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G. Mishra, V. M. Tamboli, R. Krishna, A. K. Mitra; Preparation and Charcterization of Bimatoprost Nanoparticles for Sustained Delivery in Glaucoma Therapy. Invest. Ophthalmol. Vis. Sci. 2009;50(13):5964. doi: https://doi.org/.
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To optimize preparation of bimatoprost nanoparticles for sustained delivery in the treatment of glaucoma using different grades of poly (DL-lactide-co-glycolide).
Polymeric nanoparticles of bimatoprost were prepared by single emulsification method using three different grades of poly (DL-lactide-co-glycolide) (PLGA) namely PLGA 75:25, PLGA 65:35 and PLGA 50:50.Briefly polymer and drug were dissolved in methylene chloride and then emulsified in 2.0 % aqueous solution of polyvinyl alcohol (PVA) with the help of a tip sonicator at 60 W for 5 min to form oil in water (o/w) emulsion. Residual organic solvent was removed by evaporation under vacuum and nanoparticles formed were washed three times to remove PVA and unentrapped drug on the surface of nanoparticle. Entrapment efficiency was determined by HPLC. Size was characterized by dynamic light scattering and surface morphology by scanning electron microscopy. In vitro release study was performed using dialysis method in phosphate buffer saline at pH 7.4.
The entrapment efficiency was found to be highest in case of PLGA 75:25 (60.8 % ± 2.5 %). All prepared nanoparticles are in the size range of 200-300 nm. In vitro release of bimatoprost nanoparticles showed that release was sustained for 2 weeks. Moreover, the release of bimatoprost from PLGA 75:25 nanoparticles was much slower than from the nanoparticles prepared using PLGA 65:35 and PLGA 50:50.
Drug delivery using bimatoprost nanoparticles could be a valuable tool for sustained release of drug in the treatment of glaucoma which requires daily drug administration resulting in patient noncompliance.
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