Preparation and In Vitro Drug Release Behavior of 1,10-Phenanthroline/β-cyclodextrin–poly (Glycidyl Methacrylate) Drug-Loaded Microspheres

Ya Li, W. Zhen
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Abstract

In this study, novel star-shaped polymers of I²-cyclodextrin (I²-CD)–poly (glycidyl methacrylate) (PGMA) were prepared by atom transfer radical polymerization (ATRP), formed from GMA and I²-CD. In addition, the structure, properties and hydrophilicity of the I²-CD-PGMA polymers thus prepared were systematically analyzed. 1,10-phenanthroline monohydrate (Phen)/I²-CD-PGMA drug-loaded microspheres were prepared by emulsion solvent evaporation. The optimum preparation conditions were determined by orthogonal tests. Analysis results indicated that the performance of star-shaped polymers of I²-CD-PGMA clearly changes, resulting in the increase of the contact angle from 17° to 72.5°, and their thermal degradation temperature was enhanced from 260 °C to 401 °C. Moreover, I²-CD-PGMA drug-loaded microspheres with a smooth, spherical surface were successfully prepared, and the drug-loading capacity and average particle size of drug-loaded microspheres were 26.67 % and 10 I¼m, respectively. Drug release tests indicated that the release behavior of I²-CD-PGMA drug-loaded microspheres conformed to Higuchi release kinetics, which exhibited a significant drug delivery capability. The release rate and utilization of I²-CD-PGMA were greater than that of I²-CD, demonstrating that I²-CD-PGMA was more suitable as a drug delivery material.
1,10-菲罗啉/β-环糊精 -聚甲基丙烯酸缩水甘油酯载药微球的制备及体外释药行为
本研究采用原子转移自由基聚合(ATRP)法制备了I²-环糊精(I²-CD) -聚甲基丙烯酸甘油酯(PGMA)星形聚合物。此外,系统地分析了所制备的I²-CD-PGMA聚合物的结构、性能和亲水性。采用乳化溶剂蒸发法制备了1,10-邻菲罗啉一水合物(Phen)/I²-CD-PGMA载药微球。通过正交试验确定了最佳制备条件。分析结果表明,I²-CD-PGMA星形聚合物的性能发生了明显变化,接触角从17°增加到72.5°,热降解温度从260 °C提高到401 °C。成功制备了表面光滑的I²-CD-PGMA载药微球,其载药量和平均粒径分别为26.67%和10 μ m。药物释放试验表明,I²-CD-PGMA载药微球的释放行为符合Higuchi释放动力学,具有良好的给药能力。I²-CD- pgma的释放率和利用率均大于I²-CD,表明I²-CD- pgma更适合作为给药材料。
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