中国输血杂志2025，Vol.38Issue(5)：652-659,8.DOI:10.13303/j.cjbt.issn.1004-549x.2025.05.009
负载硫酸长春新碱-血小板膜仿生脂质体的制备及体外评价
Preparation and in vitro evaluation of platelet membrane biomimetic liposomes loaded with vincristine sulfate
摘要
Abstract
Objective To prepare platelet membrane biomimetic liposomes loaded with vincristine sulfate(VCR)for targeted delivery to tumor.Methods Vincristine sulfate liposomes(LIPO)were prepared using the pH-gradient method,followed by the fusion of platelet membranes and subsequent drug loading to obtain platelet membrane biomimetic liposomes(PLM-LIPO).The particle size,polydispersity index(PDI),Zeta potential,and drug encapsulation efficiency(EE%)of both liposomes were characterized.The tumor-targeting capability was evaluated through in vitro cellular experiments and in vivo biodistribution studies.Results The optimal preparation conditions for LIPO were determined as follows:DPPC-to-cholesterol molar ratio of 1∶1,internal aqueous phase of 0.3 M pH 4.0 citrate buffer,external aqueous phase of 1 M Na2 HPO4 solution,drug-to-lipid ratio of 1∶10,drug loading temperature of 60℃,and loading time of 10 minutes.The LI-PO exhibited a mean particle size of(147.3±2.24)nm,PDI of 0.078±0.014,Zeta potential of(-3.54±0.75)mV,and EE%of 91.37±0.47.For PLM-LIPO,prepared via membrane fusion followed by drug loading,the mean particle size was(185.3±3.61)nm,PDI was 0.075±0.022,Zeta potential was(-18.91±1.54)mV,and EE%was 63.36±2.45.In the CD62P validation experiment,the fluorescence intensity of PLM-LIPO was five times higher than that of LIPO.In vitro cel-lular uptake experiments revealed that PLM-LIPO showed 1.3-fold and 1.2-fold higher uptake rates compared to LIPO at 6 h and 12 h,respectively.In vivo experiments demonstrated that 1h after administration,the accumulation of PLM-LIPO at tumor sites was 4-fold higher than that of LIPO and 6-7 times higher than that in healthy mice.Conclusion The platelet membrane biomimetic liposomes loaded with vincristine sulfate were successfully developed.Both cellular uptake and tissue distribution studies confirmed the PLM-LIPO enhanced tumor-targeting capability.关键词
血小板膜/脂质体/硫酸长春新碱/肿瘤靶向治疗Key words
platelet membrane/liposomes/vincristine sulfate/tumor targeted therapy分类
医药卫生引用本文复制引用
肖晶,游训仪,张阿龙,钟锐,刘嘉馨,曹晔,王红..负载硫酸长春新碱-血小板膜仿生脂质体的制备及体外评价[J].中国输血杂志,2025,38(5):652-659,8.基金项目
中国医学科学院医学与健康科技创新工程项目"血液安全保障及新产品技术研究"(2021-I2M-1-060) （2021-I2M-1-060）
