中文摘要：

该研究旨在构建普朗尼克F-127（PF-127）包裹的三甲基壳聚糖（TMC）纳米粒（F-S NPs）,以提高TMC纳米粒（S NPs）克服黏液屏障的能力。以胰岛素（INS）为模型药物,采用单因素筛选法优化纳米粒（F-S NPs）的处方,获得粒径为（240.6±6.51）nm、Zeta电位＋（10.42±1.60）m V、包封率（43.39±2.83）%、载药量（3.39±0.57）%的纳米粒。分别采用黏蛋白吸附实验和尤斯室实验考察纳米粒克服黏液屏障的能力。用黏液分泌型细胞HT29-MTX-E12考察纳米粒的摄取能力。结果表明,F-S NPs与黏蛋白的亲和能力仅为S NPs的28%,其表观黏液渗透系数为S NPs的2.79倍。F-S NPs的细胞摄取能力分别为游离胰岛素、S NPs的16和1.4倍。PF-127成功包裹于S NPs的表面,显著提高了纳米粒克服黏液屏障和E12细胞的摄取能力。

英文摘要：

The purpose of this investigation was to develop Pluronic F-127 coated N-trimethyl chitosan nanoparti- cles （F-S NPs） of insulin as the model drug and asses their penetration of the mueosal barriers. Single factor screening was used to optimize the formulations of nanoparticles and the nanopartieles were characterized. Their particle size, Zeta potential, encapsulation efficiencies and drug loading were assayed to be （240.6 ± 6.51）nm, （ 10. 42 ±1.60） mV, （43.39 ±2. 83） % and （ 3.39 ± 0.57） %, respectively. The impact of PF-127 on mucin binding in vitro and nanoparticles＇s transport in freshly obtained mucus were also evaluated. The mucin affinity of F-S NPs was significantly reduced when compared to that of the N-trimethyl chitosan nanoparticles （S NPs）, i. e. , 28% of the latter. And F-S NPs was found to have an improved mucosal penetrating capability. Mucus- secreting HT29-MTX-E12 （E12） cell monolayer was selected to investigate their cellular uptake. F-S NPs exhibi- ted higher penetration coefficient than both free insulin and S NPs in mucus-secreting epithelium cells, i. e. , 16- fold and 1.4-fold, respectively. Data suggest that F-S NPs be potential carriers to cross mucosal barriers and enhance the cellular uptake of insulin.