Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028, Barcelona, Spain.
Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028, Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, Barcelona, Spain.
Colloids Surf B Biointerfaces. 2019 Mar 1;175:365-374. doi: 10.1016/j.colsurfb.2018.11.065. Epub 2018 Nov 27.
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.
已经开发和优化了温敏凝胶，使其在角膜温度下变成凝胶，并且具有一定的粘度，可以使载有氟米龙（FMT）的 PLGA 纳米颗粒（NPs）充分释放，以提高针对商业制剂的眼部抗炎功效。研究表明，凝胶可避免药物在最初几小时内的爆发释放，在给药后呈现缓慢且逐渐增加的释放模式。纳米颗粒在凝胶中保持其平均粒径和球形，这一点通过透射电子显微镜（TEM）得到了证实。反过来，制剂的原位凝胶化使其能够以眼药水的形式给药，因为其在 25°C 以下的温度下呈溶液状态。眼部耐受性研究表明，没有一种制剂会引起眼部刺激。所开发制剂的给药改善了角膜前停留时间，从而反映了眼部生物利用度的提高，其中包括房水和晶状体等深层组织。总之，温敏凝胶用于 NPs 的局部应用已证明其在眼部炎症性疾病的急性和预防性治疗中的有效性。
