Department of Pharmacology, Faculty of Medicine, "Grigore T. Popa" University of Medicine and Pharmacy, 700115 Iasi, Romania.
Department of Pharmacology, Faculty of Pharmacy, University of Medicine and Pharmacy, 200349 Craiova, Romania.
Medicina (Kaunas). 2021 Feb 4;57(2):138. doi: 10.3390/medicina57020138.
: The selective kappa opioid receptor agonist U50,488 was reported to have analgesic, cough suppressant, diuretic and other beneficial properties. The aim of our study was to analyze the effects of some original chitosan-coated liposomes entrapping U50,488 in somatic and visceral nociceptive sensitivity in mice. : The influence on the somatic pain was assessed using a tail flick test by counting the tail reactivity to thermal noxious stimulation. The nociceptive visceral estimation was performed using the writhing test in order to evaluate the behavioral manifestations occurring as a reaction to the chemical noxious peritoneal irritation with 0.6% acetic acid (10 mL/kbw). The animals were treated orally, at the same time, with a single dose of: distilled water 0.1 mL/10 gbw; 50 mg/kbw U50,488; 50 mg/kbw U50,488 entrapped in chitosan-coated liposomes, according to the group they were randomly assigned. : The use of chitosan-coated liposomesas carriers for U50,488 induced antinociceptive effects that began to manifest after 2 h, andwere prolonged but with a lower intensity than those caused by the free selective kappa opioid in both tests. : In this experimental model, the oral administration of nanovesicles containing the selective kappa opioid agonist U50,488 determined a prolonged analgesic outcome in the tail flick test, as well as in the writhing test.
: 选择性 κ 阿片受体激动剂 U50488 具有镇痛、镇咳、利尿等有益特性。本研究旨在分析一些原始壳聚糖包被的脂质体包封 U50488 对躯体和内脏伤害感受敏感性的影响。 : 通过记录对热伤害性刺激的尾巴反应来评估对躯体疼痛的影响,使用尾巴闪烁试验进行评估。通过扭体试验评估内脏疼痛,以评估对 0.6%乙酸(10 mL/kbw)化学性腹膜刺激的行为表现。动物以口服方式,同时给予以下剂量之一:0.1 mL/10 gbw 的蒸馏水;50 mg/kbw U50488;50 mg/kbw U50488 包封在壳聚糖包被的脂质体中,根据它们被随机分配的组。 : 壳聚糖包被的脂质体作为 U50488 的载体,诱导的镇痛作用在 2 小时后开始显现,并在两种试验中均延长,但强度低于游离选择性 κ 阿片受体。 : 在这个实验模型中,口服含有选择性 κ 阿片受体激动剂 U50488 的纳米囊泡,在尾巴闪烁试验和扭体试验中均导致镇痛作用延长。