| 严思静,李攀,袁佩,许川山,王志刚.载10-羟基喜树碱脂质超声微泡的处方制备及一般特性研究[J].中国医学影像技术,2009,25(4):574~577 |
| 载10-羟基喜树碱脂质超声微泡的处方制备及一般特性研究 |
| Preparation and characteristics of lipid ultrasound microbubbles containing 10-hydroxycamptothecin |
| 投稿时间：2008-09-04 修订日期：2009-01-06 |
| DOI： |
| 中文关键词: 超声 造影剂 10-羟基喜树碱 |
| 英文关键词:Ultrasound Contrast agent 10-hydroxycamptothecin |
| 基金项目:863项目(2006AA02Z4FO),国家自然科学基金重点项目(30430230)。 |
| 作者 | 单位 | E-mail | | 严思静 | | | | 李攀 | Institute of Ultrasonic Image, Chongqing University of Medical Sciences, Chongqing 400010, China | | | 袁佩 | Institute of Ultrasonic Image, Chongqing University of Medical Sciences, Chongqing 400010, China | | | 许川山 | Institute of Ultrasonic Image, Chongqing University of Medical Sciences, Chongqing 400010, China | | | 王志刚 | Institute of Ultrasonic Image, Chongqing University of Medical Sciences, Chongqing 400010, China | wzg62942443@163.com |
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| 中文摘要: |
| 目的 研究载10-羟基喜树碱(HCPT)脂质超声微泡的处方制备工艺,筛选出最佳处方制备载药微泡,研究微泡的一般特性及显影效果,并检测微泡的药物包封率和载药量。方法 以机械振荡法制备载HCPT脂质超声微泡;采用正交试验优选处方;采用紫外分光光度法和反相高效液相色谱法测定微泡的包封率和载药量;在光学显微镜下计数并观察微泡的外观和分布情况;以马尔文激光粒径测量仪测量微泡粒径大小和Zeta电位; 观察并比较微泡经60Co射线灭菌前后其外观、形态、平均粒径和包封率的改变;并观察微泡在兔肝脏的增强显影效果。结果 以最佳处方制备的载10-羟基喜树碱(2 mg) 微泡的药物包封率为86.70％,载药量为21.70％;浓度为(3.07±0.58)×109／ml,粒径范围为(1.10±0.20)μm,平均粒径为1.10 μm;Zeta电位为-(3.90±0.80)mV;超声定向辐照微泡后,药物吸光度值明显增加;经60Co射线灭菌后观察微泡形态、平均粒径及包封率无明显变化;静脉注射此载药微泡后,兔肝脏超声显影持续增强。结论 采用机械振荡法制备的载HCPT脂质微泡,包封率和载药量较高,粒径分布均匀,体内显影效果好,有望实现实时监控下的体内定点靶向给药,为进一步研究奠定了基础。 |
| 英文摘要: |
| Objective To screen the optimal formulation and preparation of the containting 10-hydroxycamptothecin (HCPT) lipid ultrasound microbubble and to study its characteristics and to evaluate its effect as a new ultrasound contrast agent for chemotherapeutic drug delivery. Methods The lipid ultrasound microbubble containing HCPT was prepared by mechanical vibration, orthogonal design was used to select the optimal formulation.Ultraviolet spectrophotometry and reversed phase high-performance liquid chromatography (RP-HPLC) were used to determine the entrapment efficiency and the drug-loading amounts of HCPT lipid microbubble. The optimal one was studied for appearance, mean diameter, entrapment efficiency before and after irradiance of 60Co γ ray.The liver imaging was observed. Results The concentration of the optimal formulation was (3.07±0.58)×109/ml; the mean diameter range of the self-made lipid microbubbles containing HCPT was (1.10±0.20) μm; the mean diameter was 1.10 μm; Zeta potential was -(3.90±0.80) mV; the drug entrapment efficiency was 86.70%; the drug-loading amounts was 21.70%. After sterilization with irradiance of 60Co γ, the mean diameter and entrapment efficiency did not change obviously. The liver imaging of the rabbit could be enhanced obviously and persistently. Conclusion The self-made lipid microbubbles containting HCPT have higher entrapment efficiency and drug-loading amounts, it is effective for the enhancement of ultrasound imaging in vivo. Based on this phenomenon, the future studies for ultrasound-mediated drug delivery would be expected. |
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