和厚朴酚与siRNA共递送的阳离子脂质体研究

发布时间：2018-01-23 07:16

本文关键词： 小干扰RNA 和厚朴酚共递送阳离子脂质体肿瘤治疗　出处：《中国药学杂志》2015年18期 　论文类型：期刊论文

【摘要】：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。
[Abstract]:Objective to utilize polyethylene glycol (PEG). The modified cationic liposome and the codelivery of honokiol and siRNA were used to improve the therapeutic effect of tumor. Methods Polyethylene glycol modified cationic liposomes were prepared by thin film dispersion. The cationic liposomes of codelivery and magnolol with siRNA were constructed by hydrophobic encapsulation and honokiol and electrostatic adsorption of siRNA. The entrapment efficiency was determined by particle size, potential and encapsulation efficiency. The pharmacological properties of liposomes were investigated by serum stability method. The cellular uptake and intracellular distribution of liposomes were also investigated. Results the average particle size of each group of liposomes and honokiol liposomes was less than 100 nm. The selected co-delivery liposome preparation (N / P ~ (5)) had better blood stability, higher cellular uptake and better intracellular lysosome escape ability. The synergistic effect of honokiol and siRNA can inhibit the growth of tumor cells. Conclusion the co-delivery of honokiol and siRNA can be realized by using cationic liposomes modified with polyethylene glycol. It is beneficial to the treatment of tumor in vivo.
【作者单位】：北京大学药学院药剂学系;
【基金】：国家自然科学基金资助项目(81473158,81273455)
【分类号】：R944
【正文快照】： 新生血管的生成在肿瘤生长中必不可少,肿瘤的血管内皮细胞处于高度增殖状态,更新周期远小于正常组织的血管内皮细胞[1]。根据Folk-man提出的著名的“肿瘤饥饿疗法”,可以通过抑制肿瘤新生血管,达到抑制和治疗肿瘤的目的[2-3]。在对抗新生血管与抗肿瘤的小分子化合物的筛选过程

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