Svenson Sonke, Chauhan Abhay S
Drug Delivery Solutions LLC, Midland, MI 48642, USA.
Nanomedicine (Lond). 2008 Oct;3(5):679-702. doi: 10.2217/17435889.3.5.679.
Approximately 40% of newly developed drugs are rejected by the pharmaceutical industry and will never benefit a patient because of low water solubility. Another 17% of launched drugs exhibit suboptimal performance for the same reason. Given the growing impact and need for drug delivery, a thorough understanding of delivery technologies that enhance the bioavailability of drugs is important. The high level of control over the dendritic architecture (size, branching density, surface functionality) makes dendrimers ideal excipients for enhanced solubility of poorly water-soluble drugs. Many commercial small-molecule drugs with anticancer, anti-inflammatory and antimicrobial activity have been formulated successfully with dendrimers, such as poly(amidoamine) (PAMAM), poly(propylene imine) (PPI or DAB) and poly(etherhydroxylamine) (PEHAM). Some dendrimers themselves show pharmaceutical activity in these three areas, providing the opportunity for combination therapy in which the dendrimers serve as the drug carrier and simultaneously as an active part of the therapy.
大约40%新研发的药物因水溶性低而被制药行业拒用，永远无法使患者受益。另有17%已上市药物也因同样原因表现欠佳。鉴于药物递送的影响日益增大且需求不断增加，深入了解可提高药物生物利用度的递送技术非常重要。对树枝状结构（尺寸、分支密度、表面官能团）的高度可控性使树枝状聚合物成为提高难溶性药物溶解度的理想辅料。许多具有抗癌、抗炎和抗菌活性的商业小分子药物已成功与树枝状聚合物（如聚酰胺胺（PAMAM）、聚亚丙基亚胺（PPI或DAB）和聚醚羟胺（PEHAM））进行配方。一些树枝状聚合物本身在这三个领域显示出药物活性，为联合治疗提供了机会，其中树枝状聚合物既作为药物载体，又同时作为治疗的活性成分。
