人胃癌细胞HGC-27对PEG化聚乳酸羟基乙酸纳米粒的摄取

制备黏惰性纳米粒(mPEG-PLGA-NPs)以克服人胃癌HGC-27细胞周围黏液的黏附，研究mPEG-PLGA-NPs理化性质对纳米粒穿透黏液被HGC-27细胞摄取的影响。体外黏蛋白黏附实验证明，mPEG-PLGA-NPs具有良好的黏惰性；激光共聚焦显微镜及HPLC法考察HGC-27细胞对不同理化性质mPEG-PLGA-NPs的摄取。结果显示:HGC-27细胞对纳米粒的摄取与孵育时间(0~4 h)成依赖关系。同一孵育时间内，HGC-27细胞对纳米粒的摄取随着mPEG相对分子质量和修饰密度的增加而增加，10%PEG₂₀₀₀-PLGA-NPs的摄取量是PLGA-NPs的1.7~2.0倍，是荷正电荷CS-PLGA-NPs的摄取量的1.8~2.4倍，粒径400 nm 的纳米粒的摄取量仅为粒径120 nm的55.9%~70.3%。结果表明，亲水性且表面电荷接近中性、大小适宜的mPEG-PLGA-NPs对黏蛋白具有一定的黏惰性，能够快速穿透HGC-27细胞周围黏液被细胞摄取。mPEG-PLGA-NPs有望成为一种新型的载药系统用于胃黏液癌的治疗。

Uptake of mPEG-PLGA nanoparticles by human gastric cancer HGC-27 cell

Mucoinert nanoparticles(mPEG-PLGA-NPs)was prepared to overcome the adhesion of mucus in this study and the cellular uptake of nanoparticles with different physio-chemical properties by human gastric cancer HGC-27 cells was investigated. The muco-inert activity of nanoparticles was evaluated by pig gastric mucin(PM)binding experiments. Cellular uptake of nanoparticles in HGC-27 cells was analyzed by confocal laser scanning microscope and HPLC. The results indicated that mPEG-PLGA-NPs had good mucin-inert activity. The mPEG₂₀₀₀-PLGA-NPs could be rapidly uptaken by HGC-27 cells. The celluar uptake of 10%mPEG₂₀₀₀-PLGA-NPs was 1. 7-2. 0 folds higher than PLGA-NPs and 1. 8-2. 4 folds higher than CS-PLGA-NPs during the same incubation time. The intake of diameter nanoparticles with 400 nm was only 55. 9%-70. 3% of those with 120 nm. mPEG-PLGA-NPs possess hydrophilic and near neutrally-charged surfaces that minimize mucoadhesion. mPEG-PLGA-NPs can quickly penetrate the mucus surrounding HGC-27 cells and be uptaken by cells. mPEG-PLGA-NPs are expected to be used for the treatment of mucinous carcinoma.