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紫杉醇透过细胞膜的药物吸收过程及其脂质体制备与紫杉醇/脂质相互作用密切相关.通过Langmuir膜技术和原子力显微镜(AFM)观测,研究了不同比例的二棕榈酰磷脂胆碱(DPPC)/紫杉醇(paclitaxel)二元混合系统在空气/水界面上的单分子层相互作用.对膜压-面积(π-A)曲线的测量和基于π-A曲线的混合性分析、热力学稳定性分析及可压缩性分析表明:紫杉醇和DPPC相互混合,不同分子间存在斥力,混合单分子层出现相分离.除紫杉醇摩尔分数(xpac)为0.4外,这些现象均随单分子层压缩增加到一定程度后出现反转;对xpac=0.4,不同分子间混合程度、斥力作用和单分子层中相分离均远超过其他混合比例的单分子层,且随单分子层压缩程度持续增加,不同分子间相互作用的影响远远超过压缩程度;xpac≤0.4时,脂质单分子层结构受紫杉醇影响较小,超过0.4后脂质单分子层结构遭到严重破坏.利用原子力显微镜对紫杉醇/DPPC单分子层进行了表面形貌观测,证实了Langmuir研究的结果.
The drug absorption process of paclitaxel through the cell membrane and its preparation of liposomes are closely related to the paclitaxel / lipid interaction.Double-palmitoylphosphatidylcholine (DPPC) was studied by Langmuir membrane technology and atomic force microscopy (AFM) / Paclitaxel binary mixing system at the air / water interface.Measurements of the membrane pressure-area (π-A) curve and the mixed analysis based on the π-A curve, thermodynamic stability analysis And compressibility analysis showed that paclitaxel and DPPC mixed with each other, there was repulsion between different molecules, and the mixed monolayers appeared phase separation.Except that the paclitaxel molar fraction (xpac) was 0.4, these phenomena all increased with the compression of monolayers to some extent After xpac = 0.4, the degree of intermolecular mixing, repulsion and phase separation in the monolayer far outweigh the other monomolecular monolayers, and as the degree of compression of the monomolecular layer continues to increase, the intermolecular interactions between the different molecules The effect is much more than the degree of compression; xpac ≤ 0.4, the lipid monolayer structure is less affected by paclitaxel, more than 0.4 lipid monolayer structure was severely damaged. Force microscope paclitaxel / DPPC monolayer surface morphology were observed, confirming the results Langmuir study.