Add time:07/23/2019         Source:sciencedirect.com

The use of gelatin has been gaining recognition in ocular delivery for its safety profile and biocompatible properties. Timolol Maleate (TM) is an anti-glaucoma drug possessing poor corneal penetration while causing eye irritation making it an ideal candidate for novel nanoparticulate systems. Timolol Maleate loaded Gelatin Nanoparticles (GNPs) were prepared using the double desolvation method utilizing glutaraldehyde as the crosslinking agent. Optimization of the nanoparticles was achieved through a full-factorial design. An optimum formulation possessing particle size of 205 nm, zetapotential of 12.5 mV and an entrapment efficiency of 74.72% was selected. TEM imaging of the optimized nanoparticles was performed and the stability was tracked over 6 months. The in-vitro release studies showed a burst effect followed by a sustained profile. The selected formulae were tested in-vivo and compared to a Timolol marketed product on albino rabbits and were proven superior regarding intraocular pressure lowering and sustained efficacy. The prepared nanoparticles successfully passed Draize irritancy test and showed normal histology. These data indicate that the prepared GNPs possessed all needed qualities of a successful ocular system; corneal affinity, suitable particle size, high entrapment efficiency, sustained release, good stability, efficient lowering of intraocular pressure, high drug bioavailability and lack of irritancy.

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