MedinCell, 3 Rue des Frères Lumière, Jacou 34830, France.
MedinCell, 3 Rue des Frères Lumière, Jacou 34830, France.
J Control Release. 2020 Mar 10;319:416-427. doi: 10.1016/j.jconrel.2020.01.022. Epub 2020 Jan 10.
This article presents BEPO®, an in situ forming depot (ISFD) technology mediated by a solvent-exchange mechanism. The matrix of the in situ formed drug delivery depot is composed of the combination of a diblock (DB) and a triblock (TB) polyethylene glycol-polyester copolymer. This combination offers a broad capability to tune the release of a wide variety of drugs to the desired pharmacokinetics. The work described in the present article demonstrates that the delivery rate and profile can be adjusted by changing the composition of either TB or DB or the relative ratio between them, among other parameters. It has been shown that the polymeric composition of the formulation has a substantial impact on the solvent exchange rate between the organic solvent and the surrounding aqueous medium which subsequently determines the internal structure of the resulting depot and the delivery of the therapeutic cargo. This has been demonstrated studying the in vitro release of two model molecules: bupivacaine and ivermectin. Formulations releasing these drugs have been administered to animal models to show the possibility of delivering therapeutics from weeks to months by using BEPO® technology.
本文介绍了 BEPO®，这是一种通过溶剂交换机制介导的原位形成储库（ISFD）技术。原位形成的药物递送储库的基质由二嵌段（DB）和三嵌段（TB）聚乙二醇-聚酯共聚物的组合构成。这种组合提供了广泛的能力，可以根据所需的药代动力学来调整各种药物的释放。本文所述的工作表明，可以通过改变 TB 或 DB 的组成、它们之间的相对比例或其他参数来调整输送速率和曲线。已经表明，制剂的聚合物组成对有机溶剂和周围水介质之间的溶剂交换率有实质性影响，这随后决定了所得储库的内部结构和治疗货物的输送。通过研究两种模型分子：布比卡因和伊维菌素的体外释放来证明这一点。已经向动物模型中施用了释放这些药物的制剂，以展示使用 BEPO®技术从数周到数月输送治疗剂的可能性。
