FAN Ziliang,JIN Binghui,XU Xiafang, et al. Preparation and in vitro antitumor evaluation of curcumin-loaded micelles[J]. JOURNAL OF WEZHOU MEDICAL UNIVERSITY, 2017, 47(9): 625-630,636.
Abstract：Objective: To prepare a novel polymer micelles encapsulating curcumin (CUR) and evaluate its anti-tumor effect on glioma in vitro. Methods: A novel polymer, undecenoic acid-grafted-ε-polylysine (ε-PLL-UNA), was synthesized, and its chemical structure was confirmed by 1H-NMR and FT-IR. The CAC value of ε-PLL-UNA polymer was also detected by pyrene fluorescence probe. CUR-loaded micelle was prepared by dialysis method using ε-PLL-UNA as materials, and its particle size and morphology were also studied under dynamic light scattering (DLS) and transmission electron microscope (TEM), respectively. Furthermore, in vitro drug release profiles from CUR-Micelles were explored by dynamic dialysis method. Finally, the cellular toxicity against C6 cells spheroids and the cellular uptake of CUR-Micelles were evaluated. Results: ε-PLL-UNA polymer was successfully synthesized and able to self-assemble into micelles above its CAC value of 0.19 g/L. CUR-loaded micelle had a mean diameter of (60.6±2.1)nm, and zeta potential of (28.2±5.6)mV, exhibiting the spherical shape determined by TEM. Drug loading content and drug loading efficiency for CUR-loaded micelle were high up to 12.22%±2.13% and 85.12%±3.64%, respectively. About 84% of CUR were released from the micelles in 48 hours. CUR-loaded micelle can promote the cellular uptake of its encapsulated CUR by C6 cells, displaying a significantly higher cytotoxicity against C6 cells. Besides, the growth of C6 cells spheroids was significantly inhibited by CUR-loaded micelle. Conclusion: CUR is efficiently encapsulated in ε-PLL-UNA micelles with a particle size of less than 100 nm, which improved the cellular uptake of C6 cells. The sustained-release of CUR from CUR-loaded micelle is also observed. More importantly, CUR-Micelles has superior growth inhibition against C6 cells spheroids.
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