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化学学报
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化学学报 ›› 2007, Vol. 65 ›› Issue (19): 2175-2180. 上一篇    下一篇

研究论文

聚[碳酸(亚丁酯-co-ε-己内酯)酯]的制备及其载药微球性能的研究

刘艳飞1, 刘素琴1, 彭东明1, 颜文斌2, 黄可龙*,1   

  1. (1中南大学化学化工学院功能材料化学研究所 长沙 410083)
    (2吉首大学化学化工学院 吉首 416000)
  • 投稿日期:2006-11-21 修回日期:2007-05-28 发布日期:2007-10-14
  • 通讯作者: 黄可龙

Preparation of Poly(butylene-co-ε-caprolactone car-bonate) and Properties of Its Drug-Loaded Microspheres

LIU Yan-Fei1; LIU Su-Qin1; PENG Dong-Ming1; YAN Wen-Bin2; HUANG Ke-Long*,1   

  1. (1 Institute of Functional Material Chemistry, School of Chemistry and Chemical Engineering, Central South University, Changsha 410083)
    (2 College of Chemistry and Chemical En-gineering, Jishou University, Jishou 416000)
  • Received:2006-11-21 Revised:2007-05-28 Published:2007-10-14

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采用阴离子配位聚合方法, 合成了二氧化碳、1,2-环氧丁烷与ε-己内酯的三元共聚物: 聚[碳酸(亚丁酯-co-ε-己内酯)酯](PBCL). 并采用复相乳液(W/O/W)溶剂挥发法制备了包裹抗菌药物甲磺酸帕珠沙星的可降解微球. 对聚合物进行了FTIR, 1H NMR, 13C NMR, DSC, TGA和WAXD等表征, 以及降解性能和载药微球特性的研究. 结果表明, PBCL热稳定性及降解性能优于聚碳酸亚丁酯(PBC). 所得PBCL微球球形规整、表面光滑. 大部分微球粒径在0.5～1 μm的范围内, 载药量和包封率分别达到38.21%和87.9%. 微球的体外释药性能研究在pH 7.4的磷酸缓冲溶液中进行, 释放21 d后, PBCL微球的累积释药量为84.74%, PBC微球的释药量仅为17.29%. 药物的体外释放行为符合Higuchi方程. PBCL载药微球具有长效缓释作用.

关键词: 聚[碳酸(亚丁酯-co-ε-己内酯)酯], 甲磺酸帕珠沙星, 可降解微球, 缓释

Poly(butylene-co-ε-caprolactone carbonate) (PBCL) was synthesized by anionic coordination polymerization of carbon dioxide, 1,2-butylene oxide and ε-caprolactone (CL). PBCL microspheres containing pazufloxacian mesilate were elaborated by solvent evaporation method based on the formation of double W/O/W emulsion. The resulting polymers were characterized by FTIR, 1H NMR, 13C NMR, DSC, TGA and WAXD measurements, and the degradability of polymers and the properties of drug-loaded polymeric microspheres were studied. The results showed that the thermal properties and degradability of poly(butylene carbonate) (PBC) were improved via introduction of CL during copolymerization. The polymeric microspheres had smooth and spherical surface, and the size of most microspheres was in the range of 0.5～1 μm. The drug loading and drug encapsulation efficiency of PBCL microspheres were 38.21% and 87.9%, respectively. In vitro drug release of these microspheres was performed in a pH 7.4 phosphate-buffered solution. The drug released from PBCL microspheres was found to reach 84.74% after 21 d, and that of PBC microspheres was just 17.29%. The re-lease profile obeyed the Higuchi equation. It was suggested that PBCL was suitable for long-term sustained-release drug delivery system.

Key words: poly(butylene-co-ε-caprolactone carbonate), pazufloxacian mesilate, degradable microsphere, sustained release