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目的制备溴化双十二烷基二甲基铵(DMAB)修饰的载汉防己甲素(Tet)的聚乳酸-羟基乙酸共聚物(PLGA)纳米粒(DMAB-Tet-PLGA-NPs),考察其制备的影响因素,优化制备工艺,并对其理化性质、细胞毒性及细胞摄取进行研究。方法采用乳化分散溶剂挥发法制备DMAB-Tet-PLGA-NPs,运用均匀设计试验优化制备工艺,通过包封率、载药量、累积释药量等指标考察其载药特性;采用MTT比色法考察DMAB-Tet-PLGA-NPs对人肺腺癌细胞株A549的细胞毒性;采用定量定性法评价DMAB-Tet-PLGA-NPs细胞摄取率。结果制备的DMAB-Tet-PLGA-NPs平均粒径为(205.40±2.66)nm,表面带正电,呈规则的球形及椭圆形。药物包封率和载药量分别为(50.780±3.253)%和(2.130±0.035)%。体外释放实验显示DMAB-Tet-PLGA-NPs缓慢释药,48 h累积释药量64.56%。MTT实验表明DMAB-Tet-PLGA-NPs细胞毒性呈剂量及时间依赖性。定性定量细胞摄取实验证实DMAB-Tet-PLGA-NPs能较好地被细胞摄取。结论 DMAB-Tet-PLGA-NPs粒径大小均一,包封率高,体外释药表现出较好的缓释效果,易被细胞摄取,对A549细胞的活性有明显的抑制作用。
OBJECTIVE To prepare DMAB-Tet-PLGA nanoparticles (NPs) loaded with tetrandrine (Tet) modified with didodecyl dimethyl ammonium bromide (DMAB) Its preparation factors, optimize the preparation process, and its physical and chemical properties, cytotoxicity and cell uptake study. Methods DMAB-Tet-PLGA-NPs was prepared by emulsification-dispersion solvent evaporation method. The uniform design test was used to optimize the preparation process. The encapsulation efficiency, drug loading and cumulative release were investigated. The MTT colorimetric method The cytotoxicity of DMAB-Tet-PLGA-NPs on human lung adenocarcinoma cell line A549 was investigated. The uptake rate of DMAB-Tet-PLGA-NPs cells was evaluated by quantitative qualitative method. Results The average particle diameter of DMAB-Tet-PLGA-NPs prepared was (205.40 ± 2.66) nm. The surface of the DMAB-Tet-PLGA-NPs was positively charged with regular spherical and oval shapes. Drug entrapment efficiency and drug loading were (50.780 ± 3.253)% and (2.130 ± 0.035)%, respectively. In vitro release experiments showed that DMAB-Tet-PLGA-NPs release slowly, and the cumulative release amount at 48 h was 64.56%. MTT experiments showed that DMAB-Tet-PLGA-NPs cytotoxicity in a dose and time-dependent manner. Qualitative and quantitative cell uptake experiments confirmed that DMAB-Tet-PLGA-NPs can be well taken by cells. Conclusion The size of DMAB-Tet-PLGA-NPs is uniform, the entrapment efficiency is high, and release in vitro shows good sustained-release effect. It is easily absorbed by cells and obviously inhibits the activity of A549 cells.