基于柱芳烃的高分子药物输送载体

The applicant plans to use the newest generation of macrocyclic host pillar[n]arene. By using pillar[n]arene derivatives as macromers to form polymers or using them to graft polymers, we will get novel pillar[n]arene based polymeric materials. By investigating the interaction between pillar[n]arene based polymeric materials and small molecule or large molecule drugs, we will try to find the basic rule for its drug loading and drug releasing. We will also use pillarene based polymeric materials to assemble nanoparticles by covalent or host-guest cross-linking. By adjusting the host-guest chemistry of pillar[n]arene and small molecules, we are able to control the drug delivery behavior of pillar[n]arene based polymeric materials. By introducing targeting groups, we can also realize target specific drug delivery. After studying its biocompatibility, we will study its drug delivery to cells, biodistribution in vivo, and drug delivery effect to cancer tissues.

申请人计划利用最新一代、容易制备的主体大环分子柱芳烃，以柱芳烃衍生物为聚合单体形成高分子或者直接修饰高分子，得到新型柱芳烃高分子材料。我们将研究柱芳烃高分子材料与小分子和大分子药物的相互作用，诠释其载药与释药规律。并且利用柱芳烃高分子材料，通过共价交联或者主客体交联的办法，组装纳米粒子。我们将利用调节柱芳烃与小分子独特的主客体作用，调控柱芳烃高分子材料的药物输送行为。同时，加入靶向官能团，实现靶向给药。在系统研究其生物兼容性以后，我们将研究其细胞层面的药物输送效果，并且研究体内所输送药物的各器官分布与对癌组织的递药效果。

我们发展了柱芳烃的新型合成方法，开发了一系列基于柱芳烃的新型材料。开发的新型合成方法可以用于复杂与特定结构柱芳烃分子的制备，为该类柱芳烃用于材料制备创造了条件。小分子水溶性柱芳烃材料被用于疏水型药物的增溶，可以用于药物输送用途。新型材料包括基于柱芳烃的交联高分子，可以用于水溶性分子的吸附，为下一步的生物医学用途创造了条件。