载 CD133 适体的 PLGA 纳米粒靶向递释普萘洛尔治疗血管瘤
PLGA nanoparticles with CD133 aptamers for targeted delivery and sustained release of propranolol to hemangioma.
机构信息
Department of Vascular Surgery, Shandong Provincial Hospital affiliated to Shandong University, 324 Jingwuweiqi Road, Ji'nan 250021, China.
Department of Hemangioma & Vascular Malformation, He'nan Provincial People's Hospital, 7 Weiwu Road, Jinshui District, Zhengzhou 450003, China.
出版信息
Nanomedicine (Lond). 2017 Nov;12(21):2611-2624. doi: 10.2217/nnm-2017-0130. Epub 2017 Sep 29.
AIM
To develop propranolol-loaded poly(lactic-co-glycolic acid) nanoparticle with CD133 aptamers (PPN-CD133) to treat infantile hemangioma.
MATERIALS & METHODS: The antihemangioma activity and mechanism of PPN-CD133 were evaluated.
RESULTS & CONCLUSION: PPN-CD133 are of desired size (143.7 nm), drug encapsulation efficiency (51.8%) and sustained drug release for 8 days. PPN-CD133 could effectively bind to CD133 hemangioma stem cells, resulting in enhanced cytotoxic effect and reduced expression of angiogenesis factors in hemangioma stem cells. The therapeutic effect of PPN-CD133 in hemangioma was superior to that of untargeted PPN and propranolol in vivo, as reflected by reduced hemangioma volume, weight and microvessel density. PPN-CD133 represents a very promising approach to locally and efficiently deliver propranolol leading to significant inhibition of infantile hemangioma.
目的
研制载有 CD133 适体的普萘洛尔聚乳酸-羟基乙酸共聚物纳米粒（PPN-CD133）以治疗婴幼儿血管瘤。
材料与方法
评估 PPN-CD133 的抗血管生成活性及作用机制。
结果与结论
PPN-CD133 的粒径为（143.7±2.7）nm，药物包封率为（51.8±1.2）%，药物可持续释放 8 d。PPN-CD133 能够与 CD133 阳性的血管瘤干细胞有效结合，增强对血管瘤干细胞的细胞毒性作用，降低其血管生成因子的表达。PPN-CD133 在体内对血管瘤的治疗效果优于未靶向 PPN 和普萘洛尔，表现为血管瘤体积、重量和微血管密度降低。PPN-CD133 是一种很有前途的局部给药方法，能够高效递送普萘洛尔，显著抑制婴幼儿血管瘤。
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