Pluronic P123制备姜黄素聚合胶束及其体外抗B16细胞作用的研究

Kun-kai Su, Yunxu Yang, Qiuping Wu, Y. Mao, Ying Hu
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引用次数: 11

摘要

用Pluronic P123制备了姜黄素聚合物胶束,提高了姜黄素的溶解度和生物利用度。采用薄膜分散法制备了姜黄素p123胶束,采用高效液相色谱法测定了姜黄素的含量。采用正交设计优化包埋效率,确定最佳制备方法。通过透射电子显微镜、粒径分布、傅里叶变换和x射线衍射测定了胶束的微观形态、直径和药物填充量。采用透析法测定体外药物释放率。优化条件(姜黄素5 mg, Pluronic P123 150 mg,水10 mL,甲醇10 mL)下,姜黄素的包封率为94.7%,载药量为3.06%。圆形和椭圆形聚合物胶束的平均粒径为117.23±2.57 nm, zeta电位为7.87±2.50 mV,粒径分布均匀。根据x射线衍射和红外光谱分析,聚合物胶束以分子和非晶形式分散成嵌段共聚物。与药物溶液相比,姜黄素的聚合物胶束在体外表现出显著的缓释作用。采用(3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四氮唑)法体外检测姜黄素- p123对B16细胞的抗肿瘤作用。聚合物胶束的抗肿瘤作用高于姜黄素。所制备的姜黄素p123胶束提高了药物在水相中的溶解度。姜黄素聚合物胶束对肿瘤细胞具有持续的药物释放和良好的抑制作用,具有重要的作用和良好的研究价值。
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Preparation of Polymeric Micelles of Curcumin with Pluronic P123 and Assessment of Efficacy against B16 Cells In Vitro
Polymeric micelles of curcumin were obtained using Pluronic P123 to increase the solubility and bioavailability of curcumin. The curcumin-P123 micelles were prepared by a thin-film dispersion method and the content of curcumin was determined by high-performance liquid chromatography. The entrapment efficiency was optimized by an orthogonal design to determine the best preparation method. The microscopic morphology, diameter, and drugloaded amount of the micelles were determined by transmission electron microscopy, particle size distribution, Fourier transform, and X-ray diffraction. The in vitro drug release rates were measured by a dialysis method. The entrapment efficiency of curcumin was 94.7% and the loading capacity was 3.06% under optimized conditions (curcumin 5 mg, Pluronic P123 150 mg, water 10 mL, and methanol 10 mL). The average size and zeta potential of the round or ellipse polymeric micelles were 117.23 ± 2.57 nm and 7.87 ± 2.50 mV, respectively, with uniform particle size distribution. The polymeric micelles were dispersed into block copolymers in molecular and amorphous forms based on X-ray diffraction and FTIR analysis. The polymeric micelles of curcumin showed significant sustained drug release in vitro compared with a pharmaceutical solution. The anti-tumor efficacy of curcumin-P123 on B16 cells was assessed in vitro by a (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The antitumor effects of the polymeric micelles was higher than that of curcumin. The prepared curcumin-P123 micelles increased the drug solubility in the aqueous phase. The polymeric micelles of curcumin have an important effect and excellent research value because of their sustained drug release and excellent inhibitory effect on tumor cells.
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