| 聚合物囊泡的稳定性及H+透膜特性考察 |
| 投稿时间：2023-09-06 修订日期：2023-10-10 点此下载全文 |
| 引用本文：卞康晴,郭灵怡,迟文雅,俞媛.聚合物囊泡的稳定性及H+透膜特性考察[J].药学实践杂志,2024,42(1):12~17 |
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| 基金项目:国家自然科学基金（82273487）；全军医学科技青年培育计划（21QNPY051） |
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| 中文摘要:目的 以嵌段聚合物制备聚合物囊泡并考察其稳定性，测定聚合物囊泡膜层的H+跨膜渗透特性，及1,4-二氧六环对膜渗透性能的影响，作为聚合物囊泡载药的基础。方法 以二嵌段共聚物PEG-PLGA在溶液中自组装制备聚合物囊泡，采用pH敏感荧光探针HPTS对囊泡的H+透膜特性进行考察，并与PBD-b-PEO、PS-b-PEO制备的囊泡及脂质体进行比较。考察不同浓度的1,4-二氧六环对聚合物囊泡膜渗透特性的作用。结果 HPTS的荧光激发光谱有pH依赖性，囊泡外水相中H+浓度与t1/2呈线性相关，不同膜壁厚度的聚合物囊泡的膜渗透能力有显著区别。3种聚合物囊泡对比脂质体，H+透膜系数分别降低了2.39×104 、3.38×104、5.48×108倍。1,4-二氧六环对囊泡膜的渗透性具有调节作用，且存在浓度依赖关系。结论 聚合物囊泡的膜渗透显著低于脂质体，稳定性更好，1,4-二氧六环可调节囊泡膜的渗透性，从而调节药物的装载和释放。 |
| 中文关键词:聚合物囊泡|脂质体|纳米载体|1, 4-二氧六环|渗透性 |
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| Study on the stability and H+ permeable membrane properties of polymersomes |
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| Abstract:Objective To prepare polymersomes (PSs) by block copolymers，evaluate their membrane structural stability，investigate the H+ transmembrane permeability of PSs and the impact of 1,4-dioxane and establish a foundation for drug encapsulation within polymersomes. Methods PSs were self-assembled by a block copolymer, PEG-PLGA, in a solvent solution. The pH-sensitive fluorescence probe HPTS was employed to examine the H+ transmembrane properties of PSs and compare them with PSs prepared using PBD-b-PEO, PS-b-PEO, and liposomes. The effect of varying concentrations of 1,4-dioxane on PSs’ membrane permeability properties was also investigated. Results The fluorescence excitation spectra of HPTS exhibited pH dependency, which showed a linear correlation between extravesicular H+ concentration and t1/2. Significant differences were observed in the membrane permeability capabilities of PSs with different membrane wall thicknesses. Compared to liposomes, the H+ transmembrane coefficients for the three types of PSs were reduced by 2.39×104, 3.38×104, and 5.48×108 times, respectively. 1,4-dioxane was found to modulate the permeability of PSs’ membranes, which displayed a concentration-dependent relationship. Conclusion PSs exhibited significantly lower membrane permeability compared to liposomes, indicating superior stability. 1,4-dioxane was identified as a modulator of PSs’ permeability, which offered potential for drug loading and release within PSs. |
| keywords:polymersomes|liposomes|nanocarriers|1, 4-dioxane|permeability |
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