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通过调整可生物降解聚合物微球的表面纹理来控制药物释放。

Regulation of Drug Release by Tuning Surface Textures of Biodegradable Polymer Microparticles.

机构信息

Key Laboratory of Materials Chemistry for Energy Conversion and Storage (HUST), Ministry of Education, School of Chemistry and Chemical Engineering, Huazhong University of Science and Technology , Wuhan 430074, China.

出版信息

ACS Appl Mater Interfaces. 2017 Apr 26;9(16):14391-14400. doi: 10.1021/acsami.7b02002. Epub 2017 Apr 11.

DOI:10.1021/acsami.7b02002
PMID:28367618
Abstract

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.

摘要

一般来说,可生物降解聚合物颗粒的大小、均匀性、形状和表面化学性质会显著影响药物在体外和体内的释放行为。在这项研究中,通过结合乳液液滴的界面不稳定性和聚合物共混策略,生成了具有可调表面纹理的均匀聚(D,L-丙交酯-共-乙交酯)(PLGA)和 PLGA-b-聚(乙二醇)(PLGA-b-PEG)微米颗粒。通过微流控流聚焦技术生成含有聚合物的单分散乳液液滴。从液滴中去除有机溶剂会引发界面不稳定性(界面面积自发增加),从而形成具有纹理表面的均匀聚合物颗粒。通过将均聚物 PLGA 引入到 PLGA-b-PEG 中,可以调整聚合物体系的疏水性,并观察到在溶剂去除过程中乳液液滴具有不同的界面行为。通过改变聚合物共混物中 PLGA-b-PEG 的比例,从而生成具有可调表面粗糙度的均匀聚合物颗粒。更有趣的是,颗粒的表面纹理决定了包封疏水性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力和生物相容性,表明这些颗粒在肿瘤治疗、疫苗、生物诊断和生物成像等领域的药物或基因传递、生物诊断和生物成像等领域具有广阔的应用前景。

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