Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Santa Catarina, Campus Trindade, Florianópolis, 88040-970, Brazil.
J Biomed Nanotechnol. 2011 Jun;7(3):406-14. doi: 10.1166/jbn.2011.1296.
Curcumin is a polyphenol obtained from the plant Curcuma longa (called turmeric) that displays several pharmacological activities, including anti-inflammatory, antioxidant, antimicrobial and antitumoral activity, but clinical use has been limited by its poor solubility in water and, consequently, minimal systemic bioavailability. We have therefore formulated the drug into nanocarrier systems in an attempt to improve its therapeutic properties. This study evaluates the effect of intraperitoneally administered nanocapsules containing curcumin on subcutaneous melanoma in mice inoculated with B16-F10 cells, and on the cytotoxicity activity against B16-F10 cells in vitro. Phagocytic uptake of formulations was also evaluated upon incubation with macrophage J774 cells by fluorescence microscopy. Lipid and polymeric nanocapsules were prepared by the phase inversion and nanoprecipitation methods, respectively. The uptake of the lipid nanocapsules prepared using Solutol HS15 was significantly reduced in J774 cells. Curcumin, as free drug or as drug-loaded nanocapsules, was administrated at a dose of 6 mg/kg twice a week for 21 days. Free drug and curcumin-loaded nanocapsules significantly reduced tumor volume (P < 0.05 vs. control), but no difference was found in the antitumor activity displayed by lipid and polymeric nanocapsules. This assumption was supported by the in vitro study, in which free curcumin as well as loaded into nanocapsules caused significant reduction of cell viability in a concentration- and time-dependent manner.
姜黄素是一种从植物姜黄(称为 turmeric)中提取的多酚,具有多种药理活性,包括抗炎、抗氧化、抗菌和抗肿瘤活性,但由于其在水中的溶解度差,因此临床应用受到限制,导致其系统生物利用度极低。因此,我们将该药物制成纳米载体系统,试图改善其治疗性能。本研究评估了腹腔内给予含有姜黄素的纳米胶囊对皮下接种 B16-F10 细胞的小鼠黑色素瘤的影响,以及对体外 B16-F10 细胞的细胞毒性活性的影响。通过荧光显微镜观察与巨噬细胞 J774 细胞孵育时,还评估了制剂的吞噬摄取。脂质和聚合纳米胶囊分别通过相转化和纳米沉淀方法制备。使用 Solutol HS15 制备的脂质纳米胶囊在 J774 细胞中的摄取明显减少。姜黄素作为游离药物或载药纳米胶囊以 6mg/kg 的剂量每周两次给药 21 天。游离药物和载药纳米胶囊均显著降低肿瘤体积(P<0.05 与对照组相比),但脂质和聚合纳米胶囊显示的抗肿瘤活性无差异。体外研究支持这一假设,游离姜黄素以及负载到纳米胶囊中的姜黄素均以浓度和时间依赖的方式显著降低细胞活力。