Opiate‐Free Pain Therapy Using Carbamazepine‐Loaded Microparticles Provides Up to 2 Weeks of Pain Relief in a Neuropathic Pain Model

Dai, Haining; Tilley, Dana M.; Mercedes, Greici; Doherty, Chris; Gulati, Amitabh; Mehta, Neel; Khalil, Amer; Holzhaus, Katrin; Reynolds, Francis M.

doi:10.1111/papr.12705

Cited by 6 publications

(2 citation statements)

References 39 publications

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Section: Current Drug Delivery Systems For Local Anestheticsmentioning

confidence: 99%

“…Importantly, no toxicological or other side-effects were observed in behavioral and histochemical analyses. 55 Thus, microparticles continue to be a focus of research interest for the development of new DDSs for current anesthetics. Microneedles, representing arrays of micron-sized needles, serve as an effective carrier in DDSs due to their minimally invasive and self-administrable properties, especially for transdermal delivery of local anesthetics.…”

Section: Current Drug Delivery Systems For Local Anestheticsmentioning

confidence: 99%

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Recent Research Advances in Nano-Based Drug Delivery Systems for Local Anesthetics

Ma,

Pan,

Lai

et al. 2023

DDDT

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From a clinical perspective, local anesthetics have rather widespread application in regional blockade for surgery, postoperative analgesia, acute/chronic pain control, and even cancer treatments. However, a number of disadvantages are associated with traditional local anesthetic agents as well as routine drug delivery administration ways, such as neurotoxicity, short half-time, and non-sustained release, thereby limiting their application in clinical practice. Successful characterization of drug delivery systems (DDSs) for individual local anesthetic agents can support to achieve more efficient drug release and prolonged duration of action with reduced systemic toxicity. Different types of DDSs involving various carriers have been examined, including micromaterials, nanomaterials, and cyclodextrin. Among them, nanotechnology-based delivery approaches have significantly developed in the last decade due to the low systemic toxicity and the greater efficacy of non-conventional local anesthetics. Multiple nanosized materials, including polymeric, lipid (solid lipid nanoparticles, nanostructured lipid carriers, and nanoemulsions), metallic, inorganic non-metallic, and hybrid nanoparticles, offer a safe, localized, and long-acting solution for pain management and tumor therapy. This review provides a brief synopsis of different nano-based DDSs for local anesthetics with variable sizes and structural morphology, such as nanocapsules and nanospheres. Recent original research utilizing nanotechnology-based delivery systems is particularly discussed, and the progress and strengths of these DDSs are highlighted. A specific focus of this review is the comparison of various nano-based DDSs for local anesthetics, which can offer additional indications for their further improvement. All in all, nano-based DDSs with unique advantages provide a novel direction for the development of safer and more effective local anesthetic formulations.

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Section: Current Drug Delivery Systems For Local Anestheticsmentioning

confidence: 99%

Section: Current Drug Delivery Systems For Local Anestheticsmentioning

confidence: 99%

Recent Research Advances in Nano-Based Drug Delivery Systems for Local Anesthetics

Ma,

Pan,

Lai

et al. 2023

DDDT

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Synthesis and evaluation of anticonvulsant activities of 7‐phenyl‐4,5,6,7‐tetrahydrothieno[3,2‐b]pyridine derivatives

Wang

Liu

Wang

et al. 2019

Archiv der Pharmazie

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A series of 7‐phenyl‐4,5,6,7‐tetrahydrothieno[3,2‐b]pyridine derivatives containing triazole and other heterocycle substituents (methyltriazole, tetrazole, and triazolone) is described. Two experimental methods, maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ), were used to evaluate the anticonvulsant activity of the target compounds. Moreover, the neurotoxicity (NT) was tested using the Rotarod test. 5‐(4‐Chlorophenyl)‐4,5‐dihydrothieno[2,3‐e][1,2,4]triazolo[4,3‐a]pyridine (6c) showed the best anticonvulsant activity. In the MES and PTZ experiments, the 50% effective dose (ED50) values of compound 6c were 9.5 and 20.5 mg/kg, respectively. From the therapeutic index (PI) values, 6c (MES and PTZ with PI values of 48.0 and 22.2, respectively) showed better safety than the clinical drugs carbamazepine (MES with PI value of 6.4) and ethosuximide (PTZ with PI value of 3.2). The biological activities of the compounds were verified by using molecular docking studies. Compound 6c showed significant interactions with residues at the benzodiazepine‐binding site on gamma‐aminobutyric acid A (GABAA) receptors. The results of in vivo GABA estimation and bicuculline‐induced seizures showed that 6c may have an effect on the GABA system. The physicochemical and pharmacokinetic properties of the target compounds were predicted.

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Membrane Stabilizer Medications in the Treatment of Chronic Neuropathic Pain: a Comprehensive Review

Viswanath

Urits

Jones

et al. 2019

Curr Pain Headache Rep

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Opiate‐Free Pain Therapy Using Carbamazepine‐Loaded Microparticles Provides Up to 2 Weeks of Pain Relief in a Neuropathic Pain Model

Cited by 6 publications

References 39 publications

Recent Research Advances in Nano-Based Drug Delivery Systems for Local Anesthetics

Recent Research Advances in Nano-Based Drug Delivery Systems for Local Anesthetics

Synthesis and evaluation of anticonvulsant activities of 7‐phenyl‐4,5,6,7‐tetrahydrothieno[3,2‐b]pyridine derivatives

Membrane Stabilizer Medications in the Treatment of Chronic Neuropathic Pain: a Comprehensive Review

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