Regulation of Drug Release by Tuning Surface Textures of Biodegradable Polymer Microparticles
Regulation of Drug Release by Tuning Surface Textures of Biodegradable Polymer Microparticles
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通过调节可生物降解聚合物微粒的表面纹理来调节药物释放
DOI：
10.1021/acsami.7b02002
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发表时间：
2017-04-26
影响因子：
9.5
通讯作者：
Zhu, Jintao
中科院分区：
文献类型：
--
作者：
Hussain, Mubashir;Xie, Jun;Zhu, Jintao
通常情况下，可生物降解聚合物颗粒的大小、均匀性、形状和表面化学将显著影响其在体外和体内的药物释放行为。本研究结合乳液滴的界面不稳定性和聚合物共混策略，制备了表面结构可调的均匀聚(d，L-乳酸-乙交酯)(PLGA)和PLGA-b-聚乙二醇(PLGA-b-PEGO)微球。利用微流控流动聚焦技术制备了含聚合物的单分散乳状液滴。液滴中有机溶剂的去除引发了界面不稳定性(界面面积的自发增加)，导致了具有纹理表面的均匀聚合物粒子的形成。通过在PLGA-b-PEG中引入均聚物PLGA，调整了聚合物体系的疏水性，并观察到乳液液滴在脱溶剂过程中的界面行为发生了质的变化。通过改变共混物中PLGA-b-PEG值的比例，可以得到表面粗糙度可调的均匀聚合物粒子。更有趣的是，颗粒的表面纹理决定了疏水紫杉醇的载药效率和释放动力学，遵循扩散导向的药物释放模式。具有不同表面纹理的聚合物颗粒表现出良好的细胞活性和生物相容性，表明该颗粒在肿瘤治疗、疫苗、生物诊断和生物成像的药物或基因输送领域具有广阔的应用前景。
Generally, size, uniformity, shape, and surface chemistry of biodegradable polymer particles will significantly affect the drug-release behavior in vitro and in vivo. In this study, uniform poly(d,L-lactic-co-glycolide) (PLGA) and PLGA-b-poly(ethylene glycol) (PLGA-b-PEG) microparticles with tunable surface textures were generated by combining the interfacial instabilities of emulsion droplet and polymer-blending strategy. Monodisperse emulsion droplets containing polymers were generated through the microfluidic flow-focusing technique. The removal of organic solvent from the droplets triggered the interfacial instabilities (spontaneous increase in interfacial area), leading to the formation of uniform polymer particles with textured surfaces. With the introduction of homopolymer PLGA to PLGA-b-PEG, the hydrophobicity of the polymer system was tailored, and a qualitatively different interfacial behavior of the emulsion droplets during solvent removal was observed. Uniform polymer particles with tunable surface roughness were thus generated by changing the ratio of PLGA-b-PEG in the polymer blends. More interestingly, surface textures of the particles determined the drug-loading efficiency and release kinetics of the encapsulated hydrophobic paclitaxel, which followed a diffusion-directed drug-release pattern. The polymer particles with different surface textures demonstrated good cell viability and biocompatibility, indicating the promising role of the particles in the fields of drug or gene delivery for tumor therapy, vaccines, biodiagnostics, and bioimaging.