Neuropsychopharmacology & Psychobiology Research Group, University of Cádiz, Spain; Centro de Investigación Biomédica en Red de Salud Mental (CIBERSAM), Instituto de Salud Carlos III, Madrid, Spain; Instituto de Investigación e Innovación en Ciencias Biomédicas de Cádiz, INiBICA, Edificio "Andrés Segovia", Cádiz, Spain.
Neuropsychopharmacology & Psychobiology Research Group, University of Cádiz, Spain.
Nanomedicine. 2017 Nov;13(8):2623-2632. doi: 10.1016/j.nano.2017.07.010. Epub 2017 Jul 26.
Neuropathic pain, resistant to opiates and other drugs, is a chronic/persistent state with a complex treatment and often poor efficacy. In this scenario, cannabinoids are increasingly regarded as a genuine alternative. In this paper, and in an experimental animal model of neuropathic pain, we studied the efficacy of three kinds of PLGA nanoparticles containing synthetic cannabinoid CB13: (i) plain nanoparticles (PLGA); (ii) particles coated with PEG chains (PLGA+PEG) and (iii) particles possessing hydrophilic surfaces obtained by covalently binding PEG chains (PLGA-PEG). The optimized formulation, CB13-PLGA-PEG, showed high drug loading (13%) and small size (<300nm) with a narrow distribution and controlled surface properties (near-neutral zeta potential and stable PEG corona). Animal nociceptive behavioral studies were conducted by paw pressure and acetone tests. Versus the free CB13, CB13-PLGA-PEG nanoparticles showed a very noticeable analgesic efficacy with the longest sustained pain-relieving effect, lasting up to eleven days after one oral dose.
神经病理性疼痛对阿片类药物和其他药物有耐药性，是一种慢性/持续性状态，治疗复杂，疗效往往不佳。在这种情况下，大麻素越来越被视为一种真正的替代药物。在本文中，我们在神经病理性疼痛的实验动物模型中研究了三种含有合成大麻素 CB13 的 PLGA 纳米粒子的疗效：（i）普通纳米粒子（PLGA）；（ii）涂有聚乙二醇链的粒子（PLGA+PEG）和（iii）通过共价结合聚乙二醇链获得亲水表面的粒子（PLGA-PEG）。优化的配方 CB13-PLGA-PEG 具有高载药量（13%）和小尺寸（<300nm），分布狭窄，表面性能可控（接近中性的 Zeta 电位和稳定的 PEG 冠）。通过爪压和丙酮试验进行动物疼痛行为研究。与游离 CB13 相比，CB13-PLGA-PEG 纳米粒子表现出非常显著的镇痛效果，其最长的持续止痛效果可持续长达 11 天，口服一次即可达到。
