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目的利用聚乙二醇(PEG)修饰的阳离子脂质体实现和厚朴酚与siRNA的共递送以改善肿瘤治疗效应。方法利用薄膜分散法制备聚乙二醇修饰的阳离子脂质体,通过疏水作用包载和厚朴酚以及静电吸附作用包载siRNA的方式,构建共递送和厚朴酚与siRNA的阳离子脂质体。通过粒径、电位、包封率、血清稳定性等方法考察脂质体的制剂学性质,并考察了制剂的细胞摄取与胞内分布、溶酶体逃逸能力以及肿瘤细胞生长抑制效应。结果所制备的各组载和厚朴酚脂质体的平均粒径均在100 nm以内,均具有较高的药物包封率。优选的共递送脂质体制剂(N/P=5)具有较好的血液稳定性,可获得较高的细胞摄取和较好的胞内溶酶体逃逸能力;和厚朴酚与siRNA的协同效应具有较好的抑制肿瘤细胞生长效果。结论采用聚乙二醇修饰的阳离子脂质体可以实现和厚朴酚和siRNA的共递送并将可能有利于体内肿瘤治疗。
Objective To achieve co-delivery of honokiol with siRNA by polyethylene glycol (PEG) -modified cationic liposomes to improve the therapeutic effect of tumors. Methods Polyethylene glycol modified cationic liposomes were prepared by membrane dispersion method. The hydrophobic liposomes were coated with honokiol and electrosorptively entrapped siRNAs to construct cationic liposomes co-delivered with honokiol and siRNA . The properties of liposomes were investigated by particle size, potential, entrapment efficiency and serum stability. The cellular uptake and intracellular distribution, lysosomal escape ability and tumor cell growth inhibitory effect were also investigated. Results The average particle sizes of honokiol liposomes in each group were all within 100 nm, and both had higher drug entrapment efficiency. The preferred co-delivered liposomal formulation (N / P = 5) had better blood stability with higher cellular uptake and better intracellular lysosomal escape capacity; the synergism of honokiol with siRNA Effect has better inhibit the growth of tumor cells. Conclusions The co-delivery of honokiol and siRNA may be achieved with polyethylene glycol-modified cationic liposomes and may be beneficial for in vivo tumor therapy.