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阿霉素自组装纳米粒的制备及其抗肿瘤活性的研究

Preparation and Research on the Aniti-Tumor Activity of Adriamycin Self-assembled Nanoparticles
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摘要 [目的]制备胆固醇基普鲁兰多糖阿霉素自组装纳米粒(Self-assembled ADM-loaded cholesterol modified pullulan nanoparticles,ADM-CHSP-SAN)并考察其体外抗肿瘤活性。[方法]以胆固醇基普鲁兰多糖(cholesterol-modified pullulan,CHSP)为载体,采用透析法制备ADM-CHSP-SAN,并测定其形态、粒径、Zeta电位、包封率和载药量,采用MTT法研究其抑制U251肿瘤细胞的活性作用。[结果]ADM-CHSP-SAN外观呈圆形或类圆形,平均粒径为(112.8±1.02)nm,Zeta电位为(-27.2±0.246)mV,包封率和载药量分别为(67.14±1.21)%和(7.65±0.58)%;体外释药行为符合Higuchi方程;给药剂量大于25μg.mL-1时,ADM-CHSP-SAN抑制U251肿瘤细胞的活性作用明显优于阿霉素溶液剂(P<0.01)。[结论]将阿霉素制备成ADM-CHSP-SAN可有效提高药物的抗肿瘤活性。 [Objective] To prepare adriamycin self-assembled nanoparticles, and study the in vivo anti-tumor activity. [Methods]The self-assembled adri- amycin loaded cholesterol-modified pulhilan nanoparticles were prepared by dialysis and were characterized by morphology for particle size,Zeta potential, entrapment efl^ciency,dmg loading content.They were incubated with U251 cells to assess the inhibition ability of the self-assembled adriamycin-loaded cholesterol-modified pulhilan nanoparticles. [Results]The morphology of self-assembled adriamycin loaded cholesterol-modified pullulan nanoparticles was spherical. The mean particle size, Zeta potential, entrapment e^ciency and drag loading were (112.8+1.02)nm,(-27.2+0.246)mV,(67.14_+1.21)% and (7.65+0.58)%, respectively.The profiles of release were expressed well by Higuchi equation. When the dosages were 25p^g'mL ' plus, the inhibiton ability against U251 was stronger than adriamycin solution(P〈0.01).[Conclusion]The self-assembled adriamycin loaded cholesterol-modified pullulan nanoparticles exhibited more cycitoxic activity against U251 than adriamycin solution.
出处 《浙江中医药大学学报》 CAS 2013年第8期951-955,共5页 Journal of Zhejiang Chinese Medical University
基金 浙江中医药大学科研基金(2012ZY16)~~
关键词 阿霉素 胆固醇基普鲁兰多糖 自组装纳米粒 体外释放 抗肿瘤 adriamycin cholesterol-modified pullulan self-assembled nanoparticles in vitro release antitumor
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