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Nanoparticles laden in situ gel for sustained ocular drug delivery

机译:载有原位凝胶的纳米颗粒可实现持续的眼部药物输送

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Proper availability of drug on to corneal surface is a challenging task. However, due to ocular physiological barriers, conventional eye drops display poor ocular bioavailability of drugs (< 1%). To improve precorneal residence time and ocular penetration, earlier our group developed and evaluated in situ gel and nanoparticles for ocular delivery. In interest to evaluate the combined effect of in situ gel and nanoparticles on ocular retention, we combined them. We are the first to term this combination as “nanoparticle laden in situ gel”, that is, poly lactic co glycolic acid nanoparticle incorporated in chitosan in situ gel for sparfloxacin ophthalmic delivery. The formulation was tested for various physicochemical properties. It showed gelation pH near pH 7.2. The observation of acquired gamma camera images showed good retention over the entire precorneal area for sparfloxacin nanoparticle laden in situ gel (SNG) as compared to marketed formulation. SNG formulation cleared at a very slow rate and remained at corneal surface for longer duration as no radioactivity was observed in systemic circulation. The developed formulation was found to be better in combination and can go up to the clinical evaluation and application.KEY WORDS: Gamma scintigraphy, in situ gel, nanoparticle, nanoparticle laden in situ gel, ocular, PLGA, sparfloxacin
机译:药物在角膜表面的正确供应是一项艰巨的任务。然而,由于眼部生理障碍,常规滴眼剂显示出不良的眼部药物生物利用度(<1%)。为了改善角膜前停留时间和眼部穿透力,我们的小组较早开发并评估了用于眼部递送的原位凝胶和纳米颗粒。为了评估原位凝胶和纳米颗粒对眼部保留的综合作用,我们将它们结合在一起。我们是第一个将此组合称为“纳米颗粒负载原位凝胶”的组合,即掺入壳聚糖原位凝胶中以用于司帕沙星眼科给药的聚乳酸共乙醇酸纳米颗粒。测试了制剂的各种物理化学性质。它显示胶凝pH接近pH 7.2。与市售制剂相比,对于获得的斯巴沙星纳米颗粒原位凝胶(SNG),获得的伽马照相机图像的观察结果表明,在整个角膜前区域具有良好的保留性。由于在全身循环中未观察到放射性,SNG制剂的清除速度非常慢,并且在角膜表面的保留时间更长。发现开发的配方可以更好地结合使用,并可以用于临床评估和应用。关键词:伽玛闪烁显像,原位凝胶,纳米颗粒,载有纳米颗粒的原位凝胶,眼,PLGA,司帕沙星

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