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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >In vitro and in vivo properties of usnic acid encapsulated into PLGA-microspheres
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In vitro and in vivo properties of usnic acid encapsulated into PLGA-microspheres

机译：包裹在PLGA微球中的松萝酸的体外和体内特性

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Microparticles will probably play a promising role in the future of chemotherapy.These polymeric delivery systems are capable of maximizing the therapeutic activity while reducing side effects of anti-cancer agents.Usnic acid(UA)is a secondary metabolite produced by lichens,which exhibits an anti-tumour activity.In this study,PLGA-microspheres containing usnic acid from Cladonia substellata were prepared by the double emulsion method,with or without PEG as stabilizer.The morphology of the microspheres was examined by optical and scanning electron microscopy.The in vitro kinetic profile of usnic acid loaded-microspheres was carried out by dissolution testing.The usnic acid content was analysed by HPLC.The cytotoxicity of free and encapsulated usnic acid was evaluated against HEp-2 cells using the MTT method.The anti-tumour assay was performed in mice against Sarcoma-180 tumour(UA 15 mg kg~(-1)weight body/day)during 7 days.Animals were then sacrificed and tumour and organs were excised for histopathological analysis.Microspheres presented a smooth spherical surface with a mean diameter of 7.02 +-2.72 mum.The usnic acid encapsulation efficiency was approx100%(UA 10 mg 460 mg~(-1)microspheres).A maximum release of 92% was achieved at the fifth day.The IC_(50)values for free and encapsulated usnic acid were 12 and 14 mug ml~(-1),respectively.The encapsulation of usnic acid into microspheres promoted an increase of 21% in the tumour inhibition as compared with the free usnic acid treatment.In summary,usnic acid was efficiently encapsulated into PLGA-microspheres and the microencapsulation improved its anti-tumour activity.
机译：微粒可能在化学疗法的未来中起着有希望的作用。这些聚合物递送系统能够最大化治疗活性，同时减少抗癌药的副作用。松香酸（UA）是地衣的次生代谢产物，具有本研究采用双乳化法制备了含松枝线虫松萝酸的PLGA微球，采用或不使用PEG作为稳定剂。通过光学和扫描电镜观察了微球的形貌。用溶出度测试法测定了负载松香酸微球的动力学特性，通过高效液相色谱法分析了松香酸含量，采用MTT法评估了游离和包封的松香酸对HEp-2细胞的细胞毒性，并进行了抗肿瘤试验。在7天内针对小鼠肉瘤180瘤（UA 15 mg kg〜（-1）体重/天）进行实验，然后处死动物并切除肿瘤和器官微球呈光滑的球形表面，平均直径为7.02±-2.72微米。松萝酸的包封率约为100％（UA 10 mg 460 mg〜（-1）微球），最大释放率为92％游离和包裹的松萝酸的IC_（50）值分别为12和14毫升/ ml〜（-1）。将松萝酸包裹到微球中促进了21％的抑瘤作用。总之，将松香酸有效地包封在PLGA微球中，微囊化提高了其抗肿瘤活性。

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