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使用全因子设计开发和表征潜在的眼用粘膜粘附纳米脂质载体

Development and Characterization of Potential Ocular Mucoadhesive Nano Lipid Carriers Using Full Factorial Design.

作者信息

Kiss Eszter L, Berkó Szilvia, Gácsi Attila, Kovács Anita, Katona Gábor, Soós Judit, Csányi Erzsébet, Gróf Ilona, Harazin András, Deli Mária A, Balogh György T, Budai-Szűcs Mária

机构信息

Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.

Department of Ophthalmology, Faculty of Medicine, University of Szeged, Korányi Fasor 10-11, H-6720 Szeged, Hungary.

出版信息

Pharmaceutics. 2020 Jul 20;12(7):682. doi: 10.3390/pharmaceutics12070682.

DOI:10.3390/pharmaceutics12070682
PMID:32698334
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7408368/
Abstract

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 2 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.

摘要

一般来说，由于药物的停留时间短和渗透率低，局部应用的眼药水生物利用度较低。本研究的目的是将地塞米松（DXM）纳入含有粘膜粘附聚合物的纳米脂质载体（NLC）中，以提高药物的生物利用度。采用二因素实验设计，其中三个因素是聚合物、DXM和乳化剂浓度。对样品进行粒径、zeta电位、多分散指数和Span值分析。确定了显著因素。通过人角膜毒性试验和免疫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试验，如体外角膜PAMPA模型、人角膜细胞渗透和使用拉曼映射的离体猪角膜渗透，分析生物利用度可能的增加。结果表明，DXM可以纳入稳定的粘膜粘附NLC系统，该系统无毒且对细胞连接没有任何有害影响。粘膜粘附NLC可以在角膜表面形成一个储库，这可以预测生物利用度的提高。

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