Arli Osman Tayyar, Gök Yaşar, Gök Halil Zeki
Department of Chemistry, Faculty of Science and Letters, Burdur Mehmet Akif Ersoy University, Burdur, Turkiye.
Turk J Chem. 2023 Aug 13;47(6):1518-1528. doi: 10.55730/1300-0527.3632. eCollection 2023.
Studies on natural products with anticancer properties have gained more importance in recent years in order to not damage healthy tissues during cancer treatments or to perform the treatment causing the least damage. Curcumin is a common natural product with anticancer properties, but its low solubility, instability, and bioavailability have limited its use in clinical applications in cancer research. As a proposed solution to this problem, a new mesoporous organosilica nanocarrier () functionalized with a 1,2-diphenylethane-1,2-diamine structure capable of pH-controlled release was prepared in this study. was characterized by TGA, BET, XRD, FT-IR, and SEM-EDS analyses. Dispersion of into curcumin stock solution in ethanol afforded a curcumin-loaded system. Elevated loading capacity and pH-controlled release were provided by the Schiff base reaction that occurred during loading of curcumin with 1,2-diphenylethane-1,2-diamine placed on the silica wall of the nanocarrier system. The encapsulation efficiency was 25% for . In in vitro release experiments, curcumin release from the system was 0.5% at physiological and endosomal pH values. The resulting low release percentage indicates the presence of very strong interactions between the nanocarrier and curcumin. This strong interaction showed that nanocarrier could carry 99.5% of the curcumin without leakage under physiological and endosomal pH conditions without using pore capping agents. At a lower acidic pH value (pH 4.5), 26.3% curcumin release was obtained. These findings showed that the cumulative release of curcumin from the system can be achieved in a long-term and pH-controlled manner.
近年来，对具有抗癌特性的天然产物的研究变得越发重要，目的是在癌症治疗过程中不损害健康组织，或者进行损害最小的治疗。姜黄素是一种常见的具有抗癌特性的天然产物，但其低溶解度、不稳定性和生物利用度限制了它在癌症研究临床应用中的使用。作为对该问题的一种解决方案，本研究制备了一种新型的介孔有机硅纳米载体（），其用能够进行pH控制释放的1,2 - 二苯基乙烷 - 1,2 - 二胺结构进行了功能化。通过热重分析（TGA）、比表面积分析（BET）、X射线衍射分析（XRD）、傅里叶变换红外光谱分析（FT - IR）和扫描电子显微镜 - 能谱分析（SEM - EDS）对进行了表征。将分散到乙醇中的姜黄素储备溶液中得到了负载姜黄素的系统。纳米载体系统硅壁上放置的1,2 - 二苯基乙烷 - 1,2 - 二胺在负载姜黄素过程中发生的席夫碱反应提供了提高的负载能力和pH控制释放。的包封效率为25%。在体外释放实验中，在生理和内体pH值下，姜黄素从系统中的释放率为0.5%。由此产生的低释放百分比表明纳米载体与姜黄素之间存在非常强的相互作用。这种强相互作用表明，在不使用孔封闭剂的情况下，纳米载体在生理和内体pH条件下可以携带99.5%的姜黄素而不泄漏。在较低的酸性pH值（pH 4.5）下，获得了26.3%的姜黄素释放率。这些发现表明，姜黄素从系统中的累积释放可以以长期且pH控制的方式实现。
