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紫杉醇PLGA纳米粒的表征及体外抗肿瘤作用研究
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| 篇名： | 紫杉醇PLGA纳米粒的表征及体外抗肿瘤作用研究 |
| TITLE： | Characterization of paclitaxel-PLGA nanoparticles and their antitumor effects in vitro |
| 摘要： | 目的 表征紫杉醇纳米粒（PTX-PLGA-NPs），并评价其对Lewis肺癌细胞的体外抑制作用。方法对以乳化溶剂挥发法所制PTX-PLGA-NPs的粒径、多分散性指数（PDI）、Zeta电位、微观形态、包封率、载药量、紫外-可见光吸收特性、稳定性等进行表征；以小鼠Lewis肺癌细胞为对象，以PTX对照品为参照，分别采用CCK-8法、Calcein-AM/PI双染法检测PTX-PLGA-NPs的细胞毒性和体外杀伤活性，分别采用AnnexinⅤ-FITC/PI染色法、PI染色法评估PTX-PLGA-NPs对细胞凋亡及周期的影响。结果PTX-PLGA-NPs呈类球形，平均粒径为（172.03±0.95）nm，PDI为0.098±0.012，Zeta电位为（－1.76±0.02）mV；包封率和载药量分别为（52.32±0.66）%、（7.07±0.18）%，紫外-可见光吸收特征不受载体聚乳酸-羟基乙酸共聚物的影响；4℃下避光放置7d时，其粒径无明显变化，平均PDI（放置1、2、4、7d）均小于0.3。与PTX对照品组相比，PTX-PLGA-NPs组有更多细胞处于死亡状态，其存活率（当PTX质量浓度为11.2μg/mL时）显著降低，凋亡率和G2期细胞比例均显著升高（P＜0.05）。结论所制PTX-PLGA-NPs粒径均一、分散均匀、性质稳定，对肺癌细胞的体外杀伤作用较PTX强。 |
| ABSTRACT： | OBJECTIVE To characterize paclitaxel nanoparticles （PTX-PLGA-NPs） and evaluate their in vitro inhibitory effect on Lewis lung cancer cells. METHODS The PTX-PLGA-NPs prepared by the emulsion-solvent evaporation method were characterized in terms of particle size， polydispersity index （PDI）， Zeta potential， microscopic morphology， encapsulation efficiency， drug loading， ultraviolet-visible absorption characteristics and stability. Using mouse Lewis lung cancer cells as the subjects and paclitaxel reference substance as the control， the cytotoxicity and in vitro killing activity of PTX-PLGA-NPs were detected using CCK-8 method and Calcein-AM/PI double staining method， respectively. The effects of PTX-PLGA-NPs on cell apoptosis and cell cycle were assessed by Annexin Ⅴ-FITC/PI staining method and PI staining method， respectively. RESULTS PTX-PLGA-NPs were spherical with an average particle size of （172.03±0.95） nm， PDI of 0.098±0.012， and Zeta potential of （－1.76±0.02） mV. The encapsulation efficiency and drug loading were （52.32±0.66）% and （7.07±0.18）%， respectively， and the ultraviolet-visible absorption characteristics were not affected by the carrier polylactic-co-glycolic acid. When stored in the dark at 4 °C for 7 days， no significant change was noted in particle size， and the average PDI （after 1， 2， 4 and 7 days of storage） was under 0.3. Compared with the paclitaxel reference substance group， the PTX-PLGA-NPs group had more cells in a state of death， the survival rate （at the PTX concentration of 11.2 μg/mL） was significantly decreased， and both the apoptosis rate and the proportion of G2 phase cells were significantly increased （P＜0.05）. CONCLUSIONS The prepared PTX-PLGA-NPs indicate homogeneity in particle size， uniform dispersion， stable properties， and stronger in vitro killing effect on lung cancer cells than PTX. |
| 期刊： | 2024年第35卷第22期 |
| 作者： | 王晓静；郭子硕；张海桐；陈宛灵；李加玲；杜守颖；李鹏跃 |
| AUTHORS： | WANG Xiaojing，GUO Zishuo，ZHANG Haitong，CHEN Wanling，LI Jialing，DU Shouying，LI Pengyue |
| 关键字： | 紫杉醇；聚乳酸-羟基乙酸共聚物；纳米粒；表征；Lewis肺癌细胞；体外抗肿瘤作用 |
| KEYWORDS： | paclitaxel； polylactic-co-glycolic acid； nanoparticles； characteristics； Lewis lung cancer cells； antitumor effects in vitro |
| 阅读数： | 6 次 |
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