Poly lactic-co-glycolic acid particles are biodegradable and biocompatible drug delivery systems that provide a controlled release of drugs in specific sites. These characteristics minimize the occurrence of side effects related to overdosing. To overcome the issues associated with the conservative treatment for wound healing, the objective of this work was to develop a poly lactic-co-glycolic acid particles system to deliver anti-inflammatory compounds (epigallocatechin gallate and asiaticoside) to fibroblasts. Nanoscale (~200 nm) and microscale (~10 µm) poly lactic-co-glycolic acid particles were produced using two different protocols. Nanoscale particles reduced cell proliferation by 46% compared with untreated human skin fibroblasts, whereas microscale particles did not affect fibroblast viability significantly. The toxicity of nanoparticles and the nontoxic nature of microparticles were confirmed in live and dead cell staining experiments. In vitro drug release assays showed that particles containing epigallocatechin gallate and asiaticoside were able to release most of their payload during the first 8 h of incubation. The treatment of lipopolysaccharide-stimulated fibroblasts with epigallocatechin gallate- and asiaticoside-loaded microparticles effectively suppressed the expression of inflammatory factors: tumor necrosis factor-α, interleukin-1β, and interleukin-6. In this study, we found that the optimal size of biodegradable poly lactic-co-glycolic acid particles for the delivery of physiologically active substances to fibroblasts is about 10 μm. Moreover, our findings indicate that poly lactic-co-glycolic acid particles of this size can be effectively applied to ameliorate tissue regeneration by delivering physiologically active substances to improve skin lesion recovery.

中文翻译：

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用于皮肤损伤恢复的含有抗炎物质的聚乳酸-乙醇酸共聚物颗粒的生产和表征

聚乳酸-乙醇酸共聚物颗粒是可生物降解和生物相容性的药物递送系统，可在特定部位提供药物的受控释放。这些特性最大限度地减少了与过量服用相关的副作用的发生。为了克服与伤口愈合保守治疗相关的问题，这项工作的目的是开发一种聚乳酸-乙醇酸共聚物颗粒系统，将抗炎化合物（表没食子儿茶素没食子酸酯和积雪草苷）输送到成纤维细胞。纳米级 (~200 nm) 和微米级 (~10 µm) 聚乳酸-乙醇酸共聚物颗粒是使用两种不同的协议生产的。与未经处理的人皮肤成纤维细胞相比，纳米级颗粒使细胞增殖减少了 46%，而微米级颗粒并未显着影响成纤维细胞的活力。在活细胞和死细胞染色实验中证实了纳米颗粒的毒性和微粒的无毒性质。体外药物释放试验表明，含有表没食子儿茶素没食子酸酯和积雪草苷的颗粒在孵化的前 8 小时内能够释放大部分有效载荷。用载有表没食子儿茶素没食子酸酯和积雪草苷的微粒处理脂多糖刺激的成纤维细胞可有效抑制炎症因子的表达：肿瘤坏死因子-α、白细胞介素-1β和白细胞介素-6。在这项研究中，我们发现可生物降解的聚乳酸-乙醇酸共聚物颗粒用于将生理活性物质输送到成纤维细胞的最佳尺寸约为 10 μm。而且，