聚合物囊泡的稳定性及H+透膜特性考察  

Study on the stability and H^(+) permeable membrane properties of polymersomes

作　　者：卞康晴 郭灵怡 迟文雅 俞媛 BIAN Kangqing;GUO Lingyi;CHI Wenya;YU Yuan(Department of Pharmaceutical Science,School of Pharmacy,Naval Medical University,Shanghai 200433,China)

机构地区：[1]海军军医大学药学系药剂学教研室,上海200433

出　　处：《药学实践与服务》2024年第1期12-17,共6页Journal of Pharmaceutical Practice and Service

基　　金：国家自然科学基金(82273487);全军医学科技青年培育计划(21QNPY051)。

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t~(1/2)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2.39×10~4、3.38×10~4、5.48×10~8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。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.

关 键 词：聚合物囊泡 脂质体 纳米载体 1 4-二氧六环 渗透性 

分 类 号：TQ317[化学工程—高聚物工业] TB383.2[一般工业技术—材料科学与工程]