Laboratory of Polymer Materials, Faculty of Chemistry, University of Sciences and Technology Houari Boumediene (USTHB), BP 32, El Alia, Algiers 16111, Algeria.
Laboratory of Polymer Materials, Faculty of Chemistry, University of Sciences and Technology Houari Boumediene (USTHB), BP 32, El Alia, Algiers 16111, Algeria.
Int J Biol Macromol. 2024 Apr;263(Pt 2):130389. doi: 10.1016/j.ijbiomac.2024.130389. Epub 2024 Feb 24.
Curcumin, a bioactive compound derived from the rhizome of Curcuma longa, has gained widespread attention for its potential therapeutic properties, including anti-inflammatory, antioxidant and anticancer effects. However, its poor aqueous solubility, instability and limited bioavailability have hindered its clinical applications. New beads formulations based on sodium alginate biopolymer (SA) and poly vinyl alcohol (PVA) were successfully prepared and evaluated as a potential drug vehicle for extended release of curcumin (Cur). Pristine and curcumin loaded calcium alginate/poly vinyl alcohol beads (CA/PVA and CA/PVA/Cur) at different compositions of SA and PVA were prepared by an ionotropic gelation method of SA followed by two freeze-thawing (FT) cycles for further crosslinking of PVA. Characterization techniques, such as scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), UV-Visible spectroscopy, thermogravimetric analysis (TGA) and x-ray diffraction (XRD) were used to confirm the successful microencapsulation of curcumin within the CA/PVA microcapsules. Furthermore, the swelling of pristine beads, pH-sensitive properties and in vitro release studies of curcumin loaded beads were investigated at 37 °C in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and simulated colonic fluid (SCF). The effect of the polymer blend ratio, the encapsulation efficiency (EE %) of curcumin, the loading capacity (LC μg/mg), the sphericity factor (SF), the antioxidant activity of the elaborated beads and their antimicrobial properties against bacteria and fungi were just as much evaluated. The obtained results indicate that the swelling and the behavior of the developed beads were influenced by the pH of the test medium and the PVA content. The introduction of PVA into the SA matrix greatly enhanced the physicochemical properties, the encapsulation efficiency and the loading capacity of the elaborated microparticles. Results also suggested that the antioxidant activity of the loaded beads (CA/PVA/Cur) showed a higher DPPH radical scavenging activity while the bacterial and fungal strains proved sensitive to the different formulations used in the assay. Moreover, the important drug encapsulation efficiency and the sustainable drug release of these materials make them promising for the development of new drug carrier systems for colon targeting.
姜黄素是一种从姜黄根茎中提取的生物活性化合物，因其具有抗炎、抗氧化和抗癌等潜在治疗特性而受到广泛关注。然而，其较差的水溶性、不稳定性和有限的生物利用度限制了其临床应用。本文成功制备了基于海藻酸钠生物聚合物（SA）和聚乙烯醇（PVA）的新型珠粒制剂，并将其作为姜黄素（Cur）延长释放的潜在药物载体进行了评估。通过 SA 的离子凝胶化方法以及随后的两次冻融（FT）循环进一步交联 PVA，制备了不同 SA 和 PVA 组成的纯 CA/PVA 和 CA/PVA/Cur 负载钙藻酸盐/聚乙烯醇珠粒（CA/PVA 和 CA/PVA/Cur）。使用扫描电子显微镜（SEM）、傅里叶变换红外光谱（FTIR）、紫外可见光谱、热重分析（TGA）和 X 射线衍射（XRD）等表征技术来确认姜黄素在 CA/PVA 微胶囊内的成功微封装。此外，还研究了纯珠粒的溶胀、pH 敏感性以及载有姜黄素的珠粒在模拟胃液（SGF）、模拟肠液（SIF）和模拟结肠液（SCF）中的体外释放。还评估了聚合物共混比、姜黄素的包封效率（EE%）、载药量（LCμg/mg）、球形因子（SF）、所制得珠粒的抗氧化活性以及它们对细菌和真菌的抗菌性能。结果表明，珠粒的溶胀和行为受测试介质的 pH 和 PVA 含量的影响。PVA 引入到 SA 基质中极大地增强了所制得的微粒子的物理化学性质、包封效率和载药量。结果还表明，负载珠粒（CA/PVA/Cur）的抗氧化活性显示出更高的 DPPH 自由基清除活性，而细菌和真菌菌株对试验中使用的不同制剂敏感。此外，这些材料的重要药物包封效率和可持续药物释放使它们有望成为用于结肠靶向的新型药物载体系统的开发。
