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白屈菜红碱纳米粒的制备及体外抗黑色素瘤活性评价
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| 篇名： | 白屈菜红碱纳米粒的制备及体外抗黑色素瘤活性评价 |
| TITLE： | Preparation of Chelerythrine Nanoparticles and Evaluation of Anti-melanoma Activity in vitro |
| 摘要： | 目的：制备白屈菜红碱纳米粒（CHE-NPs），对其处方进行优化，并评价其体外释药行为及对黑色素瘤的抑制作用。方法：以甲氧基聚乙二醇-聚乳酸-羟基乙酸共聚物（mPEG-PLGA）为载体材料，采用纳米沉淀法制备CHE-NPs，采用高效液相色谱法和透析袋法测定包封率、载药量。以二者的总评归一（OD）值为因变量，以CHE投药量、mPEG-PLGA质量浓度、泊洛沙姆188（F68）浓度为自变量，采用Box-Behnken响应面设计优化CHE-NPs处方。检测最优处方所制CHE-NPs的粒径和Zeta电位，考察其体外释药特征，比较CHE原料药和CHE-NPs对小鼠B16黑色素瘤细胞存活率的影响并计算二者的半数抑制浓度。结果：最优处方为CHE投药量2mg、mPEG-PLGA质量浓度13mg/mL、F68浓度1.8％。以此所制CHE-NPs的平均包封率为（80.18±1.11）％，平均载药量为（11.36±0.28）％，平均OD值为0.96±0.04[与OD预测值（0.90）的相对偏差为6.67％]，粒径为（113.1±1.40）nm，Zeta电位为（－21.6±0.29）mV，多分散性指数为0.07±0.01（n＝3）。CHE对照品、CHE-NPs在孵育8h时的累积释放率分别为90.87％、68.68％，后者的体外释药行为符合Weibull动力学模型。CHE-NPs对B16黑色素瘤细胞的抑制作用显著强于CHE原料药，CHE-NPs和CHE原料药的24h半数抑制浓度分别为69.35、107.36μg/mL。结论：所制CHE-NPs具有缓释作用和较强的载药能力，同时增强了CHE对黑色素瘤的体外抑制作用。 |
| ABSTRACT： | OBJECTIVE：To prepare chelerythrine nanoparticles（CHE-NPs），optimize their formulation ，and evaluate its drug release behavior in vitro and its inhibitory effect on melanoma. METHODS ：Using methoxy polyethylene glycol-poly （lactic-co- glycolic acid ）（mPEG-PLGA）as carrier ，CHE-NPs were prepared by the nano-precipitation method. HPLC method and dialysis bag method were used to determine entrapment efficiency and drug loading. The formulation of CHE-NPs was optimized by Box-Behnken response surface design using overall desirability （OD）of them as dependent variables ，CHE dosage ，mPEG-PLGA concentration and poloxamer 188（F68）concentration as independent variables. The particle size and Zeta potential of CHE-NPs prepared by the optimal formulation were detected ；the characteristics of drug release in vitro were investigated ；the effects of CHE and CHE-NPs on survival rate of mice B 16 melanoma cells were compared ，and median inhibition concentrations （IC50）of them were calculated. RESULTS ：The optimal formulation included CHE of 2 mg，mPEG-PLGA of 13 mg/mL，F68 of 1.8％. Average entrapment efficiency rate of CHE-NPs prepared by the optimal formulation was （80.18±1.11）％，average drug loading was （11.36±0.28）％，average OD value was 0.96±0.04 [the relative deviation from predicted value （0.90）of OD was 6.67％]； particle size was （113.1±1.40）nm，and Zeta potential was （－21.6±0.29）mV；polydispersity index was 0.07±0.01（n＝3）； accumulative release rates of CHE control and CHE-NPs were 90.87％ and 68.68％ within 8 h，and drug release behavior in vitro of the latter was in accordance with Weibull kinetic model. Inhibitory effect of CHE-NPs on B 16 melanoma cells was significantly stronger than that of CHE ；the 24 h IC 50 of CHE-NPs and CHEwere 69.35 and 107.36 μg/mL，respectively. CONCLUSIONS ：The prepared CHE-NPs show good sustained-effect and high capacity of drug loading ，and strengthen the inhibitory effect of CHE on melanoma. |
| 期刊： | 2021年第32卷第24期 |
| 作者： | 杨锦，韩伟，张永萍，陈晓兰，李哲，刘杰，吴静澜 |
| AUTHORS： | YANG Jin，HAN Wei，ZHANG Yongping ，CHEN Xiaolan ，LI Zhe，LIU Jie，WU Jinglan |
| 关键字： | 白屈菜红碱；黑色素瘤；抑瘤作用；甲氧基聚乙二醇-聚乳酸-羟基乙酸共聚物；纳米粒；Box-Behnken响应面设计 |
| KEYWORDS： | Chelerythrine；Melanoma；Anti-tumor effect ； |
| 阅读数： | 186 次 |
| 本月下载数： | 3 次 |
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