Xia Yun, Qiu Li-yan, Jin Yi
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, China.
Yao Xue Xue Bao. 2005 Feb;40(2):187-92.
To synthesize poly(N-isopropylacrylamide)/cyclodextrin conjugate (PNIPA-beta-CD) as thermosensitive drug carrier, incorporate indomethacin into the conjugate and evaluate the drug release from the carrier in vitro.
PNIPA-beta-CD was synthesized by introducing carboxyl terminated PNIPA into the primary hydroxy group of beta-CD. The obtained conjugate was characterized by FTIR, 1H NMR and DSC. The indomethacin/PNIPA-beta-CD complex was prepared by lyophilization. In vitro drug release from the complex was carried out at 25 degrees C and 37 degrees C respectively.
Thermosensitive PNIPA-beta-CD was synthesized successfully. The LCST is 35 degrees C, as measured by turbidity method. The drug release from indomethacin/PNIPA-beta-CD complex was slower at 37 degrees C than that at 25 degrees C.
Thermosensitive PNIPA-beta-CD with molecular inclusion capacity is a potential carrier for drug sustained release.
合成聚（N-异丙基丙烯酰胺）/环糊精共轭物（PNIPA-β-CD）作为热敏性药物载体，将吲哚美辛载入共轭物并评估其体外释药情况。
通过将羧基封端的PNIPA引入β-CD的伯羟基来合成PNIPA-β-CD。所得共轭物用傅里叶变换红外光谱（FTIR）、核磁共振氢谱（1H NMR）和差示扫描量热法（DSC）进行表征。通过冻干法制备吲哚美辛/PNIPA-β-CD复合物。分别在25℃和37℃下进行复合物的体外释药实验。
成功合成了热敏性PNIPA-β-CD。用浊度法测得其低临界溶液温度（LCST）为35℃。吲哚美辛/PNIPA-β-CD复合物在37℃时的释药比在25℃时慢。
具有分子包合能力的热敏性PNIPA-β-CD是一种有潜力的药物缓释载体。
