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以壳聚糖为载体,溶剂扩散法制备乙酰半胱氨酸纳米粒,制得的纳米粒呈大小均匀的球形,平均粒径(163.0±12.8)nm,包封率(81.2+1.2)%,载药量(28.9+0.4)%。用HPLC法测定了小鼠单剂量尾静脉注射乙酰半胱氨酸纳米粒或其注射液后各脏器(心、肝、脾、肺和肾)和血浆中的药物浓度,并以相对摄取量和靶向效率评价纳米粒的靶向性。结果表明,纳米粒明显改变了药物在小鼠体内的生物分布。与注射液组相比,纳米粒组在肝组织中乙酰半胱氨酸浓度明显提高,血浆、心和肾组织中的药物浓度显著降低。
Acetylcysteine nanoparticles were prepared by solvent diffusion method with chitosan as carrier. The prepared nanoparticles were spherical with the average size of (163.0 ± 12.8) nm, entrapment efficiency (81.2 + 1.2)%, Drug loading (28.9 + 0.4)%. The concentration of drug in each organ (heart, liver, spleen, lung and kidney) and plasma after single dose intravenous injection of acetylcysteine nanoparticles or its injection was determined by HPLC. The relative concentration And targeting efficiency to evaluate the targeting of nanoparticles. The results showed that the nanoparticles significantly changed the biodistribution of the drug in mice. Compared with the injection group, the concentration of acetylcysteine in the liver tissue of the nanoparticle group was significantly increased, and the concentration of the drug in the plasma, heart and kidney tissues was significantly decreased.