薄膜超声法制备姜黄素-EGCG固体脂质纳米粒及其体外抗肿瘤活性的研究

Preparation of curcumin-EGCG solid lipid nanoparticles by film ultrasonic wave dissolving techniques and its preliminary evaluation of in-vitro anti-tumor activity

目的优选薄膜超声法制备姜黄素-EGCG固体脂质纳米粒的工艺,测定有效成分,并初步评价其抗肿瘤活性。方法以包埋率和载药量为指标,考察姜黄素与EGCG复合物、硬脂酸、卵磷脂、吐温80用量等因素对包封率和载药量的影响,并通过正交试验优化处方及制备工艺;通过MTT法测定不同浓度下姜黄素、EGCG单体及姜黄素-EGCG固体脂质纳米粒对CT-26和Hela肿瘤细胞的抑制作用。结果最佳工艺为:姜黄素与EGCG复合物用量40 mg、硬脂酸120 mg、卵磷脂60 mg、1.0%吐温80 10 m L,所得姜黄素-EGCG固体脂质纳米粒平均粒径为90.9±1.57 nm(PDI=0.147±0.01),Zeta电位为-43.6±1.93 m V,包埋率为93.6%±0.45%,载药量为13.5%±0.38%。结论优化后的处方有较高的包埋率和载药量,工艺稳定可行;姜黄素-EGCG固体脂质纳米粒对CT-26、Hela肿瘤细胞较单独给药有更强的抑制作用。

OBJECTIVE To optimize the technique for preparing eurcumin - EGCG solid nanopartieles （ Cur - EGCG - SLNs） by film- ultrasonic wave dissolving techniques, establish a method for determining the content of active components in Cur - EGCG - SLNs, and make a preliminary evaluation of in vitro anti - tumor activity. METHODS The influence of various factors, including the consumption of curcumin and EGCG, stearie acid,lecithin and tween - 80 （ 1% ）, and their effects on the entrapment efficiency and theratio of loading drug were investigated. And the optimum formula was selected through orthogonal design test. The inhibitory effect of curcumin, EGCG and Cur - EGCGG - SLNs to CT - 26 and Hela cells was determinined at the different concentrations. RESULTS Cur- EGCG -SLNs had a good size distribution under the condition of 40 mg of curcumin -EGCG, 120 mg of stearic acid,60 mg of lecithin, and 10 mL of 1.0% tween - 80, the mean particle size diameter and Zeta potential were 90.9±1. 57 nm （ PDI 0. 147 ± 0.01 ） and -43.6 ± 1.93 mV,the average entrapment efficiency and the ratio of loading drag approached 93.6% ± 0.45% and 13.5% ± 0. 38% ,respectively. CONCLUSION The technique for preparing Cur - EGCG - SLNs by film - ultrasonic wave dissolving techniques is feasible, and Cur - EGCG - SLNs reflects a better inhibitory effect to CT - 26 and Hela cells.