奥沙利铂脂质体的制备及体外释药研究
发布时间：2018-08-02 14:54
【摘要】：目的制备一种包封率较高的奥沙利铂脂质体,并考察该脂质体的体外性质。方法采用多种方法制备奥沙利铂脂质体,通过单因素试验和正交试验最终确定脂质体处方。采用高效液相色谱法检测脂质体包封率,Zeta Plus激光粒度分析仪测定脂质体粒径。同时,采用高效液相色谱法、原子吸收光谱法两种方法考察了该脂质体的体外释放情况。结果与薄膜分散法和p H梯度法相比,通过逆相蒸发法制备得到的了奥沙利铂脂质体包封率更高;在此基础上进行的处方筛选试验确定了最优处方工艺为药脂比1∶7.5,胆磷比1∶2,超声功率195 W,超声时间3 min;体外释放试验结果表明,通过高效液相色谱法和原子吸收光谱法测定的奥沙利铂脂质体24 h的累计释放率分别为25.0%和33.6%。结论通过逆相蒸发法制备得到的奥沙利铂脂质体包封率高,且具有较高的稳定性和一定的缓释作用。
[Abstract]:Aim to prepare oxaliplatin liposome with high entrapment efficiency and investigate its in vitro properties. Methods oxaliplatin liposomes were prepared by various methods. The formulation of oxaliplatin liposomes was determined by single factor test and orthogonal test. The particle size of liposome was determined by high performance liquid chromatography (HPLC) with Zeta Plus laser particle size analyzer. At the same time, the in vitro release of the liposome was investigated by high performance liquid chromatography (HPLC) and atomic absorption spectrometry (AAS). Results compared with thin film dispersion method and pH gradient method, the encapsulation efficiency of oxaliplatin liposomes prepared by inverse phase evaporation method was higher than that of thin film dispersion method and pH gradient method. On the basis of this, the optimum prescription conditions were determined as follows: ratio of drug to lipid 1: 7.5, ratio of bile to phosphorus 1: 2, ultrasonic power 195 W, ultrasonic time 3 min. The results of in vitro release test showed that: 1: 7. The cumulative release rates of oxaliplatin liposomes determined by HPLC and atomic absorption spectrometry for 24 h were 25.0% and 33.6%, respectively. Conclusion Oxaliplatin liposomes prepared by reverse phase evaporation have high entrapment efficiency, high stability and sustained release.
【作者单位】： 中国药科大学药学院药剂学教研室;
【基金】：国家自然科学基金(No.81501579) 江苏省自然科学基金(No.BK20150702) 江苏高校优势学科建设工程资助项目
【分类号】：R943
[Abstract]:Aim to prepare oxaliplatin liposome with high entrapment efficiency and investigate its in vitro properties. Methods oxaliplatin liposomes were prepared by various methods. The formulation of oxaliplatin liposomes was determined by single factor test and orthogonal test. The particle size of liposome was determined by high performance liquid chromatography (HPLC) with Zeta Plus laser particle size analyzer. At the same time, the in vitro release of the liposome was investigated by high performance liquid chromatography (HPLC) and atomic absorption spectrometry (AAS). Results compared with thin film dispersion method and pH gradient method, the encapsulation efficiency of oxaliplatin liposomes prepared by inverse phase evaporation method was higher than that of thin film dispersion method and pH gradient method. On the basis of this, the optimum prescription conditions were determined as follows: ratio of drug to lipid 1: 7.5, ratio of bile to phosphorus 1: 2, ultrasonic power 195 W, ultrasonic time 3 min. The results of in vitro release test showed that: 1: 7. The cumulative release rates of oxaliplatin liposomes determined by HPLC and atomic absorption spectrometry for 24 h were 25.0% and 33.6%, respectively. Conclusion Oxaliplatin liposomes prepared by reverse phase evaporation have high entrapment efficiency, high stability and sustained release.
【作者单位】： 中国药科大学药学院药剂学教研室;
【基金】：国家自然科学基金(No.81501579) 江苏省自然科学基金(No.BK20150702) 江苏高校优势学科建设工程资助项目
【分类号】：R943
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