Yang Chiming, Burt Helen M
Faculty of Pharmaceutical Sciences, University of British Columbia, 2146 East Mall, Vancouver, BC, Canada V6T 1Z3.
Adv Drug Deliv Rev. 2006 Jun 3;58(3):402-11. doi: 10.1016/j.addr.2006.01.017. Epub 2006 Mar 6.
Stent-based drug delivery system is a revolutionary approach to mitigate the negative affects of balloon angioplasty, improve immune responsiveness and prevent hyperplastic growth of smooth muscle in the restenotic state. Its success is therefore empirically associated with effective delivery of potent therapeutics to the target site at a therapeutic concentration, for a sufficient time, and in a biologically active form. However, local delivery with drug-eluting stents imparts large dynamic concentration gradients across tissues that can be difficult to identify, characterize and control. This review explores the factors such as physiological transport forces, drug physicochemical properties, local biological tissue properties and stent design that governs the local pharmacokinetics within the arterial wall by drug-eluting stent. Rational design and optimization of drug-eluting stents for local delivery thus requires a careful consideration of all these factors.
基于支架的药物递送系统是一种革命性的方法，可减轻球囊血管成形术的负面影响，提高免疫反应性，并防止再狭窄状态下平滑肌的增生性生长。因此，其成功经验性地与在足够长的时间内以生物活性形式将强效治疗药物以治疗浓度有效递送至靶部位相关。然而，药物洗脱支架的局部递送会在组织中产生大的动态浓度梯度，这些梯度可能难以识别、表征和控制。本综述探讨了诸如生理运输力、药物物理化学性质、局部生物组织性质和支架设计等因素，这些因素通过药物洗脱支架控制动脉壁内的局部药代动力学。因此，合理设计和优化用于局部递送的药物洗脱支架需要仔细考虑所有这些因素。
