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两性霉素B聚氰基丙烯酸正丁酯纳米粒的制备及小鼠体内分布研究
徐楠[1]邹豪[2]范国荣[3]温海[1]陈江汉[1]
0
([1]第二军医大学长征医院皮肤性病科,上海200003 [2]第二军医大学药学院药剂学教研室,上海200433 [3]第二军医大学药学院药物分析学教研室,上海200433)
摘要:
目的:制备携载两性霉素的聚氰基丙烯酸正丁酯纳米粒(AmB-PBCA-NP),研究其对血脑屏障的透过能力。方法:孵化法制备AmB-PBCA-NP,以聚山梨酯-80进行表面修饰,建立高效液相色谱分析法,流动相选择乙腈-水(40:60)及4%乙酸,405 nm处检测。小鼠分3组,每组28只,分别注射AmB粉针剂、脂质体(AmB-L)及纳米制剂(AmB-PBCA-NP),通过检测小鼠脑组织等脏器中的药物浓度,评价其主动脑靶向作用。结果:AmB-PBCA-NP平均粒径94.38 nm,平均包封率为82%,载药量56.1%。给药后AmB粉针剂组小鼠脑内未能检测出药物,AmB-L组于3 h后测得微量浓度,而AmB-PBCA-NP组小鼠30 min即测得可观浓度,3 h后达133 ng/g。结论:聚山梨酯-80修饰的AmB-PBCA-NP具有主动脑靶向作用。[
关键词:  脑膜炎,隐球菌性 两性霉素B 聚氰基丙烯酸正丁酯 血脑屏障
DOI:10.3724/SP.J.1008.2007.00242
基金项目:上海市科委纳米专项基金(0452nm016)
Preparation of amphotericin B-polybutylcyanoacrylate-loaded nanoparticles and its distribution in mice
XU Nan, ZOU Hao, FAN Guo-rong, WEN Hai, CHEN Jiang-han
(1. Department of Dermatology, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China; 2. Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433 ; 3. Department of Pharmaceutical Analysis, School of Pharmacy, Second Military Medical University, Shanghai 200433)
Abstract:
Objective: To prepare amphotericin B-polybutylcyanoacrylate-loaded nanoparticle (AmB-PBCA-NP) and to assess their ability to pass the blood-brain barrier. Methods.- AmB-PBCA-NP was prepared by incubation, with the surface modified by polysorbate 80. High-performance liquid chromatography (HPLC) method was established using acetonitrile and water (40 : 60, 4% of acetic acid) as mobile phase; detection was done at 405 nm. Mice were divided into 3 groups: AmB- injected, AmB-lipid-injected, and AmB-PBCA-NP-injected group. Brain-targeting ability of AmB-PBCA-NP was then evaluated by determination of AmB concentrations in mice brain and other specimens. Results: The mean diameter of the prepared AmB- PBCA-NP was 94.38 nm; the mean entrapment efficiency of the particles was 82% ; and the drug loading rate was 56.10%. It was found that AmB alone failed to pass the blood-brain barrier; only very low level of AmB was detected in AmB-lipid group 3 h after injection; moderate concentration of Amb was detected 30 min after injection of AmB-PBCA-NP and the concentration peaked at 133 ng/g 3 h after injection. Conclusion: AmB-PBCA-NP modified by polysorbate 80 can pass the blood-brain barrier
Key words:  meningitis,cryptococcal  amphotericin B  polybutylcyanoacrylate  blood-brain barrier