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载左氧氟沙星原位凝胶纳米粒以增强眼部滞留

Nanoparticles laden in situ gel of levofloxacin for enhanced ocular retention.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard , New Delhi , India and.

出版信息

Drug Deliv. 2013 Sep-Oct;20(7):306-9. doi: 10.3109/10717544.2013.838712.

Abstract

Availability of proper concentration of medicament on to the corneal surface is a challenging task. Many novel formulations, i.e. hydrogels, nanoparticles, ocuserts, etc. had been tested to improve ocular bioavailability, out of which our group found, in situ gel and polymeric nanoparticle are the most interesting approach to achieve ocular retention. We found that in situ gel stay only for 12 h and poly(lactic-co-glycolic acid (PLGA) nanoparticles are non mucoadhesive in nature so we try to combine both these formulations and termed it as "Nanoparticle laden in situ gel". Here we prepare nanoparticle laden in situ gel containing levofloxacin encapsulated PLGA nanoparticle, incorporated in chitosan in situ gel and evaluated its ocular retention by gamma scintigraphy in rabbits. The observations of acquired gamma camera images showed good retention over the entire precorneal area. From static and dynamic gamma scintigraphy evaluation, we can be interpret that developed nanoparticle laden in situ gel formulation cleared at a very slow rate and remained at corneal surface for longer duration than marketed formulation, in situ gel and nanosuspension alone.

摘要

将适当浓度的药物递送到角膜表面是一项具有挑战性的任务。许多新型制剂,如凝胶、纳米颗粒、眼用黏弹剂等,已被测试用于提高眼部生物利用度,其中我们小组发现,原位凝胶和聚合物纳米颗粒是实现眼部滞留的最有趣的方法。我们发现原位凝胶只能持续 12 小时,而聚(乳酸-共-乙醇酸)(PLGA)纳米颗粒在性质上是非黏膜附着的,因此我们试图将这两种制剂结合起来,并将其命名为“载纳米颗粒的原位凝胶”。在这里,我们制备了载有左氧氟沙星包封 PLGA 纳米颗粒的载纳米颗粒的原位凝胶,将其掺入壳聚糖原位凝胶中,并通过兔眼γ闪烁显像法评估其眼部滞留情况。获得的γ相机图像观察结果显示,整个角膜前区域具有良好的滞留性。从静态和动态γ闪烁显像评估可以看出,与市售的原位凝胶和纳米混悬剂相比,开发的载纳米颗粒的原位凝胶制剂的清除速度非常缓慢,并且在角膜表面的滞留时间更长。

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