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北京中医药大学中药学院,北京 102488
Received:25 March 2024,
Revised:2024-07-26,
Accepted:29 July 2024,
Published:30 November 2024
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王晓静,郭子硕,张海桐,等.紫杉醇PLGA纳米粒的表征及体外抗肿瘤作用研究[J].中国药房,2024,35(22):2721-2725.
WANG Xiaojing,GUO Zishuo,ZHANG Haitong,et al.Characterization of paclitaxel-PLGA nanoparticles and their antitumor effects in vitro[J].ZHONGGUO YAOFANG,2024,35(22):2721-2725.
王晓静,郭子硕,张海桐,等.紫杉醇PLGA纳米粒的表征及体外抗肿瘤作用研究[J].中国药房,2024,35(22):2721-2725. DOI: 10.6039/j.issn.1001-0408.2024.22.03.
WANG Xiaojing,GUO Zishuo,ZHANG Haitong,et al.Characterization of paclitaxel-PLGA nanoparticles and their antitumor effects in vitro[J].ZHONGGUO YAOFANG,2024,35(22):2721-2725. DOI: 10.6039/j.issn.1001-0408.2024.22.03.
目的
2
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
2
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Annexin Ⅴ-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
2
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7 d时,其粒径无明显变化,平均PDI(放置1、2、4、7 d)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11.2 μg/mL时)显著降低,凋亡率和G
2
期细胞比例均显著升高(
P
<0.05)。
结论
2
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。
OBJECTIVE
2
To characterize paclitaxel nanoparticles (PTX-PLGA-NPs) and evaluate their
in vitro
inhibitory effect on Lewis lung cancer cells.
METHODS
2
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
2
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 apopt
osis rate and the proportion of G
2
phase cells were significantly increased (
P
<0.05).
CONCLUSIONS
2
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.
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