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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(2 mg.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5μg.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。
This study aimed to investigate the toxicity and cellular uptake of Calu-3 cells (human lung adenocarcinoma cells) from three polyamino acid benzyl ester polyethylene glycol nanoparticles (PXA-PEG-NPs). A PXA-PEG -NPs as a carrier for curcumin nasal mucosa. Poly (lysine benzyl ester) polyethylene glycol nanoparticles (PZLL-PEG-NPs), poly (glutamic acid benzyl ester) polyethylene glycol nanoparticles (PBLGs) were prepared by emulsion solvent evaporation with curcumin as model drug. -PEG-NPs) and poly-aspartic acid benzyl ester polyethylene glycol nanoparticles (PBLA-PEG-NPs) nanoparticles. The cytotoxicity of Calu-3 of three kinds of nanoparticles was investigated by MTT assay. The uptake of Calu-3 cells by three kinds of nanoparticles was observed and quantified by fluorescence inverted microscopy and flow cytometry. The results show that: given high concentrations (2 mg.mL1) of nanoparticles, no cytotoxicity. The cellular uptake of the three curcuminoid polyamino acid nanoparticles was significantly higher than that of the curcumin solution group (curcumin concentration 5 μg.mL 1), of which Cur-PBLG-PEG-NPs group was the highest. The cell uptake of the nanoparticles The incubation time increased and increased, and the concentration of nanoparticles was positively correlated. It can be seen that PXA-PEG-NPs can deliver curcumin into cells, and PBLG-PEG-NPs are expected to be a safe carrier for nasal mucosa administration.