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AEYLR小肽修饰的紫杉醇纳米结构脂质载体的制备及抗肿瘤效果评价
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| 篇名： | AEYLR小肽修饰的紫杉醇纳米结构脂质载体的制备及抗肿瘤效果评价 |
| TITLE： | |
| 摘要： | 目的：制备序列为丙氨酸-谷氨酸-酪氨酸-亮氨酸-精氨酸（简称为“AEYLR”）的小肽修饰的紫杉醇（PTX）纳米结构脂质载体（A-P-NLC），并对其体内外抗肿瘤效果进行评价。方法：采用熔融乳化-低温固化法制备纳米结构脂质载体（NLC）、PTX纳米结构脂质载体（P-NLC）和A-P-NLC，表征其外观形态、粒径、多分散指数（PDI）、Zeta电位，并检测其包封率、载药量及体外释放度；以NCI-H1299细胞和S180细胞为对象，采用CCK-8法对游离PTX、P-NLC、A-P-NLC（0.44～44.00 μg/mL，以PTX计）的细胞抑制作用进行考察，并计算其半数抑制浓度（IC50）；以S180荷瘤小鼠为模型动物，对游离PTX、P-NLC、A-P-NLC（5 mg/kg，以PTX计）的抑瘤效果进行评价。结果：P-NLC和A-P-NLC外观均呈类圆形、分布均匀；A-P-NLC的粒径、PDI、Zeta电位分别为（43.92±0.76）nm、0.203±0.034、（－19.77±1.16）mV，较P-NLC有所增加；A-P-NLC的包封率、载药量分别为（95.71±0.68）％、（1.97±0.25）％，较P-NLC有所降低；A-P-NLC在48 h内累积释放百分率达（35.17±2.08）％，较游离PTX表现出明显的缓释作用，且比P-NLC的释放更缓慢。与游离PTX和P-NLC比较，相同质量浓度的A-P-NLC对NCI-H1299细胞和S180细胞的抑制率大部分均显著升高，IC50值均显著降低；A-P-NLC给药处理的S180荷瘤小鼠无死亡现象，一般状态良好，且瘤体积显著缩小、瘤质量显著降低、瘤质量抑制率显著升高（P＜0.05或P＜0.01）。结论：A-P-NLC具有明显的缓释作用，其对NCI-H1299细胞和S180细胞的体外抑制作用以及对小鼠S180实体瘤的抑制作用均优于游离PTX和P-NLC，且毒性有所降低。 |
| ABSTRACT： | OBJECTIVE： To prepare Paclitaxel（PTX）nanostructured lipid carriers （NLC） modified by small peptide alanine-glutamic acid-tyrosine-leucine-arginine （AEYLR）， and to evaluate its anti-tumor effect in vitro and in vivo. METHODS： NLC， PTX-NLC （P-NLC） and AEYLR modified P-NLC （A-P-NLC） were prepared by emulsion evaporation-low temperature solidification curing method. Its appearance， particle size， multi-dispersion index（PDI） and Zeta potential were characterized，encapsulation rate，drug loading and in vitro drug release were detected respectively. Using NCI-H1299 and S180 cells as objects， CCK-8 method was adopted to investigate inhibitory effects of free PTX， P-NLC and A-P-NLC （0.44-44.00 μg/mL， by PTX） to those cells. The half inhibition concentration （IC50） was calculated. Using S180 tumor-bearing mice as model animal， anti-tumor effects of free PTX， P-NLC and A-P-NLC （5 mg/kg， by PTX） were evaluated. RESULTS： P-NLC and A-P-NLC were round-like and dispersed evenly. The particle size， PDI and Zeta potential of A-P-NLC were （43.92±0.76） nm， 0.203±0.034 and （－19.77±1.16） mV， which were all increased to certain extent， compared with P-NLC. The encapsulation efficiency and drug loading of A-P-NLC were （95.71±0.68）％ and（1.97±0.25）％， which were both decreased to certain extent， compared with P-NLC. The cumulative release rate of A-P-NLC was（35.17±2.08）％ within 48 h， showing significant sustained-release effect compared with free PTX； the release of A-P-NLC was slower than P-NLC. Compared with free PTX and P-NLC， inhibitory rates of same concentration of A-P-NLC to NCI-H1299 cells and S180 cells were almost increased significantly， while IC50 values were all decreased significantly. There was no death in S180 tumor-bearing mice treated with A-P-NLC and the general condition was good； the volume of tumors was significantly reduced， the mass of tumors was significantly reduced， and the inhibition rate of tumors was significantly increased （P＜0.05 or P＜0.01）. CONCLUSIONS： A-P-NLC has significantly sustained-release effects； its inhibitory rate to NCI-H1299 cells and S180 cells in vitro， and its inhibitory effects on S180 solid tumor in mice are all better than free PTX and P-NLC， while the toxicity is decreased to certain extent. |
| 期刊： | 2019年第30卷第6期 |
| 作者： | 韩翠艳，周建文，刘畅，马晓星，袁橙，董岩，金珊珊 |
| AUTHORS： | HAN Cuiyan，ZHOU Jianwen，LIU Chang，MA Xiaoxing，YUAN Cheng，DONG Yan，JIN Shanshan |
| 关键字： | AEYLR；小肽；紫杉醇；纳米结构脂质载体；抗肿瘤；小鼠 |
| KEYWORDS： | AEYLR； Small peptide； Paclitaxel； Nano- structured lipid carriers； Anti-tumor； Mice |
| 阅读数： | 460 次 |
| 本月下载数： | 5 次 |
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