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Transdermal delivery of rapamycin with poor water-solubility by dissolving polymeric microneedles for anti-angiogenesis.
Journal of Materials Chemistry B ( IF 7 ) Pub Date : 2020-01-08 , DOI: 10.1039/c9tb00912d
Jinzhu Mao 1 , Hua Wang 2 , Ying Xie 1 , Yangxue Fu 1 , Yuce Li 2 , Pei Liu 2 , Hongyao Du 1 , Jinjin Zhu 1 , Liyun Dong 1 , Mubashir Hussain 2 , Yan Li 1 , Lianbin Zhang 2 , Jintao Zhu 2 , Juan Tao 1
Affiliation  

Angiogenesis plays an important role in the occurrence and development of skin tumors and vascular anomalies (VAs). Many drugs have been adopted for the inhibition of angiogenesis, among which rapamycin (RAPA) possesses good application prospects. However, the clinical potential of RAPA for VAs is limited by its poor solubility, low bioavailability, and high cytotoxicity. To extend its application prospect for VAs treatment, in this study, we develop RAPA-loaded dissolving polymeric microneedles (RAPA DMNs) made of polyvinylpyrrolidone (PVP) due to its excellent solubilizing ability. RAPA DMNs are shown to have sufficient mechanical strength to overcome the skin barrier of the stratum corneum and could deliver RAPA to a depth of 200 μm. The microneedle shafts completely dissolve and 80% of the drug could be released within 10 min after insertion ex vivo. The DMNs-penetrated mice skin could repair itself within 4 h after the application of RAPA DMNs. RAPA DMNs also show good anti-angiogenic effect by inhibiting the growth of human umbilical vein endothelial cells (HUVECs) and decreasing the secretion of vascular endothelial growth factor (VEGF). Therefore, RAPA DMNs promisingly provide a safe and efficient approach for VAs treatment.

中文翻译:

通过溶解聚合物微针进行抗血管生成,雷帕霉素的透皮递送水溶性差。

血管生成在皮肤肿瘤和血管异常(VA)的发生和发展中起重要作用。抑制血管生成的药物很多,其中雷帕霉素(RAPA)具有良好的应用前景。但是,RAPA对VA的临床潜力受到其溶解性差,生物利用度低和细胞毒性高的限制。为了扩展其在VAs治疗中的应用前景,在本研究中,由于其出色的增溶能力,我们开发了由聚乙烯吡咯烷酮(PVP)制成的装有RAPA的可溶性聚合物微针(RAPA DMN)。RAPA DMN具有足够的机械强度,可以克服角质层的皮肤屏障,并且可以将RAPA输送至200μm的深度。微针轴完全溶解,离体插入后10分钟内可释放80%的药物。应用RAPA DMNs后,渗透DMNs的小鼠皮肤可以在4小时内自我修复。RAPA DMN通过抑制人脐静脉内皮细胞(HUVEC)的生长并减少血管内皮生长因子(VEGF)的分泌,也显示出良好的抗血管生成作用。因此,RAPA DMN有望为VAs治疗提供一种安全有效的方法。
更新日期:2020-02-13
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