Department of Pharmacy, The Second Affiliated Hospital of Wenzhou Medical College, Zhejiang Province 325027, Wenzhou City, China.
J Microencapsul. 2013;30(6):538-45. doi: 10.3109/02652048.2012.758182. Epub 2013 Mar 14.
Biotin was conjugated on poloxamer to prepare biotin-poloxamer (BP) conjugate micelles for chemotherapeutics. Epirubicin (EPI) was encapsulated in BP micelles. The EPI-loaded BP micelles were characterized in terms of size, ζ-potential, morphology, drug loading, drug encapsulation and drug release. Marrow leukemic HL-60 cells were used for evaluating the in vitro cytotoxicity of EPI-loaded BP micelles. Nude mice were axillainoculated subcutaneously HL-60 cells to establish tumour model for investigating the inhibition effects of EPI-loaded BP micelles. From the results, the sizes of these nanoparticles were about 100 nm. Fluorescence microscope observation supported the enhanced cellular uptake of the micelles. The order of the inhibition on tumour volume growth was: EPI-loaded BP micelles >EPI-loaded MATP micelles >EPI-loaded poloxamer micelles >EPI. BP micelles showed significant antitumour activity and low toxicity, compared with the non-targeted micelles. With the advantage of EPR effect and tumour-targeting potential, BP conjugate micelles might be developed as a new system for chemotherapeutics.
生物素偶联到泊洛沙姆上以制备用于化疗的生物素-泊洛沙姆（BP）缀合物胶束。表阿霉素（EPI）被包封在 BP 胶束中。从粒径、ζ 电位、形态、载药量、包封率和体外释放度等方面对载 EPI 的 BP 胶束进行了评价。骨髓白血病 HL-60 细胞用于评价载 EPI 的 BP 胶束的体外细胞毒性。荷瘤裸鼠皮下接种 HL-60 细胞，建立肿瘤模型，考察载 EPI 的 BP 胶束的抑制作用。结果表明，这些纳米粒子的粒径约为 100nm。荧光显微镜观察支持了胶束的增强细胞摄取。抑制肿瘤体积生长的顺序为：载 EPI 的 BP 胶束＞载 EPI 的 MATP 胶束＞载 EPI 的泊洛沙姆胶束＞EPI。与非靶向胶束相比，BP 胶束具有显著的抗肿瘤活性和低毒性。BP 缀合物胶束具有 EPR 效应和肿瘤靶向潜力，可能被开发为一种新的化疗系统。
