Otto H. York Department of Chemical and Materials Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USA.
Middlesex Academy for Allied Health and Biomedical Sciences, Woodbridge, NJ 07095, USA.
Soft Matter. 2023 Jul 19;19(28):5371-5378. doi: 10.1039/d3sm00082f.
Poly(D,L-lactic--glycolic acid) (PLGA) is one of the most commonly used drug carriers in nanomedicines because of its biodegradability, biocompatibility and low toxicity. However, the physico-chemical characterization and study of drug release are often lacking the investigation of the glass transition temperature (), which is an excellent indicator of drug release behavior. In addition, the residual surfactant used during the synthesis of nanoparticles will change the glass transition temperature. We thus prepared PLGA nanoparticles with polymeric (poly(vinyl alcohol) (PVA)) and ionic (didodecyldimethylammonium bromide (DMAB)) surfactant to investigate their influence on the glass transition temperature. Determination of in dry and wet conditions were carried out. The use of concentrated surfactant during synthesis resulted in a larger amount of residual surfactant in the resulting particles. Increasing residual PVA content resulted in an increase in particle for all but the most concentrated PVA concentrations, while increasing residual DMAB content resulted in no significant change in particle . With the presence of residual surfactant, the of particle and bulk samples measured in wet conditions is much lower than that in dry conditions, except for bulk PLGA containing the ionic surfactant, which may be related to the plasticizing effect of the DMAB molecules. Notably, the of both particles in wet conditions is approaching physiological temperatures where subtle changes in could have dramatic effects on drug release properties. In conclusion, the selection of surfactant and the remaining amount of surfactant are crucial parameters to utilize in designing the physico-chemical properties of PLGA particles.
聚(D,L-乳酸-乙醇酸)(PLGA)是纳米医学中最常用的药物载体之一,因为它具有生物降解性、生物相容性和低毒性。然而,物理化学特性和药物释放研究通常缺乏对玻璃化转变温度(Tg)的研究,Tg 是药物释放行为的一个极好的指标。此外,在纳米粒子合成过程中使用的残留表面活性剂会改变玻璃化转变温度。因此,我们制备了具有聚合物(聚乙烯醇(PVA))和离子(双十二烷基二甲基溴化铵(DMAB))表面活性剂的 PLGA 纳米粒子,以研究它们对玻璃化转变温度的影响。在干燥和湿润条件下进行了 Tg 的测定。在合成过程中使用浓缩的表面活性剂会导致生成的颗粒中残留的表面活性剂含量增加。增加残留 PVA 的含量会导致除最浓 PVA 浓度外,所有浓度的颗粒的 Tg 增加,而增加残留 DMAB 的含量则不会导致颗粒的 Tg 发生显著变化。由于存在残留表面活性剂,在湿润条件下测量的颗粒和块状样品的 Tg 远低于干燥条件下的 Tg,除了含有离子表面活性剂的 PLGA 块状样品外,这可能与 DMAB 分子的塑化作用有关。值得注意的是,在湿润条件下,两种颗粒的 Tg 都接近生理温度,Tg 的微小变化可能对药物释放性质产生巨大影响。总之,表面活性剂的选择和残留表面活性剂的量是设计 PLGA 颗粒物理化学性质的关键参数。