| 陶阳春李飞范黎成冲乔友备李伟段晓吴红△.聚苹果酸- 聚乙二醇- 叶酸纳米共聚物的合成和生物活性的研究[J].,2012,12(21):4019-4022 |
| 聚苹果酸- 聚乙二醇- 叶酸纳米共聚物的合成和生物活性的研究 |
| Folated-decorated Poly (β-malic acid)-poly (ethylene glycol)Nano-copolymers: Synthesis and Biological Evaluation |
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| DOI： |
| 中文关键词: 聚苹果酸 腙键 纳米共聚物 主动靶向 pH 响应 |
| 英文关键词: Poly (β-malic acid) Hydrazone bond Nanocopolymer Active targeting pH response |
| 基金项目:国家自然科学基金（30970788） |
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| 中文摘要: |
| 目的：制备聚苹果酸- 聚乙二醇- 叶酸(PMLA-PEG-FA)纳米共聚物，为构建多功能靶向药物转运系统提供前期工作。方法：
配体叶酸(FA)通过α- 羟基-ω- 醛基聚乙二醇(HO-PEG-CHO)以腙键连接在经过水合肼修饰的聚苹果酸的主链上。核磁共振光谱
表征纳米共聚物的结构，动态透析法研究腙键响应不同pH 值的断键特性，监测不同pH 值共聚物中叶酸的稳定性。并采用SMCC-
7721 人体肝癌细胞测定该纳米共聚物的细胞毒性。结果：1、经核磁共振表征PMLA-PEG-FA 共聚物合成完成。2、在pH5.5、
pH6.5 及pH7.4 的PBS 缓冲体系中，6h 后配体叶酸累积释放率分别为88.1 %，85.3 %和41.6 %。3、MTT 实验证实PMLA-PEG-FA
无毒性。结论：PMLA-PEG-FA 有望成为智能靶向药物载体。 |
| 英文摘要: |
| Objective: To prepare the folated-decorated poly (β-malic acid)-poly (ethylene glycol) nano-copolymers (abbreviated
as PMLA-PEG-FA) which is to provide a new type of drug carrier for anticancer drug delivery system. Methods: The structure of this
copolymer was confirmed by 1H-HMR. Moreover, the FA conjugation efficiency and FA release property were determined. The cytotoxicity
was assessed by using human hepatocarcinoma SMMC-7721 cells as in vitro cell model. Results: 1. The copolymer was prepared
successfully. 2. In vitro FA release from PMLA-PEG-FA conjugate occurred at a faster rate at acidic pH compared with neutral pH(7.4).
After 6h of incubation at pH 5.5, pH 6.5 and pH7.4 the released free FA was about 88.1% , 85.3% and 41.6% . Conclusion: PMLA-
PEG-FA nanocopolymer is expected to be used as an intelligent active-targeting drug carrier. |
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