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首页> 外文期刊>RSC Advances >Fabrication, characterization, and controlled release of eprinomectin from injectable mesoporous PLGA microspheres
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Fabrication, characterization, and controlled release of eprinomectin from injectable mesoporous PLGA microspheres

机译：从注射介孔PLGA微球中的ePrinomectin的制备，表征和控制释放

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Batches of mesoporous poly(lactide-co-glycolide) (PLGA) microspheres were fabricated via an O/W emulsion-solvent evaporation method. The obtained microspheres were detected with scanning electron microscopy (SEM, S-4800) to observe their surface morphology. On observation it was found that many macropores were distributed on the microsphere surfaces. Then, eprinomectin (EPR) was employed as a model drug and was encapsulated by these mesoporous microspheres. The distribution state of the EPR in the microspheres was investigated via X-ray diffraction and differential scanning calorimetry. The test results indicated that the EPR was distributed in the microspheres with an amorphous state. After re-dispersing the EPR-loaded microspheres in ultrapure water, an extended-release formulation of EPR was obtained. The formulation was administered to Japanese white rabbits by subcutaneous injection to monitor the blood concentration of EPR. Plasma concentration profiles showed that the C-max of EPR (38.80 +/- 9.50 ng mL(-1)) appeared on the 2nd day after subcutaneous injection. During the next 40 days, the plasma concentration of EPR maintained a value of 30.0 ng mL(-1). In addition, the biocompatibility of the EPR-loaded mesoporous microspheres (EPM) was also investigated by a biological sectioning method. Photographs of the histological sections illustrated that the EPM did not trigger a serious stimulus response at the injection site. Thus, they could be used to affirm that the mesoporous microspheres have a promising application in controlling veterinary drugs for sustained release.
机译：通过O / W乳液溶剂蒸发方法制造批次的介孔聚（丙交酯 - 共乙酰化）（PLGA）微球。通过扫描电子显微镜（SEM，S-4800）检测所获得的微球，观察其表面形态。发现观察结果发现许多大孔分布在微球表面上。然后，用ePrinomectin（EPR）作为模型药物，并通过这些介孔的微球包封。通过X射线衍射和差示扫描量热法研究微球中EPR中的EPR的分布状态。测试结果表明，EPR在微球中分布在具有非晶态的微球中。在超纯水中重新分散EPR负载的微球后，获得了EPR的延长释放制剂。通过皮下注射给日本白兔施用制剂，监测EPR的血液浓度。血浆浓度分布显示，在皮下注射后第2天出现了EPR的C-MAX（38.80 +/- 9.50ng ml（-1））。在接下来的40天期间，EPR的血浆浓度保持了30.0ng ml（-1）的值。此外，还通过生物切片方法研究了EPR负载的介孔微球（EPM）的生物相容性。所示的组织学部分的照片表明EPM没有引发注射部位的严重刺激反应。因此，它们可以用来肯定介孔的微球在控制兽药中具有持续释放的有希望的应用。

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  • 来源
    《RSC Advances》 |2015年第92期|共8页
  • 作者

    Shang Qing; Zhai Jianhua; Tian Ruiqiong; Zheng Ting; Zhang Xiaoyun; Liang Xiaoyang; Zhang Jing;

  • 作者单位

    Hebei Univ Sci &

    Technol Chem &

    Pharmaceut Engn Inst Wuhan 050018 Hebei Peoples R China;

    Hebei Univ Sci &

    Technol Chem &

    Pharmaceut Engn Inst Wuhan 050018 Hebei Peoples R China;

    Hebei Univ Sci &

    Technol Chem &

    Pharmaceut Engn Inst Wuhan 050018 Hebei Peoples R China;

    Zhongqi Pharmaceut Technol SJZ Co Ltd Pharmaceut Res Inst Wuhan 050018 Hebei Peoples R China;

    Hebei Univ Sci &

    Technol Chem &

    Pharmaceut Engn Inst Wuhan 050018 Hebei Peoples R China;

    Hebei Univ Sci &

    Technol Chem &

    Pharmaceut Engn Inst Wuhan 050018 Hebei Peoples R China;

    Hebei Univ Sci &

    Technol Chem &

    Pharmaceut Engn Inst Wuhan 050018 Hebei Peoples R China;

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