Therapeutic effects of fluorescent gabapentin carbon quantum dots on pentylenetetrazol-induced seizures in rats.

IF 3.9 4区 医学 Q1 PHARMACOLOGY & PHARMACY
Ayşe Özçetin, Hüseyin Koyuncu, Gamze Camlik, Burcu Çevreli, Zeynep Kocaizmirli, Ismail Tuncer Degim, Tayfun Uzbay
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引用次数: 0

Abstract

We aimed to synthesise carbon quantum dots (CQDs) from the active molecule gabapentin (GBP) and to evaluate their effects on pentylenetetrazol (PTZ)-induced seizures in rats. Gabapentin CQDs (GBPCQDs) were synthesised using a rapid, one-pot microwave-assisted method and characterised by particle size, polydispersity index, zeta potential and fluorescence properties. Adult male Wistar rats received GBP or GBPCQDs (15, 30, 60 or 120 mg/kg, intraperitoneally) 30 min before PTZ administration (50 mg/kg). Seizure onset times and severity were assessed, and locomotor activity was evaluated at the most effective doses. While GBP did not significantly affect seizure onset, GBPCQDs at 15 mg/kg significantly prolonged the onset time of PTZ-induced seizures. Both GBP and GBPCQDs significantly reduced seizure severity at all tested doses, however, GBPCQDs at 60 and 120 mg/kg were more effective than the corresponding doses of GBP. Neither treatment produced significant changes in locomotor activity. Fluorescence imaging demonstrated the presence of GBPCQDs in the prefrontal cortex, striatum and hippocampus, with the highest fluorescence intensity observed in the prefrontal cortex. These findings indicate that GBPCQDs may provide therapeutic advantages over conventional GBP and represent a promising fluorescent nanocarrier for brain-targeted drug delivery in epilepsy.

加巴喷丁荧光碳量子点对戊四唑致大鼠癫痫发作的治疗作用。
以活性分子加巴喷丁(GBP)为原料合成碳量子点(CQDs),并研究其对戊四氮唑(PTZ)致癫痫发作的影响。采用一锅自底向上快速合成加巴喷丁CQDs (GBPCQDs)。粒度,多分散性指数和zeta电位测量进行表征。还使用荧光分光光度计评估了化学降解。以成年雄性Wistar大鼠(250 ~ 320 g)为研究对象。在PTZ (50 mg/kg, ip)治疗前30分钟,大鼠腹腔注射GBP和GBPCQDs(15、30、60和120 mg/kg)、生理盐水或对照物。评估癫痫发作的时间和严重程度。运动活动评估治疗的有效剂量。在额叶皮质、纹状体和海马体中也评估了荧光。GBPCQDs (15 mg/kg)可显著延长癫痫发作时间(p = 0.045),而GBP对该参数无明显影响。GBP和GBPCQDs在所有剂量下都显著降低了癫痫发作的严重程度(ps)
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来源期刊
CiteScore
9.10
自引率
0.00%
发文量
165
审稿时长
2 months
期刊介绍: Journal of Drug Targeting publishes papers and reviews on all aspects of drug delivery and targeting for molecular and macromolecular drugs including the design and characterization of carrier systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo applications of these drugs. Papers are not restricted to drugs delivered by way of a carrier, but also include studies on molecular and macromolecular drugs that are designed to target specific cellular or extra-cellular molecules. As such the journal publishes results on the activity, delivery and targeting of therapeutic peptides/proteins and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids (e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes), as well as aptamers, mononucleotides and monoclonal antibodies and their conjugates. The diagnostic application of targeting technologies as well as targeted delivery of diagnostic and imaging agents also fall within the scope of the journal. In addition, papers are sought on self-regulating systems, systems responsive to their environment and to external stimuli and those that can produce programmed, pulsed and otherwise complex delivery patterns.
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