Saka Ongun Mehmet, Aygüler Cemre İrem, Özdemir Neval Sevinç, Sürücü Bilge, Çakırlı Egemen, Nemutlu Emirhan, Demirbolat Gülen Melike
Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, 06560 Ankara, Türkiye.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Acıbadem Mehmet Ali Aydınlar University, 34752 Istanbul, Türkiye.
Pharmaceuticals (Basel). 2025 Mar 27;18(4):470. doi: 10.3390/ph18040470.
: Curcumin has well-established efficacy in a variety of disorders due to its prominent antioxidant, antiaging, anti-inflammatory, chemosensitizing, and anticancer activities. Despite its numerous benefits, curcumin exhibits low bioavailability mainly due to its poor solubility, poor absorption, rapid metabolism, and quick excretion, consequently limiting its clinical applications. In this study, we investigated the most convenient ingredients in SLNs to enhance curcumin's solubility by examining the effects of multiple independent variables simultaneously using an experimental design. : After curcumin's saturation solubility was investigated, SLN formulations were produced. The optimum formulation was determined with the help of experimental design. The SLNs were characterized in terms of the particle size and distribution, zeta potential, shape, entrapment efficiency, drug loading capacity, and drug release. The cell viability and cell internalization were also evaluated. : An impressive synergistic effect was achieved with the combination of Brij and Gelucire 48/16, which increased curcumin's solubility in water by 452.5 times. Curcumin-loaded SLNs were successfully produced with a spherical shape and particle size of 389.3 ± 9.95 nm. The encapsulation efficiency was directly proportionate to the amount of curcumin and the stirring speed. Curcumin in the SLNs entered the cancer cells more easily than curcumin alone. : Our results demonstrate that the quantity of surfactant is a significant factor influencing the efficiency of drug loading. Finally, the 3:1 (Brij-Gelucire48/16) ratio markedly enhanced the loading efficiency. The cellular internalization and, consequently, the anticancer efficacy against adenocarcinomic human alveolar basal epithelial cells were improved with SLNs. This could be a promising approach for lipid-based colloidal drug delivery systems.
姜黄素因其显著的抗氧化、抗衰老、抗炎、化学增敏和抗癌活性，在多种疾病中具有公认的疗效。尽管姜黄素益处众多，但其生物利用度低，主要原因是其溶解度差、吸收不良、代谢快和排泄迅速，因此限制了其临床应用。在本研究中，我们通过实验设计同时考察多个自变量的影响，研究了固体脂质纳米粒（SLNs）中最方便的成分以提高姜黄素的溶解度。：在研究姜黄素的饱和溶解度后，制备了SLN制剂。借助实验设计确定了最佳配方。对SLNs的粒径及分布、zeta电位、形状、包封率、载药量和药物释放进行了表征。还评估了细胞活力和细胞内化情况。：Brij和Gelucire 48/16的组合产生了令人印象深刻的协同效应，使姜黄素在水中的溶解度提高了452.5倍。成功制备了负载姜黄素的SLNs，其呈球形，粒径为389.3±9.95nm。包封率与姜黄素的量和搅拌速度成正比。SLNs中的姜黄素比单独的姜黄素更容易进入癌细胞。：我们的结果表明，表面活性剂的量是影响载药效率的一个重要因素。最后，3:1（Brij-Gelucire48/16）的比例显著提高了负载效率。SLNs提高了细胞内化，从而提高了对人肺泡基底上皮腺癌细胞的抗癌疗效。这可能是基于脂质的胶体药物递送系统的一种有前景的方法。
