Enhancing the efficacy of fluocinolone acetonide by encapsulating with PLGA nanoparticles and conjugating with linear PEG polymer

Zeta电位 化学 PEG比率 氟辛醇酮 纳米颗粒 粒径 色谱法 分散性 PLGA公司 肉豆蔻酸异丙酯 析因实验 高效液相色谱法 结合 核化学 材料科学 纳米技术 高分子化学 医学 经济 物理化学 统计 数学 财务 数学分析 眼科
作者
Joyce Pinto,Madiha Ahmad,Bharath Raja Guru
出处
期刊:Journal of Biomaterials Science-polymer Edition [Informa]
卷期号:30 (13): 1188-1211 被引量:11
标识
DOI:10.1080/09205063.2019.1625524
摘要

Fluocinolone acetonide (FA), a glucocorticoid is used to treat inflammation in the posterior segment of the eye. Due to short half-life and body clearance, it will not be able to give therapeutic effect for long time with a single injection. Formulating FA nanoparticles (NPs) or PEG conjugates can be an effective way to overcome these disadvantages. We prepared two formulations, FA loaded in PLGA nanoparticles (NPs-FA) and FA conjugated to linear PEG (PEG-FA). The NPs-FA were characterised for size and zeta potential using particle size analyser and shape and morphology by using scanning electron microscope (SEM). The amount of drug loaded per mg of NPs and in-vitro release of FA from NPs were calculated using reverse phase high pressure liquid chromatography (RP-HPLC). NPs synthesis was optimized with factorial and Response Surface Methodology (RSM). Chemically synthesized PEG-FA conjugates were characterized using H-NMR and purity of the conjugate was analysed using RP-HPLC. Visualization of cellular uptake of NPs was done by coumarin-6 loaded NPs under fluorescent microscope. RAW 264.7 macrophages were treated with NPs-FA and PEG-FA conjugates to study their effectiveness in inhibiting TNF-α levels compared to free FA treatment. Stability test confirmed that FA is more stable within NPs than in free form. Particle size and zeta potential were found to be 183.6 ± 12.47nm and −25.6 ± 4.4mV, respectively. 149.58 ± 11.3µg of FA was encapsulated per mg of NPs and 61 µg of FA was present per mg of PEG-FA conjugate. In vitro drug release study showed a sustained release of FA from the NPs for a period of 30 days. Fluorescent microscope images showed uptake of NPs by RAW 264.7 cells. TNF-α assay confirmed that substantial inhibition of TNF-α levels from both formulations compared to free FA. From the results, we conclude that new formulations will greatly reduce drug dosage and frequency of administration for long term treatment of inflammation in posterior part of the eye.
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