Stealth dendrimers for antiarrhythmic quinidine delivery
Stealth dendrimers for antiarrhythmic quinidine delivery
复制标题
DOI：
10.1007/s10856-007-3144-0
复制
发表时间：
2007-10-01
影响因子：
3.7
通讯作者：
Lopina, Stephanie T.
中科院分区：
文献类型：
--
作者：
Yang, Hu;Lopina, Stephanie T.
树枝状大分子由于其独特的球形纳米结构和表面大量的功能基团而受到越来越多的关注。将PEG附接到树枝状聚合物产生隐形树枝状聚合物，其具有用于药物递送的有希望的结构优势。本研究探索了以隐形树枝状大分子为载体的抗肿瘤药物奎尼丁的合成方法。特别地，奎尼丁分别通过甘氨酸间隔基共价连接到阴离子G2.5和阳离子G3.0聚酰胺胺（PAMAM）树枝状聚合物。通过FT-IR和H-1-NMR对所得奎尼丁-PAMAM-PEG缀合物进行了表征和证实。在37 ° C下在pH 7.4的PBS缓冲液中进行体外水解，以确认缀合的奎尼丁的生物利用度。
Dendrimers have been attracting growing attention because of their unique well-defined globular nanoscale architecture and numerous functional groups on the surface. Attachment of PEG to the dendrimer generates stealth dendrimers, which have promising structural advantages for drug delivery. In this study, synthetic methods were explored to deliver antiarrhythmic quinidine by stealth dendrimers. In particular, quinidine was covalently attached to anionic G2.5 and cationic G3.0 polyamidoamine (PAMAM) dendrimers via a glycine spacer, respectively. The resulting quinidine-PAMAM-PEG conjugates were characterized and confirmed by FT-IR and H-1-NMR. In vitro hydrolysis was carried out in pH 7.4 PBS buffer at 37 degrees C to confirm the bioavailability of the conjugated quinidine.