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载 25- 羟维生素 D3 的 PLA 微球:体外特性鉴定及其在糖尿病牙周炎模型中的应用。

25-Hydroxyvitamin D(3)-loaded PLA microspheres: in vitro characterization and application in diabetic periodontitis models.

机构信息

State Key Laboratory of Oral Diseases, West China Hospital of Stomatology, Sichuan University, 14 3rd Section S Renmin Road, Chengdu 610041, China.

出版信息

AAPS PharmSciTech. 2013 Jun;14(2):880-9. doi: 10.1208/s12249-013-9978-5. Epub 2013 May 8.

Abstract

This study aimed at the preparation of a sustained-release 25-hydroxyvitamin D(3) (25OHD) treatment for diabetic periodontitis, a known complication of diabetes. 25OHD-loaded polylactic acid (PLA) microspheres were prepared using oil-in-water emulsion-solvent evaporation method. The prepared microspheres exhibited intact surfaces, with average sizes ranging from 42.3 to 119.4 μm. The encapsulation efficiency ranged from 79.2% (w/w) to 88.5% (w/w), and the drug content was between 15.8% (w/w) and 17.8% (w/w). Drug release from the produced microspheres followed a near-to-zero-order release pattern and lasted over 10 weeks. In an in vitro model of diabetic periodontitis, the abnormal morphological changes and the decrease in the cell viability of bone marrow stromal cells could be effectively attenuated after the 25OHD-loaded microsphere application. Additionally, in a rat model of diabetic periodontitis, alveolar bone loss was inhibited and osteoid formation in the periodontium was promoted upon 25OHD-loaded microsphere treatment. In conclusion, 25OHD-loaded PLA microspheres may provide an effective approach for the treatment of this disease.

摘要

本研究旨在制备一种用于治疗糖尿病牙周炎的维生素 D3(25OHD)缓释制剂,糖尿病牙周炎是糖尿病的一种已知并发症。采用油包水乳液-溶剂蒸发法制备载 25OHD 的聚乳酸(PLA)微球。所制备的微球表面完整,平均粒径为 42.3 至 119.4μm。包封效率在 79.2%(w/w)至 88.5%(w/w)之间,载药量在 15.8%(w/w)至 17.8%(w/w)之间。所制得的微球中药物释放遵循近零级释放模式,持续超过 10 周。在糖尿病牙周炎的体外模型中,载 25OHD 微球应用后可有效减轻骨髓基质细胞的异常形态变化和细胞活力下降。此外,在糖尿病牙周炎大鼠模型中,载 25OHD 微球治疗可抑制牙槽骨丢失和牙周组织中类骨质形成。总之,载 25OHD 的 PLA 微球可能为该疾病的治疗提供一种有效的方法。

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