Fujisawa Ryo, Sakurai Ryuse, Oshizaka Takeshi, Mori Kenji, Saitoh Akiyoshi, Takeuchi Issei, Sugibayashi Kenji
Department of Medical Pharmacy, Graduate School of Pharmaceutical Sciences, Josai International University, 1 Gumyo Togane, Chiba 283-0002, Japan.
Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641, Yamazaki, Noda 278-8510, Japan.
Molecules. 2025 Aug 6;30(15):3292. doi: 10.3390/molecules30153292.
This study focused on the poly(DL-lactide--glycolide)--poly(ethylene glycol)--poly(DL-lactide--glycolide) (PLGA-PEG-PLGA) triblock copolymer, which was recently reported as a novel material for polymeric nanoparticles to replace poly(DL-lactide--glycolide) (PLGA) as a drug carrier for prednisolone (PSL), and aimed to evaluate the efficacy of PSL-loaded PLGA-PEG-PLGA nanoparticles (NPs) against allergic contact dermatitis (ACD). PSL-loaded PLGA-PEG-PLGA NPs were prepared using the nanoprecipitation method, and their particle size distribution and mean particle size were measured using dynamic light scattering. 1-Fluoro-2,4-dinitrobenzene (DNFB) was used to create a mouse model of contact hypersensitivity (CHS). PSL-loaded PLGA-PEG-PLGA NPs were administered before sensitization with DNFB, and the therapeutic effect was evaluated by quantifying intracutaneous TNF-α and IL-4 levels suing ELISA. When PSL-loaded PLGA-PEG-PLGA NPs were administered before sensitization, TNF-α expression and IL-4 statements were significantly lower in the PSL-loaded PLGA-PEG-PLGA NP group than in the non-treated group. No significant difference was observed between the PSL-loaded PLGA-PEG-PLGA NP and PSL-loaded ointment groups, even though the steroid dose was 40 times lower than in the PSL-containing ointment. These results suggest that PSL-loaded PLGA-PEG-PLGA NPs may have a better effect in the treatment of ACD than PSL-loaded PLGA NPs.
本研究聚焦于聚（DL-丙交酯-乙交酯）-聚（乙二醇）-聚（DL-丙交酯-乙交酯）（PLGA-PEG-PLGA）三嵌段共聚物，该共聚物最近被报道为一种用于聚合物纳米颗粒的新型材料，可替代聚（DL-丙交酯-乙交酯）（PLGA）作为泼尼松龙（PSL）的药物载体，旨在评估负载PSL的PLGA-PEG-PLGA纳米颗粒（NPs）对过敏性接触性皮炎（ACD）的疗效。采用纳米沉淀法制备负载PSL的PLGA-PEG-PLGA NPs，并使用动态光散射测量其粒径分布和平均粒径。使用1-氟-2,4-二硝基苯（DNFB）建立接触性超敏反应（CHS）小鼠模型。在DNFB致敏前给予负载PSL的PLGA-PEG-PLGA NPs，并通过酶联免疫吸附测定（ELISA）定量皮内肿瘤坏死因子-α（TNF-α）和白细胞介素-4（IL-4）水平来评估治疗效果。当在致敏前给予负载PSL的PLGA-PEG-PLGA NPs时，负载PSL的PLGA-PEG-PLGA NP组中的TNF-α表达和IL-4水平显著低于未治疗组。负载PSL的PLGA-PEG-PLGA NP组与负载PSL的软膏组之间未观察到显著差异，尽管类固醇剂量比含PSL的软膏低40倍。这些结果表明，负载PSL的PLGA-PEG-PLGA NPs在治疗ACD方面可能比负载PSL的PLGA NPs具有更好的效果。
