叶酸-白蛋白包覆阳离子纳米脂质载体的制备及体内外评价

发布时间：2018-06-29 12:35

本文选题：叶酸 + 白蛋白　；参考：《中国药科大学学报》2015年01期

【摘要】：合成叶酸-白蛋白靶向材料,通过薄膜分散法制备白蛋白包覆阳离子纳米脂质载体(BSA-c NLCs)和叶酸-白蛋白包覆阳离子纳米脂质载体(FA-BSA-c NLCs)。对两者粒径、外观、包封率、载药量、体外细胞摄取、血液和肿瘤药代动力学和药效学进行考察。结果表明,BSA-c NLCs和FA-BSA-c NLCs粒径分别为81.4和79.8 nm,Zeta电位分别为+5.12和+3.74 m V,透射电镜照片表明两者均为圆整的类球形结构。两者紫杉醇包封率都大于97%,载药量在3.7%左右。体外细胞试验证实,高表达叶酸受体的SKOV3对FA-BSA-c NLCs的摄取显著高于BSA-c NLCs,说明FA-BSA-c NLCs对SKOV3具有明显的靶向性。血液及肿瘤药代动力学显示两者体内药代动力学行为无明显差异,证实表面修饰叶酸不影响制剂的体内行为。药效学试验显示,BSA-c NLCs和FA-BSA-c NLCs抑瘤率分别为72.08%和80.75%。可见FA-BSA-c NLCs在一定程度上提高了体内外抗肿瘤疗效,在肿瘤的治疗中具有较好应用前景。
[Abstract]:Folic acid-albumin targeting materials were synthesized. Albumin coated cationic lipid carriers (BSA-c NLCs) and folic acid-albumin coated cationic nano-lipids (FA-BSA-c NLCs) were prepared by thin-film dispersion method. The particle size, appearance, encapsulation efficiency, drug loading, cell uptake in vitro, pharmacokinetics and pharmacodynamics of blood and tumor were investigated. The results show that the particle sizes of BSA-c NLCs and FA-BSA-c NLCs are 81.4 and 79.8 nm 路min ~ (-1), respectively, and the Zeta potentials are 5.12 and 3.74 MV, respectively. The entrapment efficiency of paclitaxel was higher than 97%, and the drug loading was about 3.7%. The uptake of FA-BSA-c NLCs by SKOV3 with high expression of folic acid receptor was significantly higher than that of BSA-c NLCs in vitro, which indicated that FA-BSA-c NLCs had obvious targeting to SKOV3. The pharmacokinetics of blood and tumor showed no significant difference between the two groups. It was proved that the surface modified folic acid did not affect the in vivo behavior of the preparation. The inhibition rates of BSA-c NLCs and FA-BSA-c NLCs were 72.08% and 80.75%, respectively. It can be seen that FA-BSA-c NLCs can improve the antitumor effect in vivo and in vitro to some extent, and have a good application prospect in the treatment of tumor.
【作者单位】：烟台大学药学院;南京绿叶思科药业有限公司;平邑县中医医院;中国药科大学药学院;
【分类号】：R943

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