Shenyang Pharmaceutical University, School of Pharmacy, Shenyang, China.
Expert Opin Drug Deliv. 2012 Sep;9(9):1161-76. doi: 10.1517/17425247.2012.709844. Epub 2012 Jul 27.
Polymeric microspheres have been established as a valuable parenteral drug delivery system for sustained release of therapeutic agents via subcutaneous or intramuscular injection.
Biodegradable polymers which are either synthetic or from natural sources are reviewed with respect to recent advances in exploring their applications for microsphere fabrications. New information on the impact of formulation variables on the properties of microspheres formed by an emulsion method was also presented. The characterization of microspheres using advanced physical analytical techniques was also reviewed and the utilization of the information in assessing in vivo performance of the product was also highlighted.
The broad clinical use of microspheres for delivery of therapeutic agents in particular biologics such as proteins has not been realized commercially. The limited availability of biodegradable polymers with a long history of regulatory approval and the challenges in gaining regulatory approval of a new polymer have hindered the development of microspheres for parenteral drug delivery.
高分子微球已被确立为一种有价值的注射型药物传递系统，可通过皮下或肌肉注射实现治疗剂的缓释。
本文综述了可生物降解的聚合物，包括合成聚合物和天然来源聚合物，探讨了它们在微球制备方面的应用进展。还介绍了关于通过乳液法制备微球时，制剂变量对微球性质影响的新信息。本文还综述了使用先进的物理分析技术对微球进行表征，并强调了利用这些信息评估产品体内性能的重要性。
尽管微球在递送治疗剂方面具有广泛的临床应用，特别是在蛋白类生物制剂方面，但尚未实现商业化。具有长期监管审批历史的可生物降解聚合物的供应有限，以及获得新聚合物监管审批的挑战，都阻碍了微球在注射型药物传递方面的发展。
