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百里酚纳米聚合物的合成及其对大鼠吗啡戒断综合征的影响:与可乐定的比较

Thymol Nanopolymer Synthesis and Its Effects on Morphine Withdrawal Syndrome in Comparison With Clonidine in Rats.

作者信息

Moayeri Ardeshir, Mehdizadeh Reza, Karimi Elahe, Aidy Ali, Ghaneialvar Hori, Abbasi Naser

机构信息

Department of Anatomy, Medical School, Ilam University of Medical Sciences, Ilam, Iran.

Biotechnology and Medicinal Plants Research Center, Ilam University of Medical Sciences, Ilam, Iran.

出版信息

Front Behav Neurosci. 2022 Jun 29;16:843951. doi: 10.3389/fnbeh.2022.843951. eCollection 2022.

Abstract

The drug delivery system is valuable in the treatment of the disease. A nanopolymer as a thymol and release system was synthesized and its effects on morphine withdrawal syndrome in comparison with clonidine in rats were studied. The nanopolymer was characterized by different methods, namely, IR, HNMR, CNMR, GPC, DLS, and AFM. Thymol in extract was assessed. The loading and release rate of thymol and extract on the nanopolymer were evaluated by HPLC. The median lethal dose (LD) of the extract, thymol, extract nanopolymer, and thymol nanopolymer was studied. The frequency of jumping, rearing, and teeth chattering in naloxone-induced morphine withdrawal syndrome was studied. Synthesized nanopolymer was desirable as a carrier for the drug. The loaded amount of extract and thymol on nanopolymer was estimated 55 ± 3.2% and 48 ± 2.6% and the drug released was 71 and 68%, respectively. LD of the extract, thymol, extract nanopolymer, and thymol nanopolymer was 975, 580, 1,250, and 650 mg/kg, respectively. This study showed that thymol nanopolymer was more effective than clonidine to reduce the frequency of morphine withdrawal symptoms. Our results suggest that extract, thymol, extract nanopolymer, and thymol nanopolymer are mighty in reducing the narcotic withdrawal signs. The mechanism of action and therapeutic potential is maybe similar to clonidine.

摘要

药物递送系统在该疾病的治疗中具有重要价值。合成了一种作为百里香酚释放系统的纳米聚合物,并研究了其与可乐定相比对大鼠吗啡戒断综合征的影响。通过红外光谱(IR)、核磁共振氢谱(HNMR)、核磁共振碳谱(CNMR)、凝胶渗透色谱(GPC)、动态光散射(DLS)和原子力显微镜(AFM)等不同方法对纳米聚合物进行了表征。评估了提取物中的百里香酚。通过高效液相色谱(HPLC)评估了百里香酚和提取物在纳米聚合物上的负载和释放速率。研究了提取物、百里香酚、提取物纳米聚合物和百里香酚纳米聚合物的半数致死剂量(LD)。研究了纳洛酮诱导的吗啡戒断综合征中跳跃、竖毛和牙齿打颤的频率。合成的纳米聚合物作为药物载体是理想的。纳米聚合物上提取物和百里香酚的负载量估计分别为55±3.2%和48±2.6%,药物释放率分别为71%和68%。提取物、百里香酚、提取物纳米聚合物和百里香酚纳米聚合物的LD分别为975、580、1250和650mg/kg。本研究表明,百里香酚纳米聚合物在降低吗啡戒断症状频率方面比可乐定更有效。我们的结果表明,提取物、百里香酚、提取物纳米聚合物和百里香酚纳米聚合物在减轻麻醉剂戒断症状方面作用强大。其作用机制和治疗潜力可能与可乐定相似。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ff43/9277302/dce542a0bc9e/fnbeh-16-843951-g001.jpg

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