In-situ forming gels containing fluorometholone-loaded polymeric nanoparticles for ocular inflammatory conditions

纳米颗粒 剂型 材料科学 生物利用度 药物输送 房水 PLGA公司 水溶液 化学 生物医学工程 色谱法 化学工程 房水 纳米技术 药理学 眼科 医学 有机化学 工程类
作者
Roberto González-Pizarro,Paulina Carvajal-Vidal,Lyda Halbaut,Ana C. Calpena,Marta Espina,María L. García
出处
期刊:Colloids and Surfaces B: Biointerfaces [Elsevier BV]
卷期号:175: 365-374 被引量:59
标识
DOI:10.1016/j.colsurfb.2018.11.065
摘要

Thermosensitive gels have been developed and optimized in such a way that they become gels at corneal temperature and with a viscosity that allows the adequate release of the Fluorometholone (FMT)-loaded PLGA nanoparticles (NPs) in order to improve ocular anti-inflammatory efficacy against a commercial formulation. It has been shown that gels avoid burst release of the drug in the first hours with a slow and increasing profile after administration. NPs have maintained their average size and spherical shape within the gels as confirmed by transmission electron microscopy (TEM). In turn, the in-situ gelling of the formulations allows the administration in eye drops dosage form due to its state of sol at temperatures below 25 °C. Ocular tolerance studies have shown that no formulation causes eye irritation. The administration of the developed formulations has improved the precorneal residence time reflected in the ocular bioavailability, where deep tissues as aqueous humour and crystalline were reached. In conclusion, the use of thermosensitive gels for the topical application of NPs has demonstrated their effectiveness in the acute and preventive treatment of ocular inflammatory conditions.

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