School of Nano Sciences, Central University of Gujarat, Gandhinagar, Gujarat 382030, India.
School of Life Sciences, Central University of Gujarat, Gandhinagar, Gujarat 382030, India.
Int J Biol Macromol. 2024 Apr;263(Pt 2):130274. doi: 10.1016/j.ijbiomac.2024.130274. Epub 2024 Feb 17.
Inulin (INU) is a versatile natural polysaccharide primarily derived from chicory roots. INU possesses the unique quality of evading digestion or fermentation in the early stages of the human digestive tract, instead reaching the lower colon directly. Exploiting on this distinctive attribute, INU finds application in the creation of targeted carrier systems for delivering drugs tailored to colon-related diseases. This study presents a novel method for synthesizing highly stable and non-aggregatory inulin nanoparticles (INU NPs) by ionotropic gelation method, using calcium chloride as crosslinker and natural honey as a stabilizing agent. Different formulation and process parameters were optimized for the synthesis of monodispersed INU NPs. These INU NPs efficiently encapsulated a hydrophilic drug irinotecan hydrochloride trihydrate (IHT) and drug loaded formulation (IINPs) demonstrated excellent colloidal and storage stabilities. Notably, these IINPs exhibited pH-dependent drug release, suggesting potential for colon-specific drug delivery. Anticancer activity of the NPs was found significantly higher in comparison to IHT through cytotoxicity and apoptosis studies against human colorectal carcinoma cells. Overall, this study revealed that the INU NPs synthesized by ionotropic gelation will be an efficient nanocarrier system for colon-targeted drug delivery due to their exceptional biocompatibility and stability in stomach and upper intestinal conditions.
菊粉（INU）是一种用途广泛的天然多糖，主要来源于菊苣根。INU 具有独特的性质，即在人体消化道的早期阶段不会被消化或发酵，而是直接到达结肠下部。利用这一独特的特性，INU 被应用于开发针对与结肠相关疾病的药物的靶向载体系统。本研究提出了一种通过离子凝胶化方法合成高度稳定且无聚集的菊粉纳米颗粒（INU NPs）的新方法，使用氯化钙作为交联剂，天然蜂蜜作为稳定剂。对不同的配方和工艺参数进行了优化，以合成单分散的 INU NPs。这些 INU NPs 能够有效地包封亲水性药物盐酸伊立替康三水合物（IHT），载药制剂（IINPs）表现出优异的胶体和储存稳定性。值得注意的是，这些 IINPs 表现出 pH 依赖性药物释放，表明其具有潜在的结肠特异性药物递送能力。通过对人结肠癌细胞的细胞毒性和细胞凋亡研究，发现与 IHT 相比，这些 NPs 的抗癌活性显著提高。总的来说，由于 INU NPs 在胃和上消化道条件下具有出色的生物相容性和稳定性，因此通过离子凝胶化合成的 INU NPs 将成为一种用于结肠靶向药物递送的高效纳米载体系统。
