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采用加热超声法制备了载甲氨蝶呤的纳米结构脂质载体(NLC),并考察其局部药物递送能力,以期提高甲氨蝶呤对皮肤相关疾病的疗效、减轻系统不良反应。采用生物相容的脂质材料——鲸蜡和Miglyol 812为载体,制得了外观呈球形、粒径约450 nm的载药NLC。该制品的体外释药行为符合Peppas-Korsmeyer释放动力学模型,10 h能释出50%的药量;并且稳定性达到3个月以上。与游离药物相比,该载药NLC对成纤维细胞和人角质形成细胞的毒性较小。体外
Nanostructured lipid carriers (NLC) containing methotrexate were prepared by heated ultrasound and their local drug delivery ability was investigated in order to improve the curative effect of methotrexate on skin-related diseases and reduce systemic adverse reactions. The biocompatible lipid material-spermaceti and Miglyol 812 was used as carrier to prepare drug-loaded NLC with a spherical shape and particle size of about 450 nm. The in vitro drug release behavior of the product was in accordance with the Peppas-Korsmeyer release kinetic model, and the drug release was 50% after 10 h. The stability of the product reached more than 3 months. Compared to free drug, this drug-loaded NLC is less toxic to fibroblasts and human keratinocytes. in vitro