"Grigore T. Popa" University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Technology, University street, no. 16, 700115 Iaşi, Romania; "Gheorghe Asachi" Technical University, Faculty of Chemical Engineering and Protection of the Environment, Department of Natural and Synthetic Polymers, Iaşi, Romania.
Faculty of Dental Medicine, University "Apollonia", Pacurari street, no. 11, Iași, Romania.
Int J Biol Macromol. 2020 Mar 15;147:629-642. doi: 10.1016/j.ijbiomac.2019.12.247. Epub 2020 Jan 2.
Curcumin has essential therapeutic benefits, but it is insoluble in water and thus has low bioavailability. This study aimed to immobilize curcumin into new polysaccharide-based microparticles (gellan, i-carrageenan, and chitosan) to increase its stability and bioavailability. Curcumin-loaded complex microparticles were obtained from three polysaccharides, of different ionic character, by ionic cross-linking and polyelectrolyte complexation. The immobilization efficiency was between 85.75% and 97.25%. The microparticles were characterized morphologically by SEM, and it was observed that the microparticles containing the i-carrageenan had a more pronounced porosity of the matrix. The swelling degree values at pH = 7.4 were superior to those obtained at pH = 6.8 or pH = 2 and depend on both the cross-linking degree and particles morphology. The polysaccharides microparticles, curcumin, and constituent polysaccharides were characterized by FT-IR spectroscopy. The curcumin release kinetics was studied in three different pH media, and the release efficiency ranged between 65.1% and 97.9% at pH = 7.4, between 60.2% and 82.2% at pH = 6.8 and between 56.1% and 64.0% at pH = 2. These microparticles can be intended for oral administration, having as therapeutic target the colon, for the controlled release of curcumin, since they can overcome the gastric barrier without the degradation of the active principle, which is protected by the polymer matrix.
姜黄素具有重要的治疗益处,但它不溶于水,因此生物利用度低。本研究旨在将姜黄素固定在新的多糖基微球(结冷胶、 ι-卡拉胶和壳聚糖)中,以提高其稳定性和生物利用度。通过离子交联和聚电解质络合,从三种具有不同离子特性的多糖中获得负载姜黄素的复合微球。固定化效率在 85.75%至 97.25%之间。用 SEM 对微球进行形态学表征,观察到含有 ι-卡拉胶的微球的基质具有更明显的多孔性。在 pH=7.4 时的溶胀度值优于在 pH=6.8 或 pH=2 时的值,这取决于交联度和颗粒形态。通过傅里叶变换红外光谱法对多糖微球、姜黄素和组成多糖进行了表征。在三种不同的 pH 介质中研究了姜黄素的释放动力学,在 pH=7.4 时的释放效率在 65.1%至 97.9%之间,在 pH=6.8 时在 60.2%至 82.2%之间,在 pH=2 时在 56.1%至 64.0%之间。这些微球可用于口服给药,靶向结肠,用于姜黄素的控制释放,因为它们可以克服胃屏障,而不会降解活性物质,活性物质被聚合物基质保护。