Shi Xudong, Chen Guojun, Guo Lian-Wang, Si Yi, Zhu Men, Pilla Srikanth, Liu Bo, Gong Shaoqin, Kent K Craig
Department of Surgery, University of Wisconsin Hospital and Clinics, Madison, Wisconsin, United States of America.
Wisconsin Institutes for Discovery, University of Wisconsin, Madison, Wisconsin, United States of America ; Materials Science Program, University of Wisconsin, Madison, Wisconsin, United States of America.
PLoS One. 2014 Feb 21;9(2):e89227. doi: 10.1371/journal.pone.0089227. eCollection 2014.
Open vascular reconstructions frequently fail due to the development of recurrent disease or intimal hyperplasia (IH). This paper reports a novel drug delivery method using a rapamycin-loaded poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs)/pluronic gel system that can be applied periadventitially around the carotid artery immediately following the open surgery. In vitro studies revealed that rapamycin dispersed in pluronic gel was rapidly released over 3 days whereas release of rapamycin from rapamycin-loaded PLGA NPs embedded in pluronic gel was more gradual over 4 weeks. In cultured rat vascular smooth muscle cells (SMCs), rapamycin-loaded NPs produced durable (14 days versus 3 days for free rapamycin) inhibition of phosphorylation of S6 kinase (S6K1), a downstream target in the mTOR pathway. In a rat balloon injury model, periadventitial delivery of rapamycin-loaded NPs produced inhibition of phospho-S6K1 14 days after balloon injury. Immunostaining revealed that rapamycin-loaded NPs reduced SMC proliferation at both 14 and 28 days whereas rapamycin alone suppressed proliferation at day 14 only. Moreover, rapamycin-loaded NPs sustainably suppressed IH for at least 28 days following treatment, whereas rapamycin alone produced suppression on day 14 with rebound of IH by day 28. Since rapamycin, PLGA, and pluronic gel have all been approved by the FDA for other human therapies, this drug delivery method could potentially be translated into human use quickly to prevent failure of open vascular reconstructions.
开放式血管重建术常常因复发性疾病或内膜增生(IH)的发展而失败。本文报道了一种新型药物递送方法,该方法使用负载雷帕霉素的聚(丙交酯-共-乙交酯)(PLGA)纳米颗粒(NPs)/普朗尼克凝胶系统,可在开放手术后立即在颈动脉周围的外膜周围应用。体外研究表明,分散在普朗尼克凝胶中的雷帕霉素在3天内迅速释放,而嵌入普朗尼克凝胶中的负载雷帕霉素的PLGA NPs中的雷帕霉素在4周内释放更为缓慢。在培养的大鼠血管平滑肌细胞(SMCs)中,负载雷帕霉素的NPs对mTOR途径的下游靶点S6激酶(S6K1)的磷酸化产生了持久的抑制作用(游离雷帕霉素为3天,负载雷帕霉素的NPs为14天)。在大鼠球囊损伤模型中,负载雷帕霉素的NPs在外膜周围递送在球囊损伤后14天对磷酸化S6K1产生抑制作用。免疫染色显示,负载雷帕霉素的NPs在第14天和第28天均减少了SMC增殖,而单独使用雷帕霉素仅在第14天抑制了增殖。此外,负载雷帕霉素的NPs在治疗后至少28天可持续抑制内膜增生,而单独使用雷帕霉素在第14天产生抑制作用,到第28天内膜增生出现反弹。由于雷帕霉素、PLGA和普朗尼克凝胶均已被FDA批准用于其他人类治疗,这种药物递送方法有可能很快转化为人类应用,以防止开放式血管重建术失败。
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