摘要
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。
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.
出处
《药学学报》
CAS
CSCD
北大核心
2013年第4期560-565,共6页
Acta Pharmaceutica Sinica
基金
国家自然科学青年基金资助项目(81001407)
关键词
姜黄素
聚氨基酸
纳米粒
细胞毒性
细胞摄取
curcumin
polyamino acid
nanoparticle
cytotoxicity
cellular uptake
