Maysinger D, Garofalo L, Jalsenjak I, Cuello A C
Department of Pharmacology and Therapeutics, McGill University, Montreal, Que., Canada.
Brain Res. 1989 Sep 4;496(1-2):165-72. doi: 10.1016/0006-8993(89)91062-7.
The preparation, physical characterization and effects of microcapsules containing the monosialoganglioside GM1 in an in vivo rat model are described herewith. Several preparations of microcapsules were obtained differing in physical and chemical properties. Human serum albumin (HSA) microcapsules with or without GM1 are spherical in shape, have a consistent particle size (8-10 microns in diameter) and are devoid of large pores. In agreement with our previous work, we now provide further evidence that GM1 can prevent shrinkage and the decrease of choline acetyltransferase activity in the nucleus basalis magnocellularis (NBM) of the rat following a unilateral cortical lesion. In the present study we examined the effect of microencapsulated GM1 in this in vivo rat model. Local application of HSA-microencapsulated GM1 (in doses comparable to those obtained by i.c.v. administration) onto the surface of the lesioned cortex prevents both the biochemical and morphological degenerative changes in the NBM of rats with unilateral devascularizing cortical lesions. The results from these studies show that microencapsulated GM1 can be applied successfully and a prolonged controlled release of this drug obtained, thus avoiding surgical implantation of a cannula.
本文描述了含单唾液酸神经节苷脂GM1的微胶囊在大鼠体内模型中的制备、物理特性及作用。获得了几种物理和化学性质不同的微胶囊制剂。含或不含GM1的人血清白蛋白(HSA)微胶囊呈球形,粒径一致(直径8-10微米),且无大孔。与我们之前的工作一致,我们现在提供进一步证据表明,GM1可防止大鼠单侧皮质损伤后基底大细胞核(NBM)的萎缩和胆碱乙酰转移酶活性的降低。在本研究中,我们在该大鼠体内模型中检测了微囊化GM1的作用。将HSA微囊化GM1(剂量与通过脑室内给药获得的剂量相当)局部应用于损伤皮质表面,可防止单侧去血管化皮质损伤大鼠NBM中的生化和形态学退行性变化。这些研究结果表明,微囊化GM1可以成功应用,并可实现该药物的长期控释,从而避免套管的手术植入。