Alvarez Irene, Gutiérrez Cristina, Gracia Ignacio, Rodríguez Juan Francisco, García María Teresa
Department of Chemical Engineering, University of Castilla-La Mancha, Facultad de C.C. Químicas, Avda. Camilo José Cela 12, 13071 Ciudad Real, Spain.
Department Hydrogen and Power to X, Iberian Centre for Research in Energy Storage (CIIAE), Avda. Universidades s/n, 10003 Caceres, Spain.
ACS Omega. 2025 Jul 24;10(30):33946-33958. doi: 10.1021/acsomega.5c06385. eCollection 2025 Aug 5.
The use of polymeric microparticles is widely recognized as an effective strategy for enhancing the bioavailability and biodistribution of both lipophilic and hydrophilic medications. In this study, PLGA microparticles loaded with the anticancer drug gemcitabine were synthesized by using a double emulsion process known as water-in-oil-in-water solvent evaporation. Notably, this is the first time that ethyl lactate, an FDA-approved green solvent, has been used for the microparticle synthesis. For comparison, other solvents, such as ethyl acetate and dichloromethane, were also tested. The smallest particle size was achieved, regardless of the PLA:PGA ratio of the polymer, when using ethyl lactate under the following operational conditions: a high homogenizer speed (12,000 rpm) and an initial polymeric solution concentration of 1.5% w/v. Under these conditions, the encapsulation efficiency reached 45% for PLGA 50:50 and 35% for PLGA 75:25. Microparticle analysis revealed a homogeneous distribution (100-150 μm range) and a spherical shape. Furthermore, Fourier transform infrared (FTIR) spectroscopy confirmed the presence of gemcitabine in the microparticles.
使用聚合物微粒作为提高亲脂性和亲水性药物的生物利用度和生物分布的有效策略已得到广泛认可。在本研究中，通过一种称为水包油包水溶剂蒸发的双乳液法合成了负载抗癌药物吉西他滨的聚乳酸-羟基乙酸共聚物（PLGA）微粒。值得注意的是，这是首次将美国食品药品监督管理局（FDA）批准的绿色溶剂乳酸乙酯用于微粒合成。为作比较，还测试了其他溶剂，如乙酸乙酯和二氯甲烷。在以下操作条件下使用乳酸乙酯时，无论聚合物的聚乳酸（PLA）与聚羟基乙酸（PGA）比例如何，均可获得最小粒径：高均化器速度（12,000转/分钟）和初始聚合物溶液浓度为1.5%（w/v）。在这些条件下，PLGA 50:50的包封率达到45%，PLGA 75:25的包封率达到35%。微粒分析显示其分布均匀（范围为100 - 150μm）且呈球形。此外，傅里叶变换红外（FTIR）光谱证实了微粒中存在吉西他滨。
