本文旨在考察比较3种聚氨基酸苄酯-聚乙二醇纳米粒(PXA—PEG—NPs)材料的Calu-3细胞(人肺腺癌细胞)毒性和细胞摄取作用,优选出一种PXA—PEG—NPs作为姜黄素鼻黏膜给药载体。以姜黄素(Cur)为模型药物,采用乳化溶媒蒸发法制备聚赖氨酸苄酯-聚乙二醇纳米粒(PZLL.PEG.NPs)、聚谷氨酸苄酯-聚乙二醇纳米粒(PBLG—PEG—NPs)和聚天冬氨酸苄酯-聚乙二醇纳米粒(PBLA—PEG—NPs)纳米粒。MTT法考察3种纳米粒的Calu.3细胞毒性:采用荧光倒置显微镜和流式细胞仪对3种纳米粒的Calu.3细胞摄取作用进行定性观察和定量测定。结果表明:给予高浓度(2mg·mL-1)的纳米粒时,未见细胞毒性。3种载姜黄素聚氨基酸纳米粒的细胞摄取量均显著高于姜黄素溶液组(姜黄素质量浓度5gg·mL-1),其中Cur-PBLG.PEG.NPs组最高;纳米粒的细胞摄取量随着孵育时间延长而增加,与纳米粒浓度呈正相关。可见,PXA.PEG—NPs能递送姜黄素进入细胞,PBLG-PEG.NPs有望成为一种安全的鼻黏膜给药优良载体。
The aim of this paper is to compare the cytotoxicity and cellular uptake efficiency of three kinds of poly(b-benzyl-L-amino) block-poly(ethylene glycol) nanoparticles (PXA-PEG-NPs) using Calu-3 cells, and select one as a nasal drug delivery vector for curcumin (Cur). Poly(7-benzyl-L-glutamate) block-poly(ethylene glycol) nanoparticles (PBLG-PEG-NPs), poly(y-benzyl-L-lysine) block-poly(ethyleneglycol) nanoparticles (PZLL-PEG-NPs) and poly(7-benzyl-L-aspartate) block-poly(ethylene glycol) nanoparticles (PBLA-PEG-NPs) were prepared by emulsion-solvent evaporation method. MTT assays were used to evaluate the cytotoxicity of PXA-PEG-NPs against Calu-3 cells. The cellular uptake of nanoparticles was visualized by an inverted fluorescence microscope and quantified by a flow cytometer. The results indicated that even at high concentration of 2 mg-mL the three nanoparticles had no cytotoxicity on Calu-3 cells. Compared to the curcumin solution, the three curcumin-loaded PXA-PEG-NPs showed significantly higher cellular uptake efficiency on Calu-3 cells (at equal concentration of curcumin with 5 g.mL-1 Cur solution), PBLG-PEG-NPs group was the highest. The cellular uptake increased with incubation time, and has positive correlation with nanoparticle concentration. In brief, PXA-PEG-NPs are conducive to delivery Cur into cells, and PBLG-PEG-NPs might be provided as agood nasal drug delivery carrier.