Vera-López Karin J, Aranzamendi-Zenteno María, Davila-Del-Carpio Gonzalo, Nieto-Montesinos Rita
Facultad de Ciencias Farmacéuticas, Bioquímicas y Biotecnológicas, Universidad Católica de Santa María, Urb. San José s/n, Umacollo, Arequipa 04000, Peru.
Neurol Int. 2025 Mar 3;17(3):38. doi: 10.3390/neurolint17030038.
BACKGROUND/OBJECTIVES: Epilepsy is one of the most common chronic neurological disorders, characterized by alterations in neuronal electrical activity that result in recurrent seizures and involuntary body movements. Anticonvulsants are the primary treatment for this condition, helping patients improve their quality of life. However, the development of new drugs with fewer side effects and greater economic accessibility remains a key focus in nanomedicine. Macamides, secondary metabolites derived from Maca (), represent a promising class of novel drugs with diverse therapeutic applications, particularly in the treatment of neurological disorders.
In this study, we optimized the potential of the macamide N-3-methoxybenzyl-linoleamide (3-MBL) as an anticonvulsant agent through its encapsulation in PEGylated liposomes conjugated with OX26 F(ab') fragments.
These immunoliposomes exhibited a size of 120.52 ± 9.46 nm and a zeta potential of -8.57 ± 0.80 mV. Furthermore, in vivo tests using a pilocarpine-induced status epilepticus model revealed that the immunoliposomes provided greater efficacy against epileptic seizures compared to the free form of N-3-methoxybenzyl-linoleamide at the same dose. Notably, the observed anticonvulsant effect was comparable to that of carbamazepine, a traditional FDA-approved antiepileptic drug.
This pioneering work employs liposomal nanocarriers to deliver macamides to the brain, aiming to set a new standard for the use of modified liposomes in anticonvulsant epilepsy treatment.
背景/目的:癫痫是最常见的慢性神经系统疾病之一,其特征是神经元电活动改变,导致反复发作的癫痫和不自主的身体运动。抗惊厥药物是这种疾病的主要治疗方法,有助于患者提高生活质量。然而,开发副作用更少、经济可及性更高的新药仍然是纳米医学的一个关键重点。玛咖酰胺是从玛咖中提取的次生代谢产物,是一类具有多种治疗应用前景的新型药物,尤其在治疗神经系统疾病方面。
在本研究中,我们通过将玛咖酰胺N-3-甲氧基苄基亚油酸酰胺(3-MBL)包裹于与OX26 F(ab')片段偶联的聚乙二醇化脂质体中,优化其作为抗惊厥药物的潜力。
这些免疫脂质体的大小为120.52±9.46纳米,zeta电位为-8.57±0.80毫伏。此外,使用毛果芸香碱诱导的癫痫持续状态模型进行的体内试验表明,与相同剂量的游离N-3-甲氧基苄基亚油酸酰胺相比,免疫脂质体对癫痫发作具有更高的疗效。值得注意的是,观察到的抗惊厥效果与传统的美国食品药品监督管理局(FDA)批准的抗癫痫药物卡马西平相当。
这项开创性的工作采用脂质体纳米载体将玛咖酰胺递送至大脑,旨在为修饰脂质体在抗惊厥癫痫治疗中的应用树立新的标准。