功能化表阿霉素脂质体的主药含量测定及体外释放考察

摘要

建立了功能化表阿霉素脂质体的主药含量及体外释放率的测定方法.采用薄膜分散法和硫酸铵梯度法制备各种类型的表阿霉素脂质体,建立了一种梯度洗脱方法,利用高效液相色谱仪测定脂质体中表阿霉素与塞来昔布的质量浓度及其体外释放度.结果显示脂质体中表阿霉素质量浓度在0.5~50.0 μg/mL,塞来昔布质量浓度在0.3~30.0μg/mL范围内线性关系良好.各种脂质体中表阿霉素的质量浓度分别为(101.2±2.0)、(103.1±1.8)、(98.7±1.3)g/mL,塞来昔布的质量浓度分别为(65.5±0.5)、(63.5±1.1)μg/mL.72h内表阿霉素的释放度均低于5%,36h塞来昔布的累积释放度均低于20%.所建立的HPLC方法准确可靠,简单快速,重复性好,各脂质体中表阿霉素与塞来昔布的体外释放缓慢,稳定性良好.%In this research, a particular method is establishedto determinethe main components and in vitro release rate of the functional epirubicin liposomes.The functional epirubicin liposomes were prepared by using the ammonium sulfate gradient method and membrane dispersion method.The contents of epirubicin and celecoxib in the liposomes, along with their in vitro release rates were determined viathe HPLCgradient elution.Results showed that the concentration ranges of epirubicin and celecoxib in liposomes were 0.5~50.0μg/mL, 0.3~30.0μg/mL, respectively with good linear;the concentration of epirubicin in the various liposomes was 101.2±2.0, 103.1±1.8,98.7±1.3μg/mL respectively;the concentration of celecoxibin all kinds of liposomes was 65.5±0.5, 63.5±1.1μg/mL respectively.Results of in vitro release showed that within the first 72 h, the release rate of epirubicin was lower than 5%, and that of celecoxib in 36h was less than 20%.The established HPLC method was simple, precise and replicable, and the in vitro release of epirubicin and celecoxib in various liposomes were slow, showing a good stability and a sustained release behavior.