Cai Lin, Niu Guangfeng, Hu Zhiping, Jin Wei, Wang Jianping, Sun Li
Department of Orthopaedics, Zhongnan Hospital, Wuhan University, Hubei, People's Republic of China.
J Drug Target. 2009 Apr;17(3):200-6. doi: 10.1080/10611860802650017.
The present study was designed to prepare and evaluate adriamycin-polybutylcyanoacrylate magnetic nanoparticles (ADR-PBCA-MNPs) as novel carriers of adriamycin.
ADR-PBCA-MNPs was prepared by the emulsion polymerization technique. Entrapment efficiency (ER) and drug load (DL) of nanoparticles, along with in vitro release were studied. Pharmacokinetic analysis was carried out in Kunming mice, with blood obtained at determined time points post administration. Biodistribution and recovery rate of ADR was measured and determined.
Nanoparticles were visible as approximate spherical particles with good disparity, with an average diameter of 184.6 nm, a minimum diameter of 59.07 nm, and a maximum diameter of 291.66 nm as demonstrated by transmission electron microscopy. The ER and quantity of DL of ADR-PBCA-MNPs were 90.73 and 10.68%, respectively, measured by an ultraviolet-visible light spectrophotometer. In vitro study demonstrated that the release reached a balance after 72 h, with a total release rate of approximately 80%. As shown in pharmacokinetic studies in rats,the ADR-PBCA-MNPs group displayed a slowed doxorubicin release associated with better bioavailability. ADR-PBCA-MNPs reduced ADR accumulation at nontarget sites in the magnetic field, contributing to the reduced toxicity and side effects of ADR.
ADR-PBCA-MNPs was successfully prepared and had a satisfactory targeted effect under the magnetic field, which can increase ADR concentration at target sites but not at non-target sites. As a result, the therapeutic effect of ADR may be greatly enhanced with minimized drug toxicity and side effects.
本研究旨在制备并评估阿霉素-聚氰基丙烯酸正丁酯磁性纳米粒(ADR-PBCA-MNPs)作为阿霉素的新型载体。
采用乳液聚合法制备ADR-PBCA-MNPs。研究纳米粒的包封率(ER)、载药量(DL)以及体外释放情况。在昆明小鼠体内进行药代动力学分析,给药后在特定时间点采集血液。测定并确定ADR的生物分布和回收率。
透射电子显微镜显示,纳米粒呈近似球形,分散性良好,平均直径为184.6 nm,最小直径为59.07 nm,最大直径为291.66 nm。用紫外-可见分光光度计测得ADR-PBCA-MNPs的ER和DL量分别为90.73%和10.68%。体外研究表明,72 h后释放达到平衡,总释放率约为80%。大鼠药代动力学研究显示,ADR-PBCA-MNPs组阿霉素释放减慢,生物利用度更高。ADR-PBCA-MNPs减少了磁场中非靶部位的ADR蓄积,有助于降低ADR的毒性和副作用。
成功制备了ADR-PBCA-MNPs,在磁场作用下具有令人满意的靶向效果,可提高靶部位而非非靶部位的ADR浓度。因此,可在将药物毒性和副作用降至最低的同时,大大增强ADR的治疗效果。