粒径差异化的纳米脂质载体的制备和表征

发布时间：2018-07-06 12:46

  本文选题：香豆素- + 纳米脂质载体　； 参考：《中国药科大学学报》2015年04期

【摘要】：利用特色化的中心复合设计,以香豆素-6为模型药物,通过控制特定的因素和指标,制备粒径不同而其他性质相同的纳米脂质载体(NLCs),并对其形态、Zeta电位和包封率等理化性质进行研究。通过体外稳定性实验考察NLCs在K-R液和PBS缓冲液中的稳定性,同时以透析法研究制剂的体外释药行为特性。采用MTT法研究空白NLCs和载药NLCs的细胞毒性,活体成像技术考察NLCs在小鼠胃肠道中的滞留时间。结果显示:制备所得的粒径分别为100,200及300 nm的香豆素-6纳米脂质载体,分散性良好,在K-R液和PBS缓冲液中可以稳定存在,并且体外24 h香豆素-6的累积释放量均不超过总量的7%。MTT实验表明:空白NLCs和载药NLCs对Caco-2毒性较小。小鼠肠内滞留试验显示:NLCs在灌胃给药6 h后仍然能够在胃肠道中检测到。因此,制备得到的不同粒径NLCs可以作为模型制剂,用于细胞水平和动物水平上研究NLCs粒径对口服吸收的影响。
[Abstract]:Using a specialised central composite design, using coumarin -6 as a model drug, by controlling specific factors and indicators, Nano-lipid carriers (NLCs) with different particle sizes and similar other properties were prepared and their physical and chemical properties such as Zeta potential and encapsulation efficiency were studied. The stability of NLCs in K-R solution and PBS buffer solution was investigated by in vitro stability experiment, and the release behavior of NLCs in vitro was studied by dialysis method. MTT assay was used to study the cytotoxicity of NLCs and drug loaded NLCs. The retention time of NLCs in the gastrointestinal tract of mice was studied by in vivo imaging. The results showed that the coumarin -6 nano-lipids with particle size of 100200 nm and 300nm had good dispersibility and could exist stably in K-R solution and PBS buffer solution. The cumulative release of coumarin -6 in vitro did not exceed 7. MTT. The results showed that the toxicity of NLCs and NLCs to Caco-2 was less than that of NLCs. The intestinal retention test of mice showed that WNLCs could still be detected in the gastrointestinal tract 6 h after intragastric administration. Therefore, the prepared NLCs with different particle sizes can be used as model preparations to study the effects of NLCs particle size on oral absorption at the cellular and animal levels.
【作者单位】： 中国药科大学药剂学教研室;中国药科大学新药研究中心;
【基金】：国家自然科学基金资助项目(No.81273467)~~
【分类号】：R943

【共引文献】

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