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Architecture based selectivity of Amphiphilic block copolymers of poly(ethylene oxide) and poly(ε-caprolactone) for drug delivery
Reactive & Functional Polymers ( IF 4.5 ) Pub Date : 2020-03-09 , DOI: 10.1016/j.reactfunctpolym.2020.104553
Imdad Ali , Faheem Kareem , Sana Rahim , Samina Perveen , Shakil Ahmed , Muhammad Raza Shah , Muhammad Imran Malik

Architecture of amphiphilic block copolymers is an important parameter that affects their critical micelles concentration (CMC), drug loading capacity and drug release behavior. In this context, 4-arm star-shaped block copolymers comprising of poly(ethylene oxide) as a hydrophilic segment and poly(ε-caprolactone) as a hydrophobic part, 4 s-P(CL-b-EO), is compared with its linear counterpart having otherwise similar total molar mass, chemical composition and molar mass of individual components (PCL-b-PEO-b-PCL). As a first step, the micelles prepared by linear block copolymer (LPM) and star-shaped block copolymer (SPM) were compared for CMC, drug encapsulation capacity, and drug release behavior. Micelles based on star-shaped polymers were found to have low CMC, high drug encapsulation capacity and better sustained release behavior. Blood hemolysis and cytotoxicity studies of both linear and star-shaped block copolymers revealed that these are safer to use for biological applications. Micelles based on star shaped polymers (SPM) and linear block copolymer (LPM) were further employed for individual delivery of cefixime (CEF) and its co-delivery with clarithromycin (CLA). Finally, growth inhibition efficiency of SPM, LPM, CEF, CLA, CEF-SPM, CEF-LPM, CEF-CLA-SPM, and CEF-CLA-LPM are evaluated against S. pneumoniae and S. pneumoniae (resistant) by antibacterial assay and morphological topography imaging by AFM. Minimum inhibitory concentration (MIC50) of drugs encapsulated in SPM is found to be considerably lower compared to direct application of drugs and drug encapsulated in LPM.



中文翻译:

基于体系结构的聚环氧乙烷和聚ε-己内酯两亲嵌段共聚物对药物递送的选择性

两亲性嵌段共聚物的结构是影响其临界胶束浓度(CMC),载药量和药物释放行为的重要参数。在本文中,将包含聚环氧乙烷作为亲水链段和聚ε-己内酯作为疏水部分的4臂星形嵌段共聚物4 sP(CL-b-EO)与它的线性进行了比较。在其他方面具有相似的总摩尔质量,化学组成和单个成分的摩尔质量的对应物(PCL-b-PEO-b-PCL)。第一步,比较由线性嵌段共聚物(LPM)和星形嵌段共聚物(SPM)制备的胶束的CMC,药物包封能力和药物释放行为。基于星形的胶束形状的聚合物被发现具有低CMC,高的药物包封能力和更好的持续释放性能。线性和星形嵌段共聚物的血液溶血和细胞毒性研究表明,它们在生物应用中更安全。基于星形聚合物(SPM)和线性嵌段共聚物(LPM)的胶束还用于头孢克肟(CEF)的单独递送及其与克拉霉素(CLA)的共同递送。最后,通过抗菌试验评估了SPM,LPM,CEF,CLA,CEF-SPM,CEF-LPM,CEF-CLA-SPM和CEF-CLA-LPM的生长抑制效率对肺炎链球菌肺炎链球菌的耐药性和原子力显微镜的形态学地形成像。最小抑菌浓度(MIC 50发现与直接应用药物和LPM封装的药物相比,SPM封装的药物的含量要低得多。

更新日期:2020-03-09
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