded with niosomal PG using HPMC and Carbopol 934. It was verified, by means of mechanical and rheological tests, that addition of the vesicles to the gel matrix affected significantly gel network. In vitro release and ex vivo permeation experiments were carried out. Delivery of PG molecules followed a Higuchi, non Fickian diffusion. The present work will be of interest for pharmaceutical industry as a controlled transdermal alternative to the conventional oral route.

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“…With regards to use in radiculopathy, while animal models of injury have been promising ( 40 , 41 ) our literature review revealed no studies examining the use of Diclofenac or Ibuprofen (topical or oral) for the treatment of radicular pain.…”

Section: Discussionmentioning

confidence: 98%

Novel Treatment of Radicular Pain With a Multi-Mechanistic Combination Topical Agent: A Case Series and Literature Review

et al. 2016

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IntroductionPharmacologic treatment of radicular pain with oral medications is limited by adverse effects and concern for dependence. While topical formulations have been explored in pain research, there is no published literature evaluating the efficacy in radicular pain. We present the first three cases of radicular pain successfully treated with a topical formulation of diclofenac, ibuprofen, baclofen, cyclobenzaprine, bupivacaine, gabapentin, and pentoxifylline (T7).Case PresentationCase series evaluating T7 for treatment of radicular pain in a single, outpatient pain center. Pain was rated on the numeric rating scale (NRS) on initial evaluation and follow up after a trial of T7. One to two grams of T7 was applied to the affected area 3 - 4 times daily in addition to the patient’s baseline pharmacologic management. Three patients with median age of 50 (range, 39 to 65) and diagnosis of cervical and/or lumbosacral radicular pain participated. Two of the three had chronic radicular pain despite use of analgesic agents, spinal injections and failed spinal surgery syndrome. Each reported subjective improvement in radicular pain, function and sleep. There was an average decrease in NRS score consistent with 30% - 40% global improvement in symptoms, clinically significant based on the minimal clinically important difference for radicular pain. T7 was well tolerated without adverse reactions. Surgery was prevented or delayed in all cases.ConclusionsThis is the first report of the successful treatment of radicular pain with a topical agent. This highlights the need for randomized, prospective study of both single and compounded topical agents for treatment of radicular pain.

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Topical pregabalin and diclofenac for the treatment of neuropathic orofacial pain in rats

Cited by 23 publications

References 23 publications

Pregabalin in Neuropathic Pain: Evidences and Possible Mechanisms

Pregabalin in Neuropathic Pain: Evidences and Possible Mechanisms

DOE Optimization of Nano-based Carrier of Pregabalin as Hydrogel: New Therapeutic & Chemometric Approaches for Controlled Drug Delivery Systems

Novel Treatment of Radicular Pain With a Multi-Mechanistic Combination Topical Agent: A Case Series and Literature Review

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