Kempe Henrik, Parareda Pujolràs Anna, Kempe Maria
Nanomedicine and Biomaterials, Department of Experimental Medical Science, Lund University, Biomedical Center, D11, 22184, Lund, Sweden.
Pharm Res. 2015 Feb;32(2):375-88. doi: 10.1007/s11095-014-1468-2. Epub 2014 Aug 8.
To develop and evaluate molecularly imprinted nanocarriers for sustained release of erythromycin in physiological buffer media.
Erythromycin-imprinted poly(methacrylic acid-co-trimethylolpropane trimethacrylate) nanocarriers and corresponding control nanocarriers were prepared by free-radical precipitation polymerization. The nanocarriers were characterized by transmission electron microscopy, dynamic light scattering, and nitrogen sorption analysis. Binding studies were carried out with erythromycin and five structurally unrelated drugs. Molecular descriptors of the drugs were computed and correlated to measured binding data by multivariate data analysis. Loading with erythromycin and in vitro release studies were carried out in physiological buffer media. Kinetic models were fitted to drug release data.
The template affected the size and morphology of the nanocarriers. Binding isotherms showed that erythromycin-imprinted nanocarriers had a higher erythromycin binding capacity than corresponding control nanocarriers. Multivariate data analysis, correlating binding to molecular descriptors of the drugs, indicated a molecular imprinting effect. Erythromycin loading capacity was 76 mg/g with a loading efficiency of 87%. Release studies in physiological buffer showed an initial burst release of a quarter of loaded erythromycin during the first day and an 82% release after a week. The release was best described by the Korsmeyer-Peppas model.
Sustained release of erythromycin in physiological buffer was demonstrated.
研发并评估用于在生理缓冲介质中持续释放红霉素的分子印迹纳米载体。
通过自由基沉淀聚合法制备红霉素印迹聚（甲基丙烯酸 - 三羟甲基丙烷三甲基丙烯酸酯）纳米载体及相应的对照纳米载体。采用透射电子显微镜、动态光散射和氮吸附分析对纳米载体进行表征。对红霉素和五种结构不相关的药物进行结合研究。计算药物的分子描述符，并通过多变量数据分析将其与测得的结合数据相关联。在生理缓冲介质中进行红霉素负载及体外释放研究。将动力学模型拟合到药物释放数据。
模板影响纳米载体的尺寸和形态。结合等温线表明，红霉素印迹纳米载体比相应的对照纳米载体具有更高的红霉素结合能力。多变量数据分析将结合与药物的分子描述符相关联，表明存在分子印迹效应。红霉素负载量为76 mg/g，负载效率为87%。在生理缓冲液中的释放研究表明，第一天有四分之一负载的红霉素出现初始突释，一周后释放率为82%。用Korsmeyer - Peppas模型能最好地描述该释放过程。
证明了红霉素在生理缓冲介质中的持续释放。
