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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Encapsulation and release characteristics of DCTN/PLGA microspheres
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Encapsulation and release characteristics of DCTN/PLGA microspheres

机译：DCTN / PLGA微球的包封和释放特性

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摘要

In the present study, poly (D,L-lactic-co-glycolic)-acid microspheres containing frans-Dehydrocrotonin (DCTN) were prepared by the double emulsion method. The hypoglycemic activity of DCTN-loaded microspheres was monitored in normal glycemic mice after administration of a daily dose of DCTN (50 mg kg~(-1) body weight) for 7 days. Spherical microspheres with two populations of particles with 3.20 ±0.10 and 7.60 ± 0.70 μm mean diameter size μm were observed. The encapsulation efficiency of DCTN was 85.5 ± 3.9%. The in vitro kinetic profile of DCTN from PLGA-microspheres was initially fast (burst effect of 19.4% at 2h). Such a burst step was maintained until achieving 35.7 ±2.0% at 7h, followed by a gradual release of DCTN attaining a maximum drug release at 55.7 ± 2.6% within 30 h. DCTN was able to reduce glucose levels (14.3%) of normal glycemic animals and this effect was improved by its encapsulation into microspheres (26.8%). The optimum glucose levels in the blood of animals treated with DCTN suspension and DCTN-loaded microspheres were 119.21 ±19.75 mgdL~(-1) at day 5 and 103.08 ± 18.88 mg dL~(_1) at day 7, respectively. DCTN-loaded microspheres are thus offered as a potential delivery system for the treatment of metabolic diseases characterized by hyperglycemia.
机译：在本研究中，通过双乳液法制备了含有氟烷-脱氢巴豆素（DCTN）的聚（D，L-乳酸-乙醇酸共聚物）-酸微球。在每日服用DCTN（50 mg kg〜（-1）体重）7天后，在正常血糖小鼠中监测DCTN加载的微球的降血糖活性。观察到球形微球具有两个粒子群，平均粒径为3.20±0.10和7.60±0.70μm。 DCTN的封装效率为85.5±3.9％。 PLGA微球DCTN的体外动力学曲线最初是快速的（2h时爆发效应为19.4％）。维持这样的爆发步骤，直到在7h达到35.7±2.0％，然后逐步释放DCTN，在30 h内达到55.7±2.6％的最大药物释放。 DCTN能够降低正常血糖动物的葡萄糖水平（14.3％），并且通过将其封装到微球中（26.8％）可以改善这种效果。在第5天，用DCTN悬浮液和装有DCTN的微球处理的动物血液中的最佳葡萄糖水平分别为119.21±19.75 mgdL〜（-1）和第7天为103.08±18.88 mg dL〜（_1）。因此，提供了装载DCTN的微球作为潜在的递送系统，用于治疗以高血糖为特征的代谢疾病。

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