目前，肝细胞癌（HCC）的常规治疗方法对肿瘤组织的选择性不够，导致多药耐药和药物毒性。尽管索拉非尼（SOR）是临床治疗HCC的标准一线系统疗法，但其水溶性差和快速清除导致吸收效率低，并严重限制其局部治疗的使用。本文介绍了通过乳酸-己内酯共聚物（PLGA）微球载荷SOR（PS）的可生物降解聚合物微球的合成过程。微球的特性进行了仔细的表征，重点关注微粒大小、表面电荷、形态学特征、药物载荷含量、封装效率、体外稳定性、药物释放行为，并对HepG2细胞进行了测试。此外，PLGA微球已与侧发射光纤（seOF）耦合在微流控器件中，用于光触发的局部释放。PS的尺寸为248 nm，具有可调节的表面电荷和均匀的球形形状，无聚集现象。PS显示了89.7％的封装效率和SOR负荷含量（8.9％），最高于带有SOR的PLGA制剂。将含有7.5 µM SOR的PS处理HepG2细胞，培养48、129和168小时后，细胞存活率分别降至40％、30％和17％。PS的高稳定性、持续释放特性和细胞内迅速摄取结果证实了其对HepG2细胞的增强细胞毒效应。展望开发控制药物的空间和时间释放的生物医学工具，我们成功展示了seOF光触发局部释放载体的潜力。我们的原型系统为集成微流控器件、光纤和先进载体的新型设备开辟了道路，能够实现微创的局部癌症治疗。© 2023 Caputo等人。

Currently, conventional treatments of hepatocellular carcinoma (HCC) are not selective enough for tumor tissue and lead to multidrug resistance and drug toxicity. Although sorafenib (SOR) is the standard first-line systemic therapy approved for the clinical treatment of HCC, its poor aqueous solubility and rapid clearance result in low absorption efficiency and severely limit its use for local treatment.Herein, we present the synthesis of biodegradable polymeric Poly (D, L-Lactide-co-glycolide) (PLGA) particles loaded with SOR (PS) by emulsion-solvent evaporation process. The particles are carefully characterized focusing on particle size, surface charge, morphology, drug loading content, encapsulation efficiency, in vitro stability, drug release behaviour and tested on HepG2 cells. Additionally, PLGA particles have been coupled on side emitting optical fibers (seOF) integrated in a microfluidic device for light-triggered local release.PS have a size of 248 nm, tunable surface charge and a uniform and spherical shape without aggregation. PS shows encapsulation efficiency of 89.7% and the highest drug loading (8.9%) between the SOR-loaded PLGA formulations. Treating HepG2 cells with PS containing SOR at 7.5 µM their viability is dampened to 40%, 30% and 17% after 48, 129 and 168 hours of incubation, respectively.The high PS stability, their sustained release profile and the rapid cellular uptake corroborate the enhanced cytotoxicity effect on HepG2. With the prospect of developing biomedical tools to control the spatial and temporal release of drugs, we successfully demonstrated the potentiality of seOF for light-triggered local release of the carriers. Our prototypical system paves the way to new devices integrating microfluidics, optical fibers, and advanced carriers capable to deliver minimally invasive locoregional cancer treatments.© 2023 Caputo et al.