Generally, topically applied eye drops have low bioavailability due to short residence time and low penetration of the drug. The aim of the present study was to incorporate dexamethasone (DXM) into nano lipid carriers (NLC), which contain mucoadhesive polymer, in order to increase the bioavailability of the drug. A 2³ factorial experimental design was applied, in which the three factors were the polymer, the DXM, and the emulsifier concentrations. The samples were analyzed for particle size, zeta potential, polydispersity index, and Span value. The significant factors were identified. The biocompatibility of the formulations was evaluated with human corneal toxicity tests and immunoassay analysis. The possible increase in bioavailability was analyzed by means of mucoadhesivity, in vitro drug diffusion, and different penetration tests, such as in vitro cornea PAMPA model, human corneal cell penetration, and ex vivo porcine corneal penetration using Raman mapping. The results indicated that DXM can be incorporated in stable mucoadhesive NLC systems, which are non-toxic and do not have any harmful effect on cell junctions. Mucoadhesive NLCs can create a depot on the surface of the cornea, which can predict improved bioavailability.

中文翻译：

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使用全因子设计开发和表征潜在的眼粘膜黏附纳米脂质载体。

通常，由于短的停留时间和药物的低渗透性，局部施用的滴眼剂具有低的生物利用度。本研究的目的是将地塞米松（DXM）掺入含有粘膜粘附聚合物的纳米脂质载体（NLC）中，以增加药物的生物利用度。2 ³应用析因实验设计，其中三个因素是聚合物，DXM和乳化剂浓度。分析样品的粒度，ζ电势，多分散指数和Span值。确定了重要因素。通过人角膜毒性试验和免疫测定分析评估制剂的生物相容性。通过粘膜粘附性，体外药物扩散和不同的渗透测试（例如体外角膜PAMPA模型，人角膜细胞渗透和离体猪角膜渗透），通过拉曼作图分析了生物利用度的可能增加。结果表明，DXM可掺入稳定的粘膜粘附NLC系统中，该系统无毒且对细胞连接无任何有害影响。