OBJECTIVE: To prepare anti-tumor drug H6 (lactone compound) polymeric micelles, and to investigate its in vitro anti-tumor effects. METHODS: Using mPEG2000-PCL4000 as carrier, H6/mPEG2000-PCL4000 micelles were prepared. Using particle size, PDI and 48 h whether to produce precipitation as indexes, feeding ratio, H6 concentration, volume ratio of organic solvent were screened. The encapsulation efficiency and drug-loading amount of micelle were all detected. MTT assay was used to detect the toxicity of micelles and H6 solution to human non-small cell lung cancer cell A549 and human lung cancer cell H460. RESULTS: The screened formulation was as follows as feeding ratio of 1 ∶ 25, H6 concentration of 2 mg/mL, the ratio of ethanol to chloroform of 1 ∶ 1 (V/V). The parameters of prepared H6/mPEG2000-PCL4000 micelles were as follows as particle size of (40.74±0.116 3) nm, PDI of (0.101±0.006), encapsulation efficiency of (94.87±0.016 3)%, drug-loading amount of (7.07±0.001 5)% (n=3). IC50 of micelles and H6 solution to A549 cell were 15.62 and 12.57 nmol/L; IC50 of micelles and H6 solution to H460 cell were 27.68 and 15.19 nmol/L. CONCLUSIONS: H6/mPEG2000-PCL4000 micelles are prepared successfully and show in vitro anti-tumor effects.
关键词
抗肿瘤药H6mPEG2000-PCL4000胶束抗肿瘤作用
Keywords
Anti-tumor drug H6mPEG2000-PCL4000MicellesAnti-tumor effect