Department of Biomedical Engineering, College of Engineering and Applied Sciences, Nanjing University, Nanjing, Jiangsu Province 210093, China.
Nanoscale. 2015 Oct 7;7(37):15185-90. doi: 10.1039/c5nr03303a.
Tumor targeting agents including antibodies, peptides, and small molecules, are often used to improve the delivery efficiency of nanoparticles. Despite numerous studies investigating the abilities of targeting agents to increase the accumulation of nanosized therapeutics within diseased tissues, little attention has been focused on how these ligands can affect the self-assembly of the nanoparticle's modified polymer constituents upon chemical conjugation. Here we present an actively tumor targeted nanoparticle constructed via the self-assembly of a folate modified heparin. Folate conjugation unexpectedly allowed the self-assembly of heparin, where a majority of the folate molecules (>80%) resided inside the core of the nanoparticle. The folate-heparin nanoparticles could also physically encapsulate lipophilic fluorescent dyes, enabling the use of the constructs as activatable fluorescent probes for targeted in vivo tumor imaging.
肿瘤靶向剂包括抗体、肽和小分子，常被用于提高纳米颗粒的递送效率。尽管有许多研究调查了靶向剂提高纳米药物在病变组织中积累的能力，但很少关注这些配体如何影响化学偶联时纳米颗粒修饰聚合物成分的自组装。在此，我们通过叶酸修饰肝素的自组装构建了一种主动肿瘤靶向纳米颗粒。令人意外的是，叶酸偶联允许肝素自组装，其中大部分叶酸分子（>80%）位于纳米颗粒的核心内部。叶酸-肝素纳米颗粒还可以物理包封亲脂性荧光染料，使得这些构建物可以用作靶向活体肿瘤成像的激活荧光探针。
