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 ;
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