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巯基化壳聚糖-吡诺克辛钠-层状双氢氧化物纳米复合物滴眼液的研究

张洁, 池慧波, 程艳菊, 操锋

张洁, 池慧波, 程艳菊, 操锋. 巯基化壳聚糖-吡诺克辛钠-层状双氢氧化物纳米复合物滴眼液的研究[J]. 中国药科大学学报, 2015, 46(2): 201-208. DOI: 10.11665/j.issn.1000-5048.20150211
引用本文: 张洁, 池慧波, 程艳菊, 操锋. 巯基化壳聚糖-吡诺克辛钠-层状双氢氧化物纳米复合物滴眼液的研究[J]. 中国药科大学学报, 2015, 46(2): 201-208. DOI: 10.11665/j.issn.1000-5048.20150211
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ZHANG Jie, CHI Huibo, CHENG Yanju, CAO Feng. Ophthalmic solution of thiolated chitosan-pirenoxine sodium-layered double hydroxides hybrid nanocomposites[J]. Journal of China Pharmaceutical University, 2015, 46(2): 201-208. DOI: 10.11665/j.issn.1000-5048.20150211
Citation: ZHANG Jie, CHI Huibo, CHENG Yanju, CAO Feng. Ophthalmic solution of thiolated chitosan-pirenoxine sodium-layered double hydroxides hybrid nanocomposites[J]. Journal of China Pharmaceutical University, 2015, 46(2): 201-208. DOI: 10.11665/j.issn.1000-5048.20150211
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巯基化壳聚糖-吡诺克辛钠-层状双氢氧化物纳米复合物滴眼液的研究

  • 1.

    中国药科大学药剂学教研室

  • 2.

    正大天晴药业集团股份有限公司南京研发中心

基金项目: 国家自然科学基金资助项目(No.81373362)；中央高校基本科研业务费专项基金资助项目(No.PT2014YX0054)

Ophthalmic solution of thiolated chitosan-pirenoxine sodium-layered double hydroxides hybrid nanocomposites

摘要

    摘要
  • 摘要: 将壳聚糖-谷胱甘肽(CG)与吡诺克辛钠(PRN)共插层于层状双氢氧化物(LDH)中，制备有机-无机杂化层状双氢氧化物纳米复合物(CG-PRN-LDH)滴眼液，并对其在家兔角膜前的滞留行为进行考察。采用共沉淀法制备了Mg-Al-PRN-LDH、Zn-Al-PRN-LDH和共插层的CG-PRN-LDH纳米复合物。通过X-RD、FTIR、TEM、激光粒度仪对纳米复合物进行表征。比较了3种纳米复合物和PRN在人工泪液中的释放行为，考察了PRN-LDH、CG-PRN-LDH纳米复合物滴眼液和市售滴眼液在家兔角膜前的滞留行为。PRN-LDH、CG-PRN-LDH纳米复合物滴眼液的AUC0-t分别为市售滴眼液的3.72和7.59倍，平均滞留时间(MRT)分别为市售滴眼液的2.18和2.60倍，结果表明有机-无机杂化纳米复合物CG-PRN-LDH能显著延长PRN在角膜前的滞留时间。
    Abstract: Ophthalmic solution of organic-inorganic layered double hydroxides hybrid nanocomposites based on layered double hydroxides(LDH)intercalated with pirenoxine sodium(PRN)and chitosan-glutathione(CG)was prepared, characterized and evaluated using rabbit precorneal retention. Mg-Al-PRN-LDH, Zn-Al-PRN-LDH and CG-PRN-LDH were synthesized by co-precipitation. The nanocomposites were characterized by laser particle sizer, powder X-ray diffraction(X-RD), fourier transform infrared spectra(FTIR)and transmission electron micrographs(TEM). The release of PRN from Mg-Al-PRN-LDH, Zn-Al-PRN-LDH, and CG-PRN-LDH nanocomposites and API in artificial tear was compared. Based on in vivo precorneal retention studies, PRN-LDH and CG-PRN-LDH nanocomposite dispersions showed significantly higher AUC(3. 72-, 7. 59-folds)and MRT(2. 18-, 2. 60-folds)than that of the commercial eye drops group. Organic-inorganic layered double hydroxides hybrid nanocomposites CG-PRN-LDH dispersions could remarkably improve precorneal retention of PRN.
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  • 刊出日期:  2015-04-24

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