Physicochemical characterization of epigallocatechin gallate lipid nanoparticles (EGCG-LNs) for ocular instillation
Physicochemical characterization of epigallocatechin gallate lipid nanoparticles (EGCG-LNs) for ocular instillation
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DOI：
10.1016/j.colsurfb.2014.09.042
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发表时间：
2014-11-01
影响因子：
5.8
通讯作者：
Souto, Eliana B.
中科院分区：
文献类型：
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作者：
Fangueiro, Joana F.;Andreani, Tatiana;Souto, Eliana B.
将表没食子儿茶素没食子酸酯 (EGCG) 封装在脂质纳米颗粒 (LN) 中可能是避免药物氧化和差向异构化的合适方法，这些过程是导致药物生物利用度低、限制其治疗效果的常见过程。 EGCG 对人类健康的益处引起了制药领域的广泛关注，但迄今为止还没有研究报告将其封装在 LN 中。本研究的目的是开发一种创新系统，使用 LN 作为载体来眼部输送 EGCG，用于未来治疗多种疾病，如干眼、年龄相关性黄斑变性 (AMD)、青光眼、糖尿病性视网膜病变和黄斑水肿。 LNs 分散体是通过多重乳液技术生产的，并且之前通过因子设计进行了优化。为了通过静电吸引增加眼部保留时间和粘膜粘附，使用了两种不同的阳离子脂质，即十六烷基三甲基溴化铵（CTAB）和二甲基双十八烷基溴化铵（DDAB）。 EGCG 已成功加载到 LN 分散体中，并且对超过 30 天的储存时间的纳米颗粒分析预测其具有良好的物理化学稳定性。发现这些颗粒在纳米范围内（
The encapsulation of epigallocatechin gallate (EGCG) in lipid nanoparticles (LNs) could be a suitable approach to avoid drug oxidation and epimerization, which are common processes that lead to low bioavailability of the drug limiting its therapeutic efficacy. The human health benefits of EGCG gained much interest in the pharmaceutical field, and so far there are no studies reporting its encapsulation in LNs. The purpose of this study has been the development of an innovative system for the ocular delivery of EGCG using LNs as carrier for the future treatment of several diseases, such as dry eye, age-related macular degeneration (AMD), glaucoma, diabetic retinopathy and macular oedema. LNs dispersions have been produced by multiple emulsion technique and previously optimized by a factorial design. In order to increase ocular retention time and mucoadhesion by electrostatic attraction, two distinct cationic lipids were used, namely, cetyltrimethylammonium bromide (CTAB) and dimethyldioctadecylammonium bromide (DDAB). EGCG has been successfully loaded in the LNs dispersions and the nanoparticles analysis over 30 days of storage time predicted a good physicochemical stability. The particles were found to be in the nanometer range (