Enhanced healing efficacy of an optimized gabapentin-melittin nanoconjugate gel-loaded formulation in excised wounds of diabetic rats

Asfour, Hani Z.; Alhakamy, Nabil A.; Ahmed, Osama A. A.; Fahmy, Usama A.; Md, Shadab; El‐Moselhy, Mohamed A.; Rizg, Waleed Y.; Alghaith, Adel F.; Eid, Basma G.; Abdel-Naim, Ashraf B.

doi:10.1080/10717544.2022.2086943

Cited by 8 publications

(16 citation statements)

References 50 publications

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“…This was confirmed via histological examination which disclosed that COR-MEL nanoconjugate -treated rats showed almost complete healing on the 14th day with tissue regeneration and collagen deposition. The results are associated with earlier statements highlighting the synergistic wound-healing activity of MEL when combined with other drugs ( Alhakamy et al, 2021 , Asfour et al, 2022 , Eid et al, 2022 , Kim et al, 2021a , Maiden et al, 2019 ).…”

Section: Discussionsupporting

confidence: 88%

“…In addition, COR expedites the tissue remodeling process ( Kim et al, 2021a , Kim et al, 2021b ) Melittin (MEL), an aqueous–soluble cationic peptide, consisting of 26 amino acids with no disulfide bridges, is obtained from the crude venom of honeybees. MEL possesses pharmacological activities against inflammation, oxidative stress, and multi-resistance infection of bacteria in addition to pro-collagen activity ( Asfour et al, 2022 , Tiwari et al, 2022 ). Its anti-inflammatory activities are supported by several reports showing that MEL reduces the expression of cyclooxygenase (COX)-2 and phospholipase A2, as well as the levels of TNF-α, IL-1, IL-6, nitric oxide (NO), and ROS.…”

Section: Introductionmentioning

confidence: 99%

“…Its anti-inflammatory activities are supported by several reports showing that MEL reduces the expression of cyclooxygenase (COX)-2 and phospholipase A2, as well as the levels of TNF-α, IL-1, IL-6, nitric oxide (NO), and ROS. Further, it impedes the nuclear factor kappa B (NF-κβ) signaling ( Asfour et al, 2022 , Eid et al, 2022 , Tiwari et al, 2022 ). It was further revealed that based on the pharmacological advantages of MEL, it has been formulated as a topical preparation to facilitate wound healing ( Asfour et al, 2022 ).…”

Section: Introductionmentioning

confidence: 99%

“…Further, it impedes the nuclear factor kappa B (NF-κβ) signaling ( Asfour et al, 2022 , Eid et al, 2022 , Tiwari et al, 2022 ). It was further revealed that based on the pharmacological advantages of MEL, it has been formulated as a topical preparation to facilitate wound healing ( Asfour et al, 2022 ).…”

Section: Introductionmentioning

confidence: 99%

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Cordycepin- melittin nanoconjugate intensifies wound healing efficacy in diabetic rats

Shaik¹,

Alotaibi²,

Nasrullah³

et al. 2023

Saudi Pharmaceutical Journal

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Section: Discussionsupporting

confidence: 88%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Cordycepin- melittin nanoconjugate intensifies wound healing efficacy in diabetic rats

Shaik¹,

Alotaibi²,

Nasrullah³

et al. 2023

Saudi Pharmaceutical Journal

Self Cite

View full text Add to dashboard Cite

“…The particle size, zeta potential, and polydispersity of ACR-PCL-NE were monitored for 90 days (fresh, 30 days, 60 days, and 90 days). The ACR-PCL-NE was stored at 25 °C throughout the course (Romes et al., 2021 ; Asfour et al., 2022 ; Mushtaq et al., 2022 ).…”

Section: Methodsmentioning

confidence: 99%

Polycaprolactone based pharmaceutical nanoemulsion loaded with acriflavine: optimization andin vivoburn wound healing activity

et al. 2022

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Cutaneous burn wounds are a common and troublesome critical issue of public health. Over the last decade, many researchers have investigated the development of novel therapeutic modalities which are capable of fully regeneration and reinstatement of structure and function of the skin with no or limited scar formation. Novel pharmaceutical carriers are offering a potential platform to deliver the drug effectively and to overcome the limitation associated with conventional wound dressings. The aim of this study was to investigate a pharmaceutical acriflavine-loaded polycaprolactone nanoemulsion (ACR-PCL-NE) for burn wound healing. Nanoemulsion was prepared by using the double emulsion solvent evaporation technique and it was subjected to thermodynamic stability testing, droplet size, polydispersity, zeta potential, pH, and surface morphology analysis. The in vivo study was performed to evaluate the efficacy of nanoemulsion using Sprague-Dawley rats as an animal model. The results of this study revealed that the optimized nanoemulsion was stable and had desirable physicochemical properties. The pH was about 4.02 at 25 °C and the particle size was found to be in the range of 302 ± 4.62 nm while the zeta potential was −7.8 ± 1.22 mV and the polydispersity index of 0.221 ± 0.017. The wound regeneration process was evaluated in vivo by different techniques, the formulation group (FG) showed high wound healing potential as compared to the standard group (SD) and control group (CG). These findings reveal that this nanoemulsion formulation can be used effectively for wound healing.

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Molecular Mechanisms and Therapeutic Potential of Gabapentin with a Focus on Topical Formulations to Treat Ocular Surface Diseases

Rusciano

2024

Preprint

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Gabapentin (GBP) was originally developed as a potential agonist for Gamma-Amino-Butyric-Acid (GABA) receptors, aiming to inhibit the activation of pain-signaling neurons. Contrary to initial expectations, it does not bind to GABA receptors. Instead, it exhibits several distinct pharmacological activities, including: (1) binding to the alpha-2-delta protein subunit of voltage-gated calcium channels in the central nervous system, thereby blocking the excitatory influx of calcium; (2) reducing the expression and phosphorylation of CaMKII via modulation of ERK1/2 phosphorylation; (3) inhibiting glutamate release and interfering with the activation of NMDA receptors; (4) enhancing GABA synthesis; (5) increasing cell-surface expression of δGABA_A receptors, contributing to its antinociceptive, anticonvulsant, and anxiolytic-like effects. Additionally, GBP displays (6) inhibition of NF-kB activation and subsequent production of inflammatory cytokines, and (7) stimulation of the purinergic adenosine A1 receptor, which supports its anti-inflammatory and wound-healing properties. Initially approved for treating seizures and postherpetic neuralgia, GBP is now broadly used for various conditions, including psychiatric disorders, acute and chronic neuropathic pain, and sleep disturbances. Recently, as an eye drop formulation, it has also been explored as a therapeutic option for ocular surface discomfort in conditions such as dry eye, neurotrophic keratitis, corneal ulcers, and neuropathic ocular pain. This review aims to summarize the evidence supporting the molecular effects of GBP, with a special emphasis on its applications in ocular surface diseases.

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Enhanced healing efficacy of an optimized gabapentin-melittin nanoconjugate gel-loaded formulation in excised wounds of diabetic rats

Cited by 8 publications

References 50 publications

Cordycepin- melittin nanoconjugate intensifies wound healing efficacy in diabetic rats

Cordycepin- melittin nanoconjugate intensifies wound healing efficacy in diabetic rats

Polycaprolactone based pharmaceutical nanoemulsion loaded with acriflavine: optimization andin vivoburn wound healing activity

Molecular Mechanisms and Therapeutic Potential of Gabapentin with a Focus on Topical Formulations to Treat Ocular Surface Diseases

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