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聚己内酯电纺纳米纤维载甲硝唑前体药物控释用于牙周病。

Controlled release of metronidazole benzoate from poly epsilon-caprolactone electrospun nanofibers for periodontal diseases.

机构信息

Department of Textile Engineering, Isfahan University of Technology, Isfahan, Iran.

出版信息

Eur J Pharm Biopharm. 2010 Jun;75(2):179-85. doi: 10.1016/j.ejpb.2010.02.002. Epub 2010 Feb 6.

Abstract

Poly epsilon-caprolactone (PCL) nanofibers containing metronidazole benzoate (MET) were successfully electrospun and evaluated for periodontal diseases. Solutions of 10.5% w/v PCL and 5-15%w/w MET in mixtures of dichloromethane (DCM)/N,N-dimethylformamide (DMF) with ratios of 90:10, 80:20 and 70:30 v/v were prepared, and the nanofibers were produced by electrospinning technique. Scanning electron microscopy (SEM) was used to investigate the morphology and average diameter of the electrospun nanofibers. DSC results indicated a molecular dispersion of MET in the PCL nanofibers and showed a decrease in crystallinity of PCL nanofibers by adding MET. Results showed that an increase in the DCM:DMF ratio led to a decrease in the solution conductivity and an increase in the solution viscosity as well as in the nanofibers diameter. Also increasing metronidazole benzoate concentration caused an increase in the solution conductivity and a decrease in the solution viscosity as well as in the nanofibers diameter. In vitro drug release studies in phosphate buffer solution (pH 7.4) showed that the drug release rate was affected by the solvents ratio and the drug concentration. Moreover, the burst release was low, and sustained drug release was prolonged to at least 19 days.

摘要

聚己内酯(PCL)纳米纤维载甲硝唑苯甲酸(MET)成功电纺,用于牙周病的评估。将 10.5%w/v 的 PCL 和 5-15%w/w 的 MET 溶解在二氯甲烷(DCM)/N,N-二甲基甲酰胺(DMF)混合物中,DCM:DMF 的比例为 90:10、80:20 和 70:30 v/v,并通过电纺技术制备纳米纤维。扫描电子显微镜(SEM)用于研究电纺纳米纤维的形态和平均直径。差示扫描量热法(DSC)结果表明 MET 在 PCL 纳米纤维中存在分子分散,并表明添加 MET 会降低 PCL 纳米纤维的结晶度。结果表明,DCM:DMF 比例的增加会导致溶液电导率降低,溶液粘度增加以及纳米纤维直径增加。同时,甲硝唑苯甲酸浓度的增加会导致溶液电导率增加,溶液粘度降低以及纳米纤维直径减小。在磷酸盐缓冲溶液(pH 7.4)中的体外药物释放研究表明,药物释放速率受溶剂比例和药物浓度的影响。此外,突释较低,药物释放时间延长至至少 19 天。

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