中文摘要：

目的 以人卵巢癌细胞SKOV3为模型,研究负载多烯紫杉醇（TXT）的新型生物素接枝改性聚乳酸纳米粒（TXT-BPLA NPs）的体外抗肿瘤作用。 方法 以不同剂量TXT-BPLA NPs（1、10、100、1 000、10 000 nmol/L）处理SKOV3细胞不同时间（12、24、48、72、96、120 h）后用CCK-8检测细胞增殖抑制率，流式细胞仪检测细胞凋亡率，Western blot检测caspase-3表达。 结果 在10～10 000 nmol/L浓度范围内，相同时间点下，TXT和TXT-BPLA NPs对SKOV3细胞生长的抑制率均呈现出剂量依赖性。在相同浓度下，TXT组在24 h和48 h对SKOV3细胞的增殖抑制率、凋亡率及caspase-3的表达均明显高于TXT-BPLA NPs组（P〈0.05）；72 h后，TXT-BPLA NPs组对SKOV3细胞的增殖抑制率、凋亡率及caspase-3的表达均明显高于TXT组（P〈0.05）。 结论 与TXT相比，TXT-BPLA NPs能够更加持续地抑制SKOV3细胞的增殖，并促进caspase-3介导的细胞凋亡，具有更强的持续性抗肿瘤作用。

英文摘要：

Objective To determine the antitumor effects of the novel docetaxel （TXT）-loaded biotinylated poly （lactic acid） nanoparticles （TXT-BPLA NPs） on human ovarian cancer cell line SKOV3. Methods SKOV3 cells were cultured with TXT-BPLA NPs at different concentrations （1, 10, 100, 1 000 and 10 000 nmol/L） and durations （12, 24, 48, 72, 96 and 120 h） respectively. Then proliferation and apoptosis of SKOV3 cells were determined by CCK-8 assay and flow cytometry, respectively. The apoptosisrelated protein caspase-3 was measured by Western blotting. Results Both TXT and TXT-BPLA NPs resulted in inhibited proliferation in SKOV3 cells in a dose-dependent manner when the concentration was given at 10 to 10 000 nmol/L within same duration. Under the same dose, TXT-treated SKOV3 cells for 24 and 48 h had obviously higher proliferative rate, apoptotic rate and caspase-3 expression than the cells treated by TXT-BPLA NPs （P〈0.05）, while these phenomena was reversed when the treatment time was prolonged to 72 h （P〈0.05）. Conclusion Comparing with TXT, TXT-BPLA NPs could more persistently inhibit the proliferation of SKOV3 cells and promote caspase-3-mediated apoptosis. Thus, TXT-BPLA NPs, as a new nanometer drug, has a special application value for the therapy of ovarian cancer.