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目的采用薄膜分散法制备了具有肿瘤分级靶向和pH敏感释药功能的载阿霉素聚酰胺-胺复合脂质载体c[RGDyk]-PEG2000-PSL-[PAMAM G5.0-AC80-FITC5-FA5/DOX]并对其相关性质进行了考察。方法通过微柱离心法和荧光分光光度法(spectrofluorometry,SPF)测定了聚酰胺-胺复合脂质载体的载药量及包封率;分别利用透射电镜(transmission electron microscope,TEM)、动态光散射法(dynamic light scattering,DLS)和ξ电位分析仪对聚酰胺-胺复合脂质载体的形态、粒径和表面电位进行了表征;采用透析法分别考察了聚酰胺-胺复合脂质载体在pH=7.4和pH=6.5释放介质中的体外释放行为,以及血浆对其体外释放行为的影响。结果聚酰胺-胺复合脂质载体的DOX包封率为35.17%(w),载药量为0.41%(w);其粒径分布很窄,平均粒径为106.1 nm;在透射电镜下,可见聚酰胺-胺复合脂质载体呈囊泡状,粒径大小均匀(100~150 nm);其表面ξ电位值为-6.00 mV;聚酰胺-胺复合脂质载体的体外释药行为体现出pH敏感性和对血浆的稳定性。结论以c[RGDyk]-PEG修饰的pH敏感长循环脂质体包载PAMAM G5.0-AC80-FITC5-FA5/DOX复合物构建具有肿瘤分级靶向和pH敏感释药功能的载阿霉素聚酰胺-胺复合脂质载体有可行性及良好的应用前景。
OBJECTIVE To prepare the carrier of doxorubicin polyamide-amine complex lipid carrier c [RGDyk] -PEG2000-PSL- [PAMAM G5.0-AC80-FITC5- FA5 / DOX] and examined its related properties. Methods The drug loading and entrapment efficiency of polyamide-amine complex lipid carrier were measured by microcolumn centrifugation and spectrofluorometry (SPF). Transmission electron microscopy (TEM), dynamic light scattering The morphology, particle size and surface potential of polyamide-amine composite lipid carriers were characterized by dynamic light scattering (DLS) and zeta potential analyzer. The effects of polyamide-amine complex lipid carrier = 7.4 and pH = 6.5 in vitro, and the effect of plasma on its in vitro release behavior. Results The encapsulation efficiency of polyamide - amine composite lipid carrier was 35.17% (w) and the drug loading was 0.41% (w). The particle size distribution was very narrow and the average particle size was 106.1 nm. Under the transmission electron microscope, The results showed that the polyamide-amine complex lipid vesicles were vesicular in shape with a uniform particle size (100-150 nm) and a surface zeta potential of -6.00 mV. The in vitro drug release behavior of polyamide-amine complex lipid carriers pH sensitivity and stability to plasma. Conclusion The PAMAM G5.0-AC80-FITC5-FA5 / DOX complex was encapsulated by c [RGDyk] -PEG-modified pH-sensitive long-circulating liposomes to construct apolipridin with tumor grade targeting and pH-sensitive drug release Polyamidoamine complex lipid carrier has the feasibility and good application prospect.