| 引用本文: | 蔡鑫君,王丛瑶,倪坚军,姚君,徐颖颖,王增.唑来膦酸阳离子脂质体的制备及其体外特性表征[J].中国现代应用药学,2015,32(2):161-165. |
| CAI Xinjun,WANG Congyao,NI Jianjun,YAO Jun,XU Yingying,WANG Zeng.Study of Preparation and in Vitro Characterization of Zoledronic Acid Cationic Liposomes[J].Chin J Mod Appl Pharm(中国现代应用药学),2015,32(2):161-165. |
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| 摘要: |
| 目的 制备唑来膦酸阳离子脂质体，并对其体外特性进行表征。方法 采用薄膜分散法制备唑来膦酸阳离子脂质体，以包封率、载药量、平均粒径、Zeta电位为评价指标，对处方及工艺进行单因素考察，并对其体外特性进行表征。结果 确定处方工艺为DPPC与DC-Chol比例为3∶1，PBS水化体积10 mL，旋转蒸发时间60 min，超声均化5 min，制备得到的阳离子脂质体的平均粒径、聚分散指数、包封率、载药量和Zeta电位分别为(106.76±1.94)nm，0.262±0.027，(38.54±0.99)%，(3.42±0.27)%，+(42.37±2.60)mV，唑来膦酸阳离子脂质体体外释药具有缓释靶向特性，药物释放曲线符合Weibull方程模型。结论 采用薄膜分散法制备的唑来膦酸阳离子脂质体具有较高的稳定性，为其药动学和药效学研究奠定了基础。 |
| 关键词: 唑来膦酸 阳离子脂质体 表征 |
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| 基金项目:浙江省医药卫生科研一般项目(2014KYB039)；杭州市医药卫生科技计划(2011A308) |
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| Study of Preparation and in Vitro Characterization of Zoledronic Acid Cationic Liposomes |
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CAI Xinjun1, WANG Congyao2, NI Jianjun1, YAO Jun1, XU Yingying1, WANG Zeng3
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1.Integrated Chinese and Western Medicine Hospital of Zhejiang Province, Hangzhou 310003, China;2.First People’s Hospital of Xiaoshan, Hangzhou 311200, China;3.Zhejiang Cancer Hospital, Hangzhou 310022, China
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| Abstract: |
| OBJECTIVE To prepare zoledronic acid cationic liposome, and evaluate its characteristics in vitro. METHODS Film dispersion method was used to prepare the zoledronic acid cationic liposome, then the single factor test of formulation and technology was investigated including the evaluation indexes as follows, the entrapment efficiency, drug loading amount, average particle size and Zeta potential. Moreover, its in vitro characterization was studied. RESULTS The prescription process was determined first, in detail, the ratio of DPPC and DC-Chol was 3∶1, PBS hydrated volume was 10 mL, rotary evaporation time was 60 min, ultrasonic averaging time was 5 min, the average particle size, PDI, entrapment efficiency, drug loading and Zeta potential of cationic liposomes were (106.76±1.94 )nm, 0.262±0.027, (38.54±0.99)%, (3.42±0.27)%, +(42.37±2.60)mV, respectively. The profiles of release in vitro was expressed well by Weibull equationin. CONCLUSION The zoledronic acid cationic liposome which prepared by the film dispersion method has relatively high stability, this characteristics would be its basis for pharmacokinetic and pharmacodynamic research in future. |
| Key words: zoledronic acid cationic liposomes characterization |
