夏芸, 邱利焱, 金一. 温敏性吲哚美辛/β-环糊精包合物的制备及体外评价J. 药学学报, 2005, 40(2): 187-192.
引用本文: 夏芸, 邱利焱, 金一. 温敏性吲哚美辛/β-环糊精包合物的制备及体外评价J. 药学学报, 2005, 40(2): 187-192.
XIA Yun, QIU Li-yan, JIN Yi. Preparation and characterization of indomethacin/poly(N-isopropylacrylamide)-β-cyclodextrin complex with temperature-sensitivityJ. Acta Pharmaceutica Sinica, 2005, 40(2): 187-192.
Citation: XIA Yun, QIU Li-yan, JIN Yi. Preparation and characterization of indomethacin/poly(N-isopropylacrylamide)-β-cyclodextrin complex with temperature-sensitivityJ. Acta Pharmaceutica Sinica, 2005, 40(2): 187-192.

温敏性吲哚美辛/β-环糊精包合物的制备及体外评价

Preparation and characterization of indomethacin/poly(N-isopropylacrylamide)-β-cyclodextrin complex with temperature-sensitivity

  • 摘要: 目的合成兼具温敏性及药物包合能力的新型药物载体聚(N-异丙基丙烯酰胺)-β-环糊精(PNIPA-β-CD),以吲哚美辛为模型药物,考察该载体的释药行为。方法末端带羧基的PNIPA与改性后的环糊精衍生物在1-(3-二甲氨基丙基)-3-乙基-碳二亚胺(EDC)的作用下缩合,得到PNIPA-β-CD,采用冻干法制备吲哚美辛/PNIPA-β-CD包合物。红外、1H NMR和DSC表征载体的结构及包合物的形成;用分光光度法测定载体材料的LCST,并进行包合物体外释药研究。结果PNIPA-β-CD在35 ℃发生相转变,吲哚美辛/PNIPA-β-CD包合物的载药量为5.8%,药物与载体摩尔比为0.97∶1。体外释放研究表明吲哚美辛/PNIPA-β-CD包合物在37 ℃的释药比其在25 ℃的释放要慢,在LCST以上具有一定的缓释作用。结论该载体既具有温敏性,又具有药物包合作用,并且在体温条件下具有缓释作用,是一种新型的温敏性药物载体。

     

    Abstract: AimTo synthesize poly(N-isopropylacrylamide)/cyclodextrin conjugate (PNIPA-β-CD) as thermosensitive drug carrier, incorporate indomethacin into the conjugate and evaluate the drug release from the carrier in vitro. MethodsPNIPA-β-CD was synthesized by introducing carboxyl terminated PNIPA into the primary hydroxy group of β-CD. The obtained conjugate was characterized by FTIR, 1H NMR and DSC. The indomethacin/PNIPA-β-CD complex was prepared by lyophilization. In vitro drug release from the complex was carried out at 25 ℃ and 37 ℃ respectively. ResultsThermosensitive PNIPA-β-CD was synthesized successfully. The LCST is 35 ℃, as measured by turbidity method. The drug release from indomethacin/PNIPA-β-CD complex was slower at 37 ℃ than that at 25 ℃. Conclusion Thermosensitive PNIPA-β-CD with molecular inclusion capacity is a potential carrier for drug sustained release.

     

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