Kotla Niranjan G, Burke Orla, Pandit Abhay, Rochev Yury
Centre for Research in Medical Devices (CÚRAM), National University of Ireland Galway, Galway H91 W2TY, Ireland.
Sechenov First Moscow State Medical University, Institute for Regenerative Medicine, Moscow 119992, Russia.
Nanomaterials (Basel). 2019 Sep 2;9(9):1246. doi: 10.3390/nano9091246.
There is a pressing clinical need for advanced colon-specific local drug delivery systems that can provide major advantages in treating diseases associated with the colon, such as inflammatory bowel disease (IBD) and colon cancer. A precise colon targeted drug delivery platform is expected to reduce drug side effects and increase the therapeutic response at the intended disease site locally. In this study, we report the fabrication of hyaluronan (HA) functionalized polymeric hybrid nanoparticulate system (Cur-HA NPs) by using curcumin as a model fluorescent drug. The Cur-HA NPs were about 200-300 nm in size, -51.3 mV overall surface charge after HA functionalization, with 56.0% drug released after 72 h in simulated gastrointestinal fluids. The Cur-HA NPs did not exhibit any cytotoxicity by AlamarBlue, PicoGreen and Live/Dead assays. Following the Cur-HA NPs use on HT-29 monolayer cell cultures demonstrating, the efficacy of HA functionalization increases cellular interaction, uptake when compared to uncoated nanoparticulate system. These findings indicate that HA functionalized nano-hybrid particles are effective in delivering drugs orally to the lower gastrointestinal tract (GIT) in order to treat local colonic diseases.
对于先进的结肠特异性局部给药系统存在迫切的临床需求，这类系统在治疗与结肠相关的疾病（如炎症性肠病（IBD）和结肠癌）方面具有显著优势。一个精确的结肠靶向给药平台有望减少药物副作用，并在局部预期疾病部位提高治疗反应。在本研究中，我们报道了以姜黄素作为模型荧光药物制备透明质酸（HA）功能化的聚合物杂化纳米颗粒系统（Cur-HA NPs）。Cur-HA NPs的尺寸约为200 - 300 nm，HA功能化后整体表面电荷为 -51.3 mV，在模拟胃肠液中72小时后药物释放率为56.0%。通过AlamarBlue、PicoGreen和活/死检测，Cur-HA NPs未表现出任何细胞毒性。在HT-29单层细胞培养中使用Cur-HA NPs后表明，与未包被的纳米颗粒系统相比，HA功能化提高了细胞相互作用和摄取效率。这些发现表明，HA功能化的纳米杂化颗粒在口服给药至下胃肠道（GIT）以治疗局部结肠疾病方面是有效的。
