以PLGA为载体,采用复乳-溶剂挥发法制备神经毒素(1)纳米粒,考察其形态、粒径、ζ电位、包封率和载药量。并以大鼠为动物模型,评价1纳米粒溶液肌注及鼻腔给药和1溶液肌注的药动学行为。与1溶液相比,1纳米粒肌注能缩短达峰时间,升高AUC值,延长体循环时间。1纳米粒经鼻腔给药,效果优于肌注。
Neurotoxin- I (1) nanoparticles were prepared by a (water-in-oil)-in water emulsion-solvent evaporation method with poly (lactic-co-glycolic acid) (PLGA) as carrier material. The shape, particle size, ζ potential, encapsulation efficiency and drug loading of the products were investigated. The pharmacokinetics in rats of 1 nanoparticles administrated by intramuscular injection and intranasal administration and 1 solution administrated by intramuscular injection were investigated, respectively. Compared with the pharmacokinetic parameters of 1 solution, the tmax of 1 nanoparticles by intramuscular injection was shortened, AUC value was increased and MRT was prolonged significantly. The therapeutic effect of 1 nanoparticles by intranasal administrated was more satisfactory than that of intramuscular injection.