背景:糖尿病并发症是糖尿病患者死亡的主要原因。常见的并发症是抗氧化能力下降和微炎症综合征的发作。目前,葡萄糖响应性纳米粒子被广泛使用,因为它们可以智能地释放负载胰岛素的超细颗粒,并有效地降低血糖。然而,这种方法的毒理学尚未完全阐明。蝶芪(PTE)植物提取物具有广泛的生物应用,如抗氧化和炎症反应的改善。因此,我们提出了植物提取物和生物材料交叉应用的新思路,特别是作为降血糖纳米药物递送系统的一部分。
结果:基于PTE,我们成功合成了聚(3-丙烯酰胺基苯基硼酸-b-蝶芪)(p[AAPBA-b-PTE])纳米颗粒(NPs)。NP的形状为圆形,尺寸在150和250nm之间。NP具有良好的pH和葡萄糖敏感性。负载胰岛素的NP的包封效率(EE)约为56%,载药量(LC)约为13%。胰岛素的最高释放量为70%,PTE的最高释放量为85%。同时,胰岛素可以根据葡萄糖浓度的变化进行自我调节,从而实现有效的,持续释放。体内和体外实验均表明NPs是安全无毒的。在正常生理条件下,NPs在40天内完全降解。小鼠注射p(AAPBA-b-PTE)NP后14天,心脏没有明显的异常,肝脏,脾,脾肺,或肾。此外,NPs有效降低血糖,改善小鼠的抗氧化能力和逆转微炎症。
结论:以PTE为原料成功制备了p(AAPBA-b-PTE)NPs,有效降低了血糖,提高抗氧化能力,减轻炎症反应。这种新的制剂可以使植物提取物和生物材料的新组合能够通过NP或其他剂型施用以调节和治疗疾病。
BACKGROUND: Diabetes complications are the leading cause of mortality in diabetic patients. The common complications are decline in antioxidant capacity and the onset of micro-inflammation syndrome. At present, glucose-responsive nanoparticles are widely used, as they can release insulin-loaded ultrafine particles intelligently and effectively reduce blood sugar. However, the toxicology of this method has not been fully elucidated. The plant extracts of pterostilbene (PTE) have a wide range of biological applications, such as antioxidation and inflammatory response improvement. Therefore, we have proposed new ideas for the cross application of plant extracts and biomaterials, especially as part of a hypoglycaemic nano-drug delivery system.
RESULTS: Based on the PTE, we successfully synthesised poly(3-acrylamidophenyl boric acid-b-pterostilbene) (p[AAPBA-b-PTE]) nanoparticles (NPs). The NPs were round in shape and ranged between 150 and 250 nm in size. The NPs possessed good pH and glucose sensitivity. The entrapment efficiency (EE) of insulin-loaded NPs was approximately 56%, and the drug loading (LC) capacity was approximately 13%. The highest release of insulin was 70%, and the highest release of PTE was 85%. Meanwhile, the insulin could undergo self-regulation according to changes in the glucose concentration, thus achieving an effective, sustained release. Both in vivo and in vitro experiments showed that the NPs were safe and nontoxic. Under normal physiological conditions, NPs were completely degraded within 40 days. Fourteen days after mice were injected with p(AAPBA-b-PTE) NPs, there were no obvious abnormalities in the heart, liver, spleen, lung, or kidney. Moreover, NPs effectively reduced blood glucose, improved antioxidant capacity and reversed micro-inflammation in mice.
CONCLUSIONS: p(AAPBA-b-PTE) NPs were successfully prepared using PTE as raw material and effectively reduced blood glucose, improved antioxidant capacity and reduced the inflammatory response. This novel preparation can enable new combinations of plant extracts and biomaterials to adiministered through NPs or other dosage forms in order to regulate and treat diseases.