Department of Industrial Biotechnology, Atta ur Rahman School of Applied Biosciences, National University of Sciences and Technology, Islamabad 44000, Pakistan.
Department of Industrial Biotechnology, Atta ur Rahman School of Applied Biosciences, National University of Sciences and Technology, Islamabad 44000, Pakistan.
Int J Biol Macromol. 2020 Jun 15;153:36-45. doi: 10.1016/j.ijbiomac.2020.02.191. Epub 2020 Feb 22.
Amygdalin, despite possessing anticancerous properties, has been viewed as a controversial choice due to the presence of the cyanide group. Here, we synthesise and investigate the potential of alginate-chitosan nanoparticles (ACNPs) as drug delivery agents for amygdalin encapsulation and its delivery to cancer cells. Amygdalin loaded ACNPs were made with both anionic and cationic outer layer to further investigate charge dependency on drug delivery and cytotoxicity. ACNPs encapsulating amygdalin were monodisperse, colloidally stable with ~90% drug encapsulation efficiency and were entirely made from natural materials. The nanoparticles exhibited sustained drug release for a duration of 10 h and significant swelling rates in neutral and slightly acidic environments. The ACNPs successfully adhered to porcine mucin type II when assessed for its mucoadhesion and shown to transmigrate with an average velocity of 1.68 μm/s in uncoated channels, under biomimicked flow conditions. To investigate charge dependency on drug delivery and cytotoxicity, amygdalin loaded ACNPs were made with both anionic and cationic outer layer and assessed. ACNPs demonstrated greater yet sustained anti-cancerous effect on H1299 cell lines in a dose-dependent manner than free amygdalin suggesting greater cellular uptake of the former. In conclusion, biocompatible and biodegradable alginate-chitosan nanoparticles can be used as an effective drug delivery system for sustained and controlled amygdalin release with its improved cytotoxic effect on cancerous cells while protecting normal cells and tissues.
尽管苦杏仁苷具有抗癌特性，但由于存在氰基基团，它被认为是一种有争议的选择。在这里，我们合成并研究了海藻酸钠-壳聚糖纳米粒子（ACNPs）作为苦杏仁苷包封及其递送至癌细胞的药物传递剂的潜力。用带阴离子和阳离子外层的海藻酸钠-壳聚糖纳米粒子来进一步研究药物传递和细胞毒性对电荷的依赖性。负载苦杏仁苷的 ACNPs 呈单分散性，胶体稳定，具有~90%的药物包封效率，并且完全由天然材料制成。纳米粒子在 10 小时内持续释放药物，在中性和略酸性环境中具有显著的溶胀率。当评估其黏膜黏附性时，ACNPs 成功地黏附在猪黏膜 II 型上，并在模拟生物条件下的未涂层通道中以 1.68μm/s 的平均速度迁移。为了研究电荷对药物传递和细胞毒性的依赖性，用阴离子和阳离子外层制备了负载苦杏仁苷的 ACNPs 并进行了评估。ACNPs 对 H1299 细胞系表现出更大但持续的抗癌作用，呈剂量依赖性，比游离苦杏仁苷更能持续抗癌，这表明前者的细胞摄取量更大。总之，生物相容和可生物降解的海藻酸钠-壳聚糖纳米粒子可用作苦杏仁苷持续和控制释放的有效药物传递系统，其对癌细胞的细胞毒性作用得到改善，同时保护正常细胞和组织。
