Department of Biosciences and BioEngineering, Indian Institute of Technology Bombay, Bombay, India.
Colloids Surf B Biointerfaces. 2012 May 1;93:161-8. doi: 10.1016/j.colsurfb.2011.12.033. Epub 2012 Jan 3.
Most conventional ophthalmic dosage forms, though simplistic are limited by poor bioavailability in the posterior chamber of the eye. Application of nanotechnology has the potential to overcome this problem. By varying aspirin albumin ratios from 0.06 to 1.0, we obtained electrokinetically stable, pharmacologically active albumin based aspirin nanoparticles of <200 nm diameter with low polydispersity. In vitro release study showed nanoparticle formulation can release aspirin at a sustained rate for prolonged duration (90% at 72 h) and 11% drug release in the posterior chamber over a period of 72 h under simulated condition. Stability of the formulation was well maintained on storage for six months and after reconstitution for 24 h. The formulation showed no hemolysis in contrast to the high hemolysis due to the free drug. This study shows that aspirin loaded albumin nanoparticles prepared by coacervation holds promise as a formulation for topical delivery in diabetic retinopathy.
大多数传统的眼科剂型虽然简单，但由于在后眼房的生物利用度差而受到限制。纳米技术的应用有潜力克服这个问题。通过改变阿司匹林白蛋白比例从 0.06 到 1.0，我们获得了电动力学稳定、具有药理活性的<200nm 直径的、低多分散性的基于白蛋白的阿司匹林纳米颗粒。体外释放研究表明，纳米粒制剂可以以持续的速度释放阿司匹林，延长时间（72 小时时 90%），并且在模拟条件下 72 小时内药物在后房的释放率为 11%。在储存 6 个月和再配制 24 小时后，制剂的稳定性得到了很好的保持。与游离药物引起的高溶血相比，该制剂没有溶血。这项研究表明，通过凝聚作用制备的载阿司匹林白蛋白纳米粒作为糖尿病性视网膜病变的局部递药制剂具有很大的应用前景。
