Chen Weiluan, Habraken Tom C J, Hennink Wim E, Kok Robbert J
Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Universiteitsweg 99, 3584 CG Utrecht, The Netherlands.
Bioconjug Chem. 2015 Jul 15;26(7):1277-88. doi: 10.1021/acs.bioconjchem.5b00192. Epub 2015 Jun 18.
Clinical evaluations have proven the efficacy of drug-elution stents (DES) in reduction of in-stent restenosis rates as compared to drug-free bare metal stents (BMS). Typically, DES are metal stents that are covered with a polymer film loaded with anti-inflammatory or antiproliferative drugs that are released in a sustained manner. However, although favorable effects of the released drugs have been observed, the polymer coating as such has been associated with several adverse clinical effects, such as late stent thrombosis. Elimination of the polymeric carrier of DES may therefore potentially lead to safer DES. Several technologies have been developed to design polymer-free DES, such as the use of microporous stents and inorganic coatings that can be drug loaded. Several drugs, including sirolimus, tacrolimus, paclitaxel, and probucol have been used in the design of carrier-free stents. Due to the function of the polymeric coating to control the release kinetics of a drug, polymer-free stents are expected to have a faster drug elution rate, which may affect the therapeutic efficacy. However, several polymer-free stents have shown similar efficacy and safety as the first-generation DES, although the superiority of polymer-free DES has not been established in clinical trials.
临床评估已证实，与无药物的裸金属支架（BMS）相比，药物洗脱支架（DES）在降低支架内再狭窄率方面具有疗效。通常，DES是金属支架，上面覆盖有载有抗炎或抗增殖药物的聚合物薄膜，这些药物以持续方式释放。然而，尽管已观察到释放药物的有利效果，但聚合物涂层本身却与多种不良临床效应相关，如晚期支架血栓形成。因此，去除DES的聚合物载体可能会使DES更安全。已开发出多种技术来设计无聚合物DES，如使用可载药的微孔支架和无机涂层。包括西罗莫司、他克莫司、紫杉醇和普罗布考在内的多种药物已用于无载体支架的设计。由于聚合物涂层具有控制药物释放动力学的功能，预计无聚合物支架的药物洗脱速度会更快，这可能会影响治疗效果。然而，尽管无聚合物DES的优越性尚未在临床试验中得到证实，但几种无聚合物支架已显示出与第一代DES相似的疗效和安全性。
