Biophysics Department, Faculty of Science, Cairo University, Giza, Egypt.
BMC Pharmacol Toxicol. 2023 Mar 30;24(1):21. doi: 10.1186/s40360-023-00662-1.
Oral insulin administration has recently become one of the most exciting research subjects. Different approaches have been carried out to get an effective oral insulin delivery system using nanotechnology. The development of a delivery system that overcomes the difficulties of oral insulin administration, achieving high stability and minimal side effects, is still an urgent need. Therefore, this study is considered one of the efforts to design a new prospective drug delivery nano-composite (silica-coated chitosan-dextran sulfate nanoparticles).
Chitosan-dextran sulfate nanoparticles (CS-DS NPs) were prepared via a complex coacervation method and then coated with silica. Uncoated and silica-coated CS-DS NPs were physically characterized via different techniques. Transmission electron microscopy (TEM), scanning electron microscopy (SEM), energy-dispersive X-ray (EDX) analysis, and atomic force microscopy (AFM) have been used to investigate the chemical elements, size, morphology, and surface properties of the prepared formulations. Differential scanning calorimetry (DSC) to assess the thermal properties of formed nano-formulations. Fourier transform infrared (FT-IR) spectroscopy investigated the silica coat and chitosan interaction. The encapsulation efficiency was evaluated using high-performance liquid chromatography (HPLC) analysis. The insulin release profile of nano-formulations was performed with and without silica coat at two different pHs (5.5,7), nearly simulating the environment of the gastrointestinal tract (GIT).
The silica-coated CS-DS NPs revealed interesting physicochemical properties exemplified by suitable core particle size obtained by TEM images (145.31 ± 33.15 nm), hydrodynamic diameter (210 ± 21 nm), high stability indicated by their zeta potential value (-32 ± 3.2 mV), and adequate surface roughness assessed by AFM. The encapsulation efficiency of insulin-loaded chitosan nanoparticles (ICN) was (66.5%) higher than that of insulin-chitosan complex nanoparticles (ICCN). The silica-coated ICN demonstrated a controlled insulin release profile at pHs (5.5 and 7) compared with uncoated ICN.
The silica-coated ICN can be an efficient candidate as a desired oral delivery system, overcoming the common obstacles of peptides and proteins delivery and achieving high stability and controlled release for further applications.
口服胰岛素给药最近成为最令人兴奋的研究课题之一。为了开发一种克服口服胰岛素给药困难、实现高稳定性和最小副作用的递送系统,已经采用了不同的方法。因此,这项研究被认为是设计新型口服递药纳米复合材料(硅涂层壳聚糖-葡聚糖硫酸酯纳米粒)的努力之一。
壳聚糖-葡聚糖硫酸酯纳米粒(CS-DS NPs)通过复凝聚法制备,然后用硅涂层包裹。未涂层和硅涂层 CS-DS NPs 通过不同的技术进行物理特性表征。使用透射电子显微镜(TEM)、扫描电子显微镜(SEM)、能量色散 X 射线(EDX)分析和原子力显微镜(AFM)研究了所制备配方的化学元素、大小、形态和表面特性。差示扫描量热法(DSC)评估了形成的纳米制剂的热特性。傅里叶变换红外(FT-IR)光谱研究了硅涂层和壳聚糖的相互作用。使用高效液相色谱(HPLC)分析评估了包封效率。在两种不同 pH 值(5.5、7)下,进行了纳米制剂的胰岛素释放曲线研究,几乎模拟了胃肠道(GIT)的环境。
硅涂层 CS-DS NPs 表现出有趣的物理化学性质,例如 TEM 图像显示的合适的核粒径(145.31±33.15nm)、水动力直径(210±21nm)、高稳定性(由其 zeta 电位值-32±3.2mV 表示)和通过 AFM 评估的足够表面粗糙度。载胰岛素壳聚糖纳米粒(ICN)的包封效率(66.5%)高于载胰岛素壳聚糖复合物纳米粒(ICCN)。与未涂层 ICN 相比,硅涂层 ICN 在 pH 值(5.5 和 7)下表现出了胰岛素的控制释放曲线。
硅涂层 ICN 可以作为一种有效的口服递药系统候选物,克服了肽和蛋白质递药的常见障碍,实现了高稳定性和控释,可进一步应用。