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首页> 外文期刊>Biomaterials >Preparation, characterization, and in vitro evaluation of physostigmine-loaded poly(ortho ester) and poly(ortho ester)/poly(d,l-lactide-co-glycolide) blend microspheres fabricated by spray drying.
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Preparation, characterization, and in vitro evaluation of physostigmine-loaded poly(ortho ester) and poly(ortho ester)/poly(d,l-lactide-co-glycolide) blend microspheres fabricated by spray drying.

机译：喷雾干燥制得的装有毒扁豆碱的聚（原酸酯）和聚（原酸酯）/聚（d，l-丙交酯-乙交酯）共混微球的制备，表征和体外评价。

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The physostigmine-loaded poly(ortho ester) (POE), poly(dl-lactide-co-glycolide) (PLGA) and POE/PLGA blend microspheres were fabricated by a spray drying technique. The in vitro degradation of, and physostigmine release from, the microspheres were investigated. SEM analysis showed that the POE and POE/PLGA blend particles were spherical. They were better dispersed when compared to the pure PLGA microspheres. Two glass transition temperature ( [Formula: see text] ) values of the POE/PLGA blend microspheres were observed due to the phase separation of POE and PLGA in the blend system. XPS analysis proved that POE dominated the surfaces of POE/PLGA blend microspheres, indicating that the blend microspheres were coated with POE. The encapsulation efficiencies of all the microspheres were more than 95%. The incorporation of physostigmine reduced the [Formula: see text] value of microspheres. The [Formula: see text] value of the degrading microspheres increased with the release of physostigmine. For instance,POE blank microspheres and physostigmine-loaded POE microspheres had a [Formula: see text] value of 67 degrees C and 48 degrees C, respectively. After 19 days in vitro incubation, [Formula: see text] of the degrading POE microspheres increased to 55 degrees C. Weight loss studies showed that the degradation of the blend microspheres was accelerated with the presence of PLGA because its degradation products catalyzed the degradation of both POE and PLGA. The release rate of physostigmine increased with increase of PLGA content in the blend microspheres. The initial burst release of physostigmine was effectively suppressed by introducing POE to the blend microspheres. However, there was an optimized weight ratio of POE to PLGA (85:15 in weight), below which a high initial burst was induced. The POE/PLGA blend microspheres may make a good drug delivery system.
机译：通过喷雾干燥技术制备了装载有毒扁豆碱的聚原酸酯（POE），聚（dl-丙交酯-共-乙交酯）（PLGA）和POE / PLGA共混微球。研究了微球的体外降解和毒扁豆碱的释放。 SEM分析表明POE和POE / PLGA共混物颗粒是球形的。与纯PLGA微球相比，它们的分散性更好。由于POE / PLGA共混体系中POE和PLGA的相分离，观察到了POE / PLGA共混微球的两个玻璃化转变温度（[公式：参见文本]）值。 XPS分析证明POE占了POE / PLGA混合微球的表面，表明该混合微球被POE包覆。所有微球的包封效率均超过95％。毒扁豆碱的掺入降低了微球的[式：见正文]值。降解的微球的[配方：见正文]值随毒扁豆碱的释放而增加。例如，POE空白微球和装有毒扁豆碱的POE微球的[公式：参见文本]值分别为67摄氏度和48摄氏度。体外温育19天后，降解的POE微球的[分子式：见正文]升高至55摄氏度。减肥研究表明，在PLGA存在下，共混微球的降解得以加速，因为其降解产物催化了PGA的降解。 POE和PLGA都可以。毒扁豆碱的释放速率随混合微球中PLGA含量的增加而增加。通过将POE引入共混微球可有效抑制毒扁豆碱的初始突释。但是，存在POE与PLGA的最佳重量比（重量比为85:15），低于该重量比时会引发高初始爆裂。 POE / PLGA共混微球可能是一个好的药物递送系统。

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