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应用薄膜法制备小单层脂质体,阿霉素包封率为38.43%±3.46%,平均每个单抗携带阿霉素分子9.6个,每个单抗携带脂质体阿霉素分子336个。应用ADM、ADM脂质体、McAb-ADM-脂质体各4mg/4ml,分别给三组家兔腹腔注射。结果发现腹腔组织中,AUC(μg·hr/g)0~24在脂质体ADM组为311.933,ADM组为111.86(P<0.01)。心肌组织中AUC(μg·hr/g)0~24在ADM组为75.33,脂质全ADM组为11.29(P<0.01)。说明脂体ADM腹腔注射后能在腹腔组织中形成较高浓度,心肌组织内浓度较低,有利于提高化疗效果,降低心肌毒性。
The single-layer liposomes were prepared by the membrane method. The doxorubicin encapsulation efficiency was 38.43% ± 3.46%. On average, each monoclonal antibody had 9.6 doxorubicin molecules. Each mAb contained lipid Body doxorubicin molecules 336. The ADM, ADM liposomes and McAb-ADM-liposomes were respectively administrated 4mg / 4ml, and were injected intraperitoneally into three groups of rabbits respectively. The results showed that the AUC (μg · hr / g) 0-24 in the peritoneal cavity was 311.933 in the liposome ADM group and 111.86 in the ADM group (P <0.01). AUC (μg · hr / g) 0-24 in myocardium were 75.33 in ADM group and 11.29 in ADM group (P <0.01). Lipid ADM intraperitoneal injection can form a higher concentration in the peritoneal tissue, myocardial tissue concentration is lower, is conducive to improving the efficacy of chemotherapy and reduce myocardial toxicity.