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载有用于眼科药物递送的三羟甲基氨基甲烷的聚乙烯醇-羟乙基纤维素插入物浸渍的尤特奇®L100纳米颗粒的制备与评价

Preparation and Evaluation of Eudragit® L100 Nanoparticles Loaded Impregnated with KT Tromethamine Loaded PVA -HEC Insertions for Ophthalmic Drug Delivery.

作者信息

Mohammadi Ghobad, Mirzaeei Shahla, Taghe Shiva, Mohammadi Pardis

机构信息

Pharmaceutical Sciences Research Center, Health Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran.

出版信息

Adv Pharm Bull. 2019 Oct;9(4):593-600. doi: 10.15171/apb.2019.068. Epub 2019 Oct 24.

Abstract

The purpose of the present study was to improve the ocular delivery for ketorolac tromethamine (KT) used to treat inflammation of the eye. Eudragit nanoparticles loaded with KT were prepared and incorporated in polyvinyl alcohol (PVA) and hydroxyethyl cellulose (HEC) films. Nanoparticles were characterized by Fourier transform-infrared (FT-IR), scanning electron microscopy (SEM). Physicochemical properties and encapsulation effciency were investigated for nanoparticles. Also, the inserts were evaluated for their physiochemical parameters like percentage moisture absorption, percentage moisture loss, thickness and folding endurance. Mean particle size and zeta potential were in range of 153.8-217 nm and (-10.8) - (-40.7) mV, respectively. The results show that the use of a surfactant has not led to any major change on drug loading. The loading increases with the amount of polymer. The insert had a thickness varying from 0.072 ± 0.0098 to 0.0865 ± 0.0035 mm. The thicknesses of the inserts and the folding endurance increased with the total polymer concentration. The physicochemical properties showed that the Eudragit® L-100 nanoparticles loaded PVA-HEC films could be an effective carrier for KT. For the first time, inserts of Eudragit nanoparticles were successfully prepared for ophthalmic drug delivery system to prevent frequent drug administration and enhance patient compliance.

摘要

本研究的目的是改善用于治疗眼部炎症的酮咯酸氨丁三醇(KT)的眼部给药。制备了负载KT的Eudragit纳米颗粒,并将其掺入聚乙烯醇(PVA)和羟乙基纤维素(HEC)薄膜中。通过傅里叶变换红外光谱(FT-IR)、扫描电子显微镜(SEM)对纳米颗粒进行表征。研究了纳米颗粒的物理化学性质和包封效率。此外,还对插入物的物理化学参数进行了评估,如吸湿率、失湿率、厚度和耐折性。平均粒径和zeta电位分别在153.8 - 217 nm和(-10.8) - (-40.7)mV范围内。结果表明,表面活性剂的使用并未导致药物负载量发生任何重大变化。负载量随聚合物用量的增加而增加。插入物的厚度在0.072±0.0098至0.0865±0.0035 mm之间变化。插入物的厚度和耐折性随聚合物总浓度的增加而增加。物理化学性质表明,负载Eudragit® L-100纳米颗粒的PVA-HEC薄膜可能是KT的有效载体。首次成功制备了用于眼科给药系统的Eudragit纳米颗粒插入物,以防止频繁给药并提高患者依从性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/88ba/6912175/eae99c6e9620/apb-9-593-g001.jpg

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