Hollow nanosphere fabricated from β-cyclodextrin-grafted α,β-poly(aspartic acid) as the carrier of camptothecin.
Hollow nanosphere fabricated from β-cyclodextrin-grafted α,β-poly(aspartic acid) as the carrier of camptothecin.
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由β-环糊精接枝α，β-聚（天冬氨酸）作为喜树碱载体制成的中空纳米球。
DOI：
10.1016/j.colsurfb.2012.12.024
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发表时间：
2013-05
期刊：
影响因子：
--
通讯作者：
Junping Zeng,Haitao Huang, Shiyuan Liu,Haibo Xu,
中科院分区：
文献类型：
--
作者：
Junping Zeng,Haitao Huang, Shiyuan Liu,Haibo Xu,
本研究旨在研制一种以β-环糊精接枝α、β-聚天冬氨酸（β- cd接枝pasp）为载体的空心纳米球，以提高喜树碱（CPT）在水介质中的稳定性。首先，通过与乙二胺的取代反应，合成单(6-（2-氨基乙基）氨基-6-脱氧-β-环糊精（β-CDen）；然后用β-CDen依次打开聚（l-琥珀酰亚胺）（PSI）中的五元环，得到β- cd接枝- pasp。合成的β-CD接枝- pasp形成了独特的空心纳米球，其内孔约为17nm，壳上散布着许多0.7nm的β-CD空腔。以CPT作为β-CD的客体分子，对空心纳米球的载药性能进行了评价。值得注意的是，以β- cd -接枝- pasp空心纳米球为载体，提高了CPT在水介质中的稳定性，并且从β- cd -接枝- pasp空心纳米球中提取的CPT具有缓释特性，从而显著降低了L929细胞株的细胞毒性。此外，β- cd -移植物- pasp几乎没有细胞毒性，不适合作为药物载体应用。因此，β- cd接枝- pasp空心纳米球作为CPT的载体具有很大的潜力。
This research is aimed to develop a kind of hollow nanosphere based on β-cyclodextrin-grafted α, β-poly(aspartic acid) (β-CD-graft-PAsp) as drug carrier to enhance the stability of camptothecin (CPT) in aqueous media. Firstly, mono(6-(2-aminoethyl) amino-6-deoxy)-β-cyclodextrin (β-CDen) was synthesized by a substitution reaction between mono-6-deoxy-6-(p-tolylsulfonyl)-β-cyclodextrin (6-OTs-β-CD) and ethylenediamine; and then, the five-member rings in poly(l-succinimide) (PSI) were successively opened by β-CDen to obtain β-CD-graft-PAsp. The synthesized β-CD-graft-PAsp was found to form the unique hollow nanosphere with the internal hole of about 17nm and many β-CD cavities of 0.7nm interspersed on the shell. The drug-loading behavior of the hollow nanosphere was also evaluated by using CPT as guest molecule of β-CD. It was worth of note that the β-CD-graft-PAsp hollow nanosphere as carrier enhanced the stability of CPT in aqueous media, and the CPT from the β-CD-graft-PAsp hollow nanosphere displayed a sustained release profile and hence resulted in the essential decrease of cytotoxicity to L929 cell line. Furthermore, almost no cytotoxicity of the β-CD-graft-PAsp is desirable for the application of drug carrier. As a result, the β-CD-graft-PAsp hollow nanosphere showed a great potential as the carrier of CPT.
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