Novartis Pharma AG, Postfach 4002, Basel, Switzerland.
Pole of Pediatric Hepatology, Institute of Clinical and Experimental Research (IREC), Université catholique de Louvain, Brussels, Belgium; Advanced Drug Delivery and Biomaterials, Louvain Drug Research Institute (LDRI), Université catholique de Louvain, Brussels, Belgium.
J Control Release. 2018 Nov 10;289:10-13. doi: 10.1016/j.jconrel.2018.09.017. Epub 2018 Sep 20.
Poly(lactic-co-glycolic acid) (PLGA) is well known for its biocompatibility and minimal toxicity. It is one of the most promising biodegradable polymeric drug delivery systems able to get endorsement from regulatory bodies to enter market. For many decades, PLGA has been functioning as an excipient, which by definition is pharmaceutically inert at a given dose of formulation. Lactate (one of the hydrolysis products of PLGA) has a key role in biochemical pathways and could improve physiological activities in certain illnesses by exerting therapeutic effects such as angiogenesis and promotion of healing. These activities, however, depend on the released amounts and metabolic clearance of lactate and route of formulation delivery. In the current commentary, along with several key notes on the lactate interactions, we would like to inform the PLGA research community that lactate (resulting from local delivery of physiologically significant amount of PLGA) may positively or negatively affect therapeutic efficacy of certain drugs. Hence, the excipient role of PLGA may be investigated for its potential pharmacological contributions in some biomedical applications.
聚（乳酸-共-乙醇酸）（PLGA）以其生物相容性和低毒性而闻名。它是最有前途的可生物降解聚合物药物输送系统之一，能够获得监管机构的批准进入市场。几十年来，PLGA 一直作为赋形剂发挥作用，根据定义，在给定剂量的制剂中，赋形剂在药物上是惰性的。乳酸（PLGA 的水解产物之一）在生化途径中起着关键作用，通过发挥血管生成和促进愈合等治疗作用，可以改善某些疾病的生理活性。然而，这些活性取决于乳酸的释放量和代谢清除率以及制剂递送途径。在当前的评论中，我们将结合关于乳酸相互作用的几个要点，告知 PLGA 研究界，乳酸（源自局部输送生理上大量的 PLGA）可能会对某些药物的治疗效果产生积极或消极的影响。因此，PLGA 的赋形剂作用可能会因其在某些生物医学应用中的潜在药理学贡献而受到研究。
