Preparation and in vitro-in vivo evaluation of salmon calcitonin-loaded polymeric nanoparticles
Preparation and in vitro-in vivo evaluation of salmon calcitonin-loaded polymeric nanoparticles
复制标题
DOI：
10.3109/02652040902751125
复制
发表时间：
2010-01-01
影响因子：
3.9
通讯作者：
Maincent, Philippe
中科院分区：
文献类型：
--
作者：
Glowka, Eliza;Sapin-Minet, Anne;Maincent, Philippe
本研究的目的是开发和表征聚合物纳米颗粒作为鲑鱼降钙素（sCT）的缓释系统。使用Eudragit RS和两种类型的可生物降解的聚（乳酸-共-乙醇酸）共聚物（PLGA），通过双乳液溶剂蒸发法制备纳米颗粒。结果表明，sCT被掺入纳米颗粒中，包封效率在69- 83%的范围内。在体外释放研究，非常规地在5%乙酸中进行，显示sCT释放时间曲线的巨大差异。具有快速释放特性的纳米颗粒（RS，PLGA/RS）在几小时内释放80-100%的包封药物。相比之下，纯PLGA纳米颗粒的sCT释放非常缓慢，不完全，4周后仅达到20%。在Wistar大鼠中进行的体内研究证明，皮下给予PLGA纳米颗粒后，血清sCT水平升高可持续3天，并且与sCT溶液相比，达到的生物利用度增加。
The aim of the study was to develop and characterize polymeric nanoparticles as a sustained release system for salmon calcitonin (sCT). Nanoparticles were prepared by a double emulsion solvent evaporation method using Eudragit (R) RS and two types of a biodegradable poly(lactic-co-glycolic) copolymer (PLGA). It was demonstrated that sCT was incorporated into nanoparticles with encapsulation efficiencies in the range 69-83%. In vitro release studies, unconventionally conducted in 5% acetic acid, showed great differences in sCT release time profiles. Nanoparticles with fast release profile (Eudragit (R) RS, PLGA/Eudragit (R) RS) released 80-100% of the encapsulated drug within a few hours. In contrast, the sCT release from pure PLGA nanoparticles was very slow, incomplete and reached only 20% after 4 weeks. In vivo study, conducted in Wistar rats, proved that elevated serum sCT levels could be sustained for 3 days after subcutaneous administration of PLGA nanoparticles and the achieved bioavailability was increased compared to sCT solution.